Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
10020353 13776 13 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL1196161 13776 13 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL556024 13776 13 None 12022 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
133538 3562 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
8443 3562 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL574558 3562 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
146025713 171045 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 171045 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025713 171045 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 171045 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 165872 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 165872 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None 95 4 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75202022 170243 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1016/j.ejmech.2022.114378
CHEMBL4453318 170243 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1016/j.ejmech.2022.114378
16219951 171494 1 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL4472022 171494 1 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
75202022 170243 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 170243 2 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
173871 3557 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
936 3557 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL1193571 3557 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/acs.jmedchem.8b00435
46869265 16081 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 16081 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
10742 3560 27 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
1225 3560 27 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL35354 3560 27 None 4 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
92044504 171161 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 171161 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
92044504 171161 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 171161 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
1241 99716 19 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL288090 99716 19 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL552611 99716 19 None 22 3 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/acs.jmedchem.8b00435
44320092 161339 0 None 346 2 Human 9.0 pEC50 = 9.0 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL415080 161339 0 None 346 2 Human 9.0 pEC50 = 9.0 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
167715 2832 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2832 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2832 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
167715 2832 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2832 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2832 12 None -151 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
1242 3556 23 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
935 3556 23 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL286080 3556 23 None 1 3 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/acs.jmedchem.8b00435
10506 2488 15 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
86290953 2488 15 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
CHEMBL3421729 2488 15 None 20 3 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.8b01767
135 168716 117 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
3702506 168716 117 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
CHEMBL441343 168716 117 None - 1 Human 9.0 pEC50 = 9.0 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 138 1 2 2 1.1 O=C(O)c1ccc(O)cc1 10.1021/acs.jmedchem.8b01767
75201961 169063 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4437012 169063 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
75201961 169063 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4437012 169063 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acs.jmedchem.9b00351
146025701 170004 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 170004 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025701 170004 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 170004 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
44320024 106584 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315750 106584 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442480 174698 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
44320050 106348 0 None 1 3 Rat 8.8 pEC50 = 8.8 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 106348 0 None 1 3 Rat 8.8 pEC50 = 8.8 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442480 174698 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
146025715 175622 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4593703 175622 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025715 175622 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4593703 175622 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3[nH]ncc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
122324 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
6077 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
CHEMBL86931 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
122324 203 17 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
6077 203 17 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
CHEMBL86931 203 17 None 4 4 Rat 8.7 pEC50 = 8.7 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm9502100
122324 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
90134269 173634 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 173634 1 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
75201899 171350 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 171350 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
71722299 102007 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397383 102007 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040217 102007 0 None -3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
44282985 119974 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL35426 119974 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
146025707 170541 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4457872 170541 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44320256 204590 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87172 204590 0 None - 1 Human 7.0 pEC50 = 7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
13720688 11449 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180542 11449 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL129634 11449 0 None 1 2 Rat 7.0 pEC50 = 7 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
146025696 169136 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
CHEMBL4437975 169136 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
44331742 4374 0 None - 1 Rat 6.0 pEC50 = 6 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2 10.1021/jm9502100
CHEMBL101617 4374 0 None - 1 Rat 6.0 pEC50 = 6 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2 10.1021/jm9502100
14708665 167642 1 None - 1 Rat 5.0 pEC50 = 5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
CHEMBL43345 167642 1 None - 1 Rat 5.0 pEC50 = 5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
146025696 169136 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
CHEMBL4437975 169136 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 7 5.0 COC(=O)c1cccn2c(-c3ccc(Oc4nccc5occc45)cc3C)cnc12 10.1021/acs.jmedchem.9b00351
146025707 170541 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4457872 170541 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 397 4 0 6 5.7 Cc1cc(N(c2nccc3occc23)C(C)C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
75201901 165872 14 None 95 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165872 14 None 95 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
146034919 191602 2 None - 1 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2cccc(OC(F)F)c2)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5204559 191602 2 None - 1 Human 5.0 pEC50 = 5.0 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2cccc(OC(F)F)c2)cc1 10.1021/acs.jmedchem.2c00949
146025721 171143 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4466769 171143 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
10684715 160093 0 None - 1 Goldfish 8.0 pEC50 = 8.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL41132 160093 0 None - 1 Goldfish 8.0 pEC50 = 8.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
71563083 87144 0 None 19 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335737 87144 0 None 19 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
75201901 165872 14 None 95 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
CHEMBL4277264 165872 14 None 95 4 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
146025721 171143 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4466769 171143 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1c(Oc2nccc3occc23)ccc(-c2cccc3nccn23)c1C 10.1021/acs.jmedchem.9b00351
44276535 97937 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL275379 97937 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
44417647 81749 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 81749 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 81749 0 None -52 3 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
24878061 140879 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 140879 0 None -4 2 Human 6.0 pEC50 = 6.0 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
146025709 174009 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4556763 174009 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
145982261 166179 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4283176 166179 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
146192959 169947 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4449550 169947 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl 10.1021/acsmedchemlett.9b00547
44282985 119974 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL35426 119974 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 279 0 0 3 3.2 CN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
130442557 166520 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4289538 166520 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
146025709 174009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4556763 174009 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 423 4 0 6 6.2 Cc1cc(N(c2nccc3occc23)C2CCCC2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
71722297 101999 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397382 101999 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040156 101999 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
85090332 180137 0 None -9 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 180137 0 None -9 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
90134199 171676 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4474245 171676 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
90134199 171676 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4474245 171676 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 361 5 0 6 5.1 CCOc1ncnc(C)c1-c1ccc(Oc2nccc3occc23)cc1C 10.1021/acs.jmedchem.9b00351
44320303 163415 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420788 163415 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
130442471 175510 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 175510 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
681 1437 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
940 1437 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
947 1437 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
CHEMBL59 1437 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
DB00988 1437 65 None -41 12 Human 6.9 pEC50 = 6.9 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm0604979
44554468 105787 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099225 105787 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139011 105787 0 None -151 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
146025716 173393 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4541632 173393 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44276651 99279 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL284959 99279 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
85090319 180028 0 None -5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 180028 0 None -5 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
130442534 166344 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286177 166344 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
2030130 20779 13 None -6 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 20779 13 None -6 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
146025716 173393 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4541632 173393 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 316 3 0 5 4.2 Cc1cc(Oc2ccccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
145988779 166726 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
CHEMBL4293356 166726 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
44320328 204506 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
CHEMBL86669 204506 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
10689581 99700 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL287931 99700 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
3106 48256 14 None -25 3 Rat 4.9 pEC50 = 4.9 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1021/jm00390a009
CHEMBL15564 48256 14 None -25 3 Rat 4.9 pEC50 = 4.9 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1021/jm00390a009
168278276 190522 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 295 5 1 3 2.6 CNS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187937 190522 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 295 5 1 3 2.6 CNS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
146192950 175457 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F 10.1021/acsmedchemlett.9b00547
CHEMBL4590150 175457 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F 10.1021/acsmedchemlett.9b00547
168280742 190490 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187578 190490 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 230 4 0 2 3.5 O=Cc1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
130442471 175510 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 175510 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
146192960 170953 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4464150 170953 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44320116 163556 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 163556 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
117720272 118309 1 None 18 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
CHEMBL3421730 118309 1 None 18 3 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
1242 3556 23 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
935 3556 23 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
CHEMBL286080 3556 23 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.12.016
146025697 174779 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4574454 174779 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
168276676 189868 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 280 4 0 3 3.1 CS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5178743 189868 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 280 4 0 3 3.1 CS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
146025697 174779 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4574454 174779 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 345 4 1 5 4.1 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc(C(N)=O)c1 10.1021/acs.jmedchem.9b00351
130442561 166340 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286110 166340 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
161665 172016 33 None -28 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 172016 33 None -28 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
85090324 180110 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 180110 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
6603820 95330 13 None 1 7 Human 7.9 pEC50 = 7.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL25856 95330 13 None 1 7 Human 7.9 pEC50 = 7.9 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
146025712 174910 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4577432 174910 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
10666053 99921 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289927 99921 0 None - 1 Goldfish 6.9 pEC50 = 6.9 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
146025703 170701 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4460394 170701 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
75201901 165872 14 None 95 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165872 14 None 95 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
146025703 170701 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
CHEMBL4460394 170701 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 378 3 0 6 4.9 Cc1ncc2nccn2c1-c1cc(F)c(Oc2nccc3occc23)c(F)c1 10.1021/acs.jmedchem.9b00351
15696481 79256 0 None 75 2 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2115213 79256 0 None 75 2 Human 6.9 pEC50 = 6.9 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
146025712 174910 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4577432 174910 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 366 3 0 5 5.4 Cc1cc(Oc2nccc3ccccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
132435 130187 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL130795 130187 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL368456 130187 6 None 8 2 Rat 7.8 pEC50 = 7.8 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
146025704 171782 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4475848 171782 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44554818 103789 0 None -89 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099234 103789 0 None -89 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44554472 105802 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099226 105802 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139040 105802 0 None -1071 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
85090328 180453 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 180453 0 None -6 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090323 181340 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 181340 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
146025813 175014 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175014 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025813 175014 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175014 0 None -2 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90134304 165961 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4278861 165961 1 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b00435
146025821 169104 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169104 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025821 169104 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169104 0 None 100 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025820 172651 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 172651 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025820 172651 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 172651 0 None 6 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
85090329 182100 0 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 182100 0 None -8 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
137364078 191627 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 4 0 3 3.7 CN=S(C)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5204914 191627 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 4 0 3 3.7 CN=S(C)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
3246443 37453 2 None -16 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 37453 2 None -16 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
146025704 171782 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4475848 171782 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 1 6 4.9 Cc1cc(Nc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44320053 204059 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 204059 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
11938 2379 5 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
146192952 2379 5 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4468760 2379 5 None 11 4 Human 7.8 pEC50 = 7.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44287454 13117 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1191276 13117 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL542351 13117 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
146025718 174621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4570859 174621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
117720272 118309 1 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 118309 1 None -18 3 Rat 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of rat D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
146025718 174621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4570859 174621 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 3 1 6 4.2 Cc1cc(Oc2nccc(O)c2C)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
85090333 180719 0 None -10 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 180719 0 None -10 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
76284419 182666 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 182666 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
85090325 179169 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 179169 0 None -3 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
75201901 165872 14 None 95 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b00435
CHEMBL4277264 165872 14 None 95 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b00435
10854877 141483 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL38757 141483 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10733562 146481 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL39266 146481 0 None - 1 Goldfish 6.8 pEC50 = 6.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
1242 3556 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
935 3556 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
CHEMBL286080 3556 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assayAgonist activity at dopamine D1 receptor assessed as [35S]GTPgammaS binding in cell-based assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2012.05.057
136326241 178848 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 178848 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
146192966 174744 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acsmedchemlett.9b00547
CHEMBL4573538 174744 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acsmedchemlett.9b00547
44319988 204359 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85552 204359 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10758745 99967 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 99967 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 99967 0 None - 1 Goldfish 5.8 pEC50 = 5.8 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44276414 97179 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL27101 97179 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
155548298 173179 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4536851 173179 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
44320001 204297 0 None -3 2 Rat 7.7 pEC50 = 7.7 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 204297 0 None -3 2 Rat 7.7 pEC50 = 7.7 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
1242 3556 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
935 3556 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
CHEMBL286080 3556 23 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2014.09.024
146025729 173587 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4546823 173587 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44276652 99034 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL283247 99034 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
146025729 173587 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4546823 173587 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 6 4.9 FC(F)(F)c1cc(Oc2nccn3ccnc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
85090322 178879 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 178879 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090321 182231 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 182231 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
168294420 191912 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccccc2OC(F)F)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5209228 191912 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccccc2OC(F)F)cc1 10.1021/acs.jmedchem.2c00949
6603820 95330 13 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 95330 13 None 1 7 Human 7.7 pEC50 = 7.7 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
44554820 105805 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099222 105805 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139044 105805 0 None -31 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
146025724 171698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4474567 171698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025819 175079 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4581262 175079 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025819 175079 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4581262 175079 0 None 3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 385 2 0 5 3.9 CC(=O)Oc1c(Cl)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025724 171698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4474567 171698 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 363 3 0 5 5.2 Fc1cc(-c2cccc3nccn23)cc(F)c1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
85090334 180043 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 180043 0 None -11 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090331 180871 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 180871 0 None -6 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
12668019 10143 6 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL1160787 10143 6 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
44320061 105552 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313304 105552 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
14809027 106546 0 None 3 3 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 106546 0 None 3 3 Human 8.7 pEC50 = 8.7 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
122324 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None -4 4 Human 8.7 pEC50 = 8.7 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
146025727 171119 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025727 171119 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 171342 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 171342 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10506 2488 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 2488 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 2488 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
130442473 166783 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 166783 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 166783 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 166783 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
1153 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
12668023 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026874 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026875 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
3341 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
6603851 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
933 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
939 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
985 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1160786 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1161520 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL588 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
DB00800 1598 53 None 6 6 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as reversal of Ro 20-1724 mediated decrease in cAMP accumulation after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
681 1437 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
940 1437 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
947 1437 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
CHEMBL59 1437 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
DB00988 1437 65 None -41 12 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2010.07.052
75201899 171350 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1016/j.ejmech.2022.114378
CHEMBL4469983 171350 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1016/j.ejmech.2022.114378
201536 110980 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 110980 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
201536 110980 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL3276140 110980 4 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 351 2 0 5 3.3 CC(=O)Oc1ccc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
133741 197388 8 None -38 2 Rat 4.7 pEC50 = 4.7 Functional
Dopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
CHEMBL587 197388 8 None -38 2 Rat 4.7 pEC50 = 4.7 Functional
Dopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
90134211 173457 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4543306 173457 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
71722293 102002 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL2397380 102002 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL3040164 102002 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
44554984 103786 0 None -208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099231 103786 0 None -208 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155541775 172475 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
CHEMBL4519136 172475 0 None 1 2 Human 6.7 pEC50 = 6.7 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
137364059 189726 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 3.4 C[S+]([O-])c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5176312 189726 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 3.4 C[S+]([O-])c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
168289194 190898 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 4.5 O=Cc1ccc(-c2ccccc2SC(F)F)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5193714 190898 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 264 4 0 2 4.5 O=Cc1ccc(-c2ccccc2SC(F)F)cc1 10.1021/acs.jmedchem.2c00949
10662054 83991 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114444 83991 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219803 83991 0 None - 1 Goldfish 7.7 pEC50 = 7.7 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
90134211 173457 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4543306 173457 1 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 332 3 1 6 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1nc(N)cnc1C 10.1021/acs.jmedchem.9b00351
155519631 169837 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
CHEMBL4448100 169837 0 None 15 2 Human 7.7 pEC50 = 7.7 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
145979741 166132 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4282096 166132 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
6917970 3635 54 None 40 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
8370 3635 54 None 40 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
CHEMBL487387 3635 54 None 40 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assayAgonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
44276412 97216 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL27117 97216 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44320116 163556 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 163556 0 None -1 3 Rat 7.6 pEC50 = 7.6 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44554649 103790 0 None -457 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099235 103790 0 None -457 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44276557 98858 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL282136 98858 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
21936384 190916 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccc(OC(F)F)cc2)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5193924 190916 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 248 4 0 2 3.8 O=Cc1ccc(-c2ccc(OC(F)F)cc2)cc1 10.1021/acs.jmedchem.2c00949
681 1437 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
940 1437 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
947 1437 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
CHEMBL59 1437 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
DB00988 1437 65 None -41 12 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
15696482 79149 0 None 21 2 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2114209 79149 0 None 21 2 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
85090326 182191 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 182191 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
44320218 204698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
CHEMBL87897 204698 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
146025811 171195 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171195 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025811 171195 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171195 0 None -416 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10640108 83990 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114441 83990 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219802 83990 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
9841398 99058 3 None -2 3 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL28338 99058 3 None -2 3 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
44320267 204490 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 204490 0 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10588327 13669 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1195441 13669 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL554571 13669 0 None - 1 Goldfish 6.6 pEC50 = 6.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
145990190 166300 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4285528 166300 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
85090337 182699 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 182699 0 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
21786101 155191 0 None -38 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
CHEMBL405519 155191 0 None -38 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21 10.1016/j.bmc.2007.06.036
1241 99716 19 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
CHEMBL288090 99716 19 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
CHEMBL552611 99716 19 None -22 3 Rat 7.6 pEC50 = 7.6 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00384a006
228 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
33 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
CHEMBL53 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
DB00714 441 26 None -10 8 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
155541775 172475 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
CHEMBL4519136 172475 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1 10.1021/acs.jmedchem.8b01767
145979741 166132 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b00435
CHEMBL4282096 166132 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulationAgonist activity at dopamine D1 receptor (unknown origin) assessed as increase in cAMP accumulation
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b00435
145979741 166132 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1016/j.ejmech.2022.114378
CHEMBL4282096 166132 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation by HTRF assay
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1016/j.ejmech.2022.114378
4901726 180217 9 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 180217 9 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
146025714 169730 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4446525 169730 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025714 169730 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4446525 169730 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 7 3.8 Cc1cc(Oc2nccn3ccnc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 166783 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4294397 166783 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
146025730 171402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4470740 171402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025730 171402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4470740 171402 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 4 5.2 FC(F)(F)c1cc(Oc2ccccn2)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
9796958 146045 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 146045 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 146045 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 146045 0 None 4 2 Goldfish 5.6 pEC50 = 5.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44320304 106552 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1 10.1021/jm00112a034
CHEMBL315516 106552 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1 10.1021/jm00112a034
85090318 178865 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 178865 0 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
10758744 100041 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL291100 100041 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
10710466 155874 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL40667 155874 0 None - 1 Goldfish 7.6 pEC50 = 7.6 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
2407 3320 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
59227 3320 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
941 3320 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
CHEMBL1303 3320 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
DB05271 3320 73 None -11 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1016/j.bmc.2013.11.012
146192958 169946 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4449549 169946 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl 10.1021/acsmedchemlett.9b00547
146192964 174138 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4559891 174138 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acsmedchemlett.9b00547
10519435 170903 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL446350 170903 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
15981509 141426 1 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 141426 1 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
10856744 59710 10 None 6 2 Rat 6.5 pEC50 = 6.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
ChEMBL 210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12 10.1021/jm00390a009
CHEMBL17357 59710 10 None 6 2 Rat 6.5 pEC50 = 6.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
ChEMBL 210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12 10.1021/jm00390a009
85090330 180491 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 180491 0 None -7 2 Human 6.5 pEC50 = 6.5 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
10506 2488 15 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 2488 15 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 2488 15 None 20 3 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
44320050 106348 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 106348 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44320357 204673 0 None 54 2 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87734 204673 0 None 54 2 Human 8.5 pEC50 = 8.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86293768 118310 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421836 118310 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
228 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6604773 16082 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2 10.1016/j.bmc.2010.07.052
CHEMBL1224528 16082 1 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2 10.1016/j.bmc.2010.07.052
228 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -10 8 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6852376 91167 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL1467585 91167 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL24077 91167 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
CHEMBL503958 91167 11 None -1 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2007.06.036
6603820 95330 13 None -1 7 Rat 7.5 pEC50 = 7.5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
CHEMBL25856 95330 13 None -1 7 Rat 7.5 pEC50 = 7.5 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9502100
145867041 173957 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4555682 173957 3 None - 1 Human 7.5 pEC50 = 7.5 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in CHO cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
44320327 162872 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 162872 0 None 1 2 Rat 7.5 pEC50 = 7.5 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
1242 3556 23 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 3556 23 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 3556 23 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assayAgonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
137364067 190481 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 5 1 3 4.1 CCS(=N)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5187471 190481 0 None - 1 Human 4.5 pEC50 = 4.5 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 293 5 1 3 4.1 CCS(=N)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
10709445 100893 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 100893 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 100893 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
3033200 173955 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173955 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
3033200 173955 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173955 5 None -616 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
117720272 118309 1 None -34 3 Mouse 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 118309 1 None -34 3 Mouse 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of mouse D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
71722291 101987 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397385 101987 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040059 101987 0 None -4 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
146025708 172952 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4531083 172952 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
25142456 81994 2 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 81994 2 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP productionActivity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
146025708 172952 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4531083 172952 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 409 5 0 6 5.7 Cc1cc(N(CC2CC2)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44276404 98621 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL28054 98621 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
10802235 13148 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1191487 13148 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL542593 13148 0 None - 1 Goldfish 5.5 pEC50 = 5.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
10732044 83992 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114440 83992 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219804 83992 0 None - 1 Goldfish 7.5 pEC50 = 7.5 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
75201901 165872 14 None 95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165872 14 None 95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
44554474 105804 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099227 105804 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139043 105804 0 None -301 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155519631 169837 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to controlPositive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to control
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
CHEMBL4448100 169837 0 None -15 2 Rat 6.5 pEC50 = 6.5 Functional
Positive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to controlPositive allosteric modulation of rat D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation relative to control
ChEMBL 421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12 10.1021/acs.jmedchem.8b01767
146025818 169195 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4438800 169195 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44320076 204700 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87910 204700 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
681 1437 65 None -41 12 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
940 1437 65 None -41 12 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
947 1437 65 None -41 12 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
CHEMBL59 1437 65 None -41 12 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
DB00988 1437 65 None -41 12 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2007.06.036
146025706 171058 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4465592 171058 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
681 1437 65 None -1380 12 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
940 1437 65 None -1380 12 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
947 1437 65 None -1380 12 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
CHEMBL59 1437 65 None -1380 12 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
DB00988 1437 65 None -1380 12 Rat 5.5 pEC50 = 5.5 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00390a009
146025818 169195 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4438800 169195 0 None 3 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 429 2 0 5 4.1 CC(=O)Oc1c(Br)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025706 171058 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4465592 171058 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 383 4 0 6 5.3 CCN(c1ccc(-c2c(C)ncc3nccn23)c(C)c1)c1nccc2occc12 10.1021/acs.jmedchem.9b00351
44555137 103787 0 None -28 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099232 103787 0 None -28 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
155537335 171746 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 388 2 1 6 3.2 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1nccc2occc12 10.1021/acsmedchemlett.9b00050
CHEMBL4475239 171746 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 388 2 1 6 3.2 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1nccc2occc12 10.1021/acsmedchemlett.9b00050
681 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
940 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
947 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
CHEMBL59 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
DB00988 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2011.07.057
44320002 106558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315535 106558 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44276556 99241 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL284644 99241 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
146025814 172210 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 172210 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
6852376 91167 11 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL1467585 91167 11 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL24077 91167 11 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL503958 91167 11 None -1 4 Human 6.4 pEC50 = 6.4 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
1242 3556 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
935 3556 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
CHEMBL286080 3556 23 None 1 3 Human 6.4 pEC50 = 6.4 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
146025814 172210 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 172210 0 None 6 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10540201 99765 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL288536 99765 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
681 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
940 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
947 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
CHEMBL59 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
DB00988 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.11.012
44320267 204490 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 204490 0 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44555138 103788 0 None -117 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099233 103788 0 None -117 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
49866139 16076 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CO2 10.1016/j.bmc.2010.07.052
CHEMBL1224452 16076 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CO2 10.1016/j.bmc.2010.07.052
1218 3559 24 None -177 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 3559 24 None -177 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 3559 24 None -177 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
44554987 103791 0 None -114 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099239 103791 0 None -114 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
13720694 12863 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1189465 12863 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL538785 12863 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
13720690 12979 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1190300 12979 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL540575 12979 0 None -1 2 Rat 6.4 pEC50 = 6.4 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1 10.1021/jm00384a006
155521159 169963 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 374 2 1 6 2.9 Cc1c(-c2ccc3c(c2)CCN3c2nccc3occc23)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
CHEMBL4449782 169963 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 374 2 1 6 2.9 Cc1c(-c2ccc3c(c2)CCN3c2nccc3occc23)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
6917970 3635 54 None -2454 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
8370 3635 54 None -2454 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
CHEMBL487387 3635 54 None -2454 3 Rat 4.4 pEC50 = 4.4 Functional
Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activityAgonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
90134304 165961 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
CHEMBL4278861 165961 1 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
85090339 181723 0 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
CHEMBL4784143 181723 0 None -8 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
10518837 100007 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290842 100007 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
76284418 181736 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4784295 181736 0 None -1 2 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090320 181981 0 None -10 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4787728 181981 0 None -10 2 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
53494980 66161 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1822918 66161 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1852340 66161 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
10830234 99912 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289867 99912 0 None - 1 Goldfish 7.4 pEC50 = 7.4 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
681 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1437 65 None -41 12 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
86302251 172286 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 448 4 1 5 3.5 CN(Cc1nc2cc(Br)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
CHEMBL4514994 172286 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 448 4 1 5 3.5 CN(Cc1nc2cc(Br)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
155549423 173241 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 349 3 2 7 2.3 Cc1c(-c2ccc(Nc3nccc4occc34)nc2)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
CHEMBL4538358 173241 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 349 3 2 7 2.3 Cc1c(-c2ccc(Nc3nccc4occc34)nc2)n(C)c(=O)[nH]c1=O 10.1021/acsmedchemlett.9b00050
44320327 162872 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 162872 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
85470885 174088 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 438 4 1 5 3.8 CN(Cc1nc2cc(C(F)(F)F)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
CHEMBL4558647 174088 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assayPositive allosteric modulation of human D1R expressed in CHO cells assessed as 2-fold increase in dopamine-induced cAMP accumulation preincubated for 10 mins followed by dopamine addition and measured after 20 mins by fluorescence assay
ChEMBL 438 4 1 5 3.8 CN(Cc1nc2cc(C(F)(F)F)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21 10.1021/acs.jmedchem.8b01767
10081286 98319 2 None 1 2 Rat 5.3 pEC50 = 5.3 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effectDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effect
ChEMBL 192 2 3 3 0.4 NCCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
CHEMBL278188 98319 2 None 1 2 Rat 5.3 pEC50 = 5.3 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effectDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effect
ChEMBL 192 2 3 3 0.4 NCCc1ccc(O)c2c1CC(=O)N2 10.1021/jm00390a009
10588326 158320 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL40950 158320 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
10831251 162623 0 None - 1 Goldfish 6.3 pEC50 = 6.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL41809 162623 0 None - 1 Goldfish 6.3 pEC50 = 6.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
13864380 204706 1 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87958 204706 1 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
13864381 206603 3 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL542683 206603 3 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL99361 206603 3 None 5 3 Human 6.3 pEC50 = 6.3 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
44331310 106882 1 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9502100
CHEMBL317741 106882 1 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9502100
168291403 191408 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 281 4 1 3 2.3 NS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
CHEMBL5201584 191408 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 281 4 1 3 2.3 NS(=O)(=O)c1ccc(-c2ccccc2OCF)cc1 10.1021/acs.jmedchem.2c00949
71563084 87143 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335736 87143 0 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
64638 105661 1 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313530 105661 1 None 1 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
6603703 206 7 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm9502100
9637 206 7 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm9502100
CHEMBL291143 206 7 None -1 4 Rat 8.3 pEC50 = 8.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm9502100
44320001 204297 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 204297 0 None 3 2 Human 8.3 pEC50 = 8.3 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86764103 131915 7 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL3697578 131915 7 None 2 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
6453963 71195 8 None 10000 2 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1950491 71195 8 None 10000 2 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
CHEMBL1962947 71195 8 None 10000 2 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmcl.2012.01.005
130442590 169232 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 169232 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
130442590 169232 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 169232 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
44320026 204379 0 None 131 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85689 204379 0 None 131 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
117720272 118309 1 None 18 3 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL3421730 118309 1 None 18 3 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assayPositive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay
ChEMBL 421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
10851849 169366 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL44414 169366 0 None - 1 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
13720686 11455 0 None 3 2 Rat 7.3 pEC50 = 7.3 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL1180562 11455 0 None 3 2 Rat 7.3 pEC50 = 7.3 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
CHEMBL131313 11455 0 None 3 2 Rat 7.3 pEC50 = 7.3 Functional
Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclaseDopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
ChEMBL 389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1 10.1021/jm00384a006
681 1437 65 None -1380 12 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
940 1437 65 None -1380 12 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
947 1437 65 None -1380 12 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
CHEMBL59 1437 65 None -1380 12 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
DB00988 1437 65 None -1380 12 Rat 5.3 pEC50 = 5.3 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9502100
146025816 169411 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 169411 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
146025816 169411 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 169411 0 None -2 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
9796958 146045 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 146045 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 146045 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 146045 0 None 4 2 Goldfish 7.3 pEC50 = 7.3 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
228 441 26 None -10 8 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
33 441 26 None -10 8 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
6005 441 26 None -10 8 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
CHEMBL53 441 26 None -10 8 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
DB00714 441 26 None -10 8 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2007.06.036
44320053 204059 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 204059 0 None -3 2 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
146025720 172379 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4517022 172379 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025720 172379 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4517022 172379 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 341 3 0 5 5.2 Cc1cc(-c2cccc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025700 174800 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4574838 174800 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
146192953 171044 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1ccc(F)cc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4465386 171044 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1ccc(F)cc1Cl 10.1021/acsmedchemlett.9b00547
145992269 166400 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
CHEMBL4287192 166400 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
146025700 174800 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
CHEMBL4574838 174800 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 370 3 0 6 5.3 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)c(C)c1C 10.1021/acs.jmedchem.9b00351
85090335 180532 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
CHEMBL4760355 180532 0 None 1 2 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
6852376 91167 11 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
CHEMBL1467585 91167 11 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
CHEMBL24077 91167 11 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
CHEMBL503958 91167 11 None -1 4 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2011.07.057
145867041 173957 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4555682 173957 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Positive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulationPositive allosteric modulation of human D1R expressed in HEK cells assessed as increase in dopamine-induced cAMP accumulation
ChEMBL 421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl 10.1021/acs.jmedchem.8b01767
1153 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
12668023 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
30026874 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
30026875 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
3341 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
6603851 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
933 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
939 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
985 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
CHEMBL1160786 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
CHEMBL1161520 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
CHEMBL588 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
DB00800 1598 53 None -6 6 Rat 7.2 pEC50 = 7.2 Functional
Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranesDopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00390a009
53494976 66267 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1822919 66267 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1852625 66267 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
155560177 174358 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 378 3 1 6 2.7 Cc1nc2c(c(Oc3ccc(-c4c(C)c(=O)[nH]c(=O)n4C)c(C)c3)n1)CCC2 10.1021/acsmedchemlett.9b00050
CHEMBL4565185 174358 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 378 3 1 6 2.7 Cc1nc2c(c(Oc3ccc(-c4c(C)c(=O)[nH]c(=O)n4C)c(C)c3)n1)CCC2 10.1021/acsmedchemlett.9b00050
53494978 66169 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1822920 66169 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
CHEMBL1852349 66169 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2 10.1016/j.bmc.2011.07.057
44320129 167331 0 None 56 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL431220 167331 0 None 56 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44319976 106480 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
CHEMBL315005 106480 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
44320378 204343 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85409 204343 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10015860 98820 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL281932 98820 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
12170 3847 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 10.1021/acs.jmedchem.2c00949
137364063 3847 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 10.1021/acs.jmedchem.2c00949
CHEMBL5172089 3847 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Positive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assayPositive allosteric modulation of human D1R expressed in SK-N-MC cells assessed as inhibition of DA-induced cAMP production pretreated with compound for 15 mins followed by dopamine EC70 addition measured after 15 mins by HTRF assay
ChEMBL 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 10.1021/acs.jmedchem.2c00949
146025699 169919 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4449153 169919 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
146025710 169549 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4443737 169549 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025699 169919 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
CHEMBL4449153 169919 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 356 3 0 6 4.9 Cc1cc(-c2c(C)ncc3nccn23)ccc1Oc1nccc2occc12 10.1021/acs.jmedchem.9b00351
155534541 171407 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 380 4 2 6 2.5 CC(=O)Nc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 10.1021/acsmedchemlett.9b00050
CHEMBL4470808 171407 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 380 4 2 6 2.5 CC(=O)Nc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 10.1021/acsmedchemlett.9b00050
146025710 169549 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4443737 169549 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 396 4 0 6 5.8 Cc1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
10506 2488 15 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
86290953 2488 15 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
CHEMBL3421729 2488 15 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 10.1021/acs.jmedchem.9b01234
44276405 99647 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
CHEMBL287513 99647 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
130442514 165979 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4279267 165979 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
10666423 161752 0 None - 1 Goldfish 6.2 pEC50 = 6.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 363 1 3 4 4.7 Cc1cccc(-c2cc3c(s2)CN[C@H]2CCc4cc(O)c(O)cc4[C@H]32)c1 10.1021/jm970038v
CHEMBL416435 161752 0 None - 1 Goldfish 6.2 pEC50 = 6.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 363 1 3 4 4.7 Cc1cccc(-c2cc3c(s2)CN[C@H]2CCc4cc(O)c(O)cc4[C@H]32)c1 10.1021/jm970038v
146025719 170641 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4459395 170641 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025719 170641 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4459395 170641 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 399 4 0 6 5.2 Cc1cc(Oc2cc(N3CCCCC3)ccn2)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44319915 204249 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84557 204249 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
146025726 170200 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4452764 170200 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025823 169010 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 169010 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
1242 3556 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 minsAgonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2019.04.014
935 3556 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 minsAgonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2019.04.014
CHEMBL286080 3556 23 None 1 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 minsAgonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in cAMP accumulation measured after 30 mins
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2019.04.014
146025823 169010 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 169010 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
146025726 170200 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4452764 170200 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 405 3 0 4 6.4 FC(F)(F)c1cc(Oc2nccc3ccccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44320123 106599 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL315849 106599 0 None 4 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
15696487 163247 1 None 97 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420604 163247 1 None 97 2 Human 7.2 pEC50 = 7.2 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10758745 99967 0 None - 1 Goldfish 7.2 pEC50 = 7.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 99967 0 None - 1 Goldfish 7.2 pEC50 = 7.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 99967 0 None - 1 Goldfish 7.2 pEC50 = 7.2 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
14809027 106546 0 None -3 3 Rat 8.2 pEC50 = 8.2 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 106546 0 None -3 3 Rat 8.2 pEC50 = 8.2 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
6603820 95330 13 None 1 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2011.07.057
CHEMBL25856 95330 13 None 1 7 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2011.07.057
146025728 175440 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4589664 175440 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025728 175440 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4589664 175440 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 394 3 0 5 5.5 FC(F)(F)c1cc(Oc2nccn3cccc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
6604005 156575 2 None 1 4 Rat 6.2 pEC50 = 6.2 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm9502100
CHEMBL407489 156575 2 None 1 4 Rat 6.2 pEC50 = 6.2 Functional
Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activityEffective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm9502100
133642 171385 9 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 171385 9 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
133642 171385 9 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 171385 9 None -9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
44554986 105803 0 None -35 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099236 105803 0 None -35 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3139041 105803 0 None -35 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
71722301 102000 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3040157 102000 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3216146 102000 0 None -4 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
130442508 170516 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
CHEMBL4457399 170516 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
71563082 86853 0 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2331599 86853 0 None -5 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
86293768 118310 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
CHEMBL3421836 118310 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assayPositive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.9b01234
10664137 162205 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL417164 162205 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
130442508 170516 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
CHEMBL4457399 170516 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 346 4 0 5 5.3 COc1ccc(-c2ccc(Oc3nccc4occc34)cc2C)c(C)n1 10.1021/acs.jmedchem.9b00351
146025725 170983 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4464545 170983 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
146025725 170983 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4464545 170983 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 435 4 0 5 6.8 FC(F)(F)c1cc(Oc2nccc3occ(C4CC4)c23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
71722295 101994 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397381 101994 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040115 101994 0 None -1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 minsAgonist activity at human dopamine D1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 15 mins
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
10546132 160708 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL41196 160708 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
146025711 172463 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4518891 172463 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025711 172463 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4518891 172463 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2cccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
71562964 87147 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335740 87147 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamineAgonist activity at dopamine D1 receptor (unknown origin) transfected in CHO cell membranes assessed as increase in cAMP level after 8 mins by flash plate assay in presence of dopamine
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
6603703 206 7 None -2 4 Goldfish 8.1 pEC50 = 8.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
9637 206 7 None -2 4 Goldfish 8.1 pEC50 = 8.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
CHEMBL291143 206 7 None -2 4 Goldfish 8.1 pEC50 = 8.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
64638 105661 1 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313530 105661 1 None -1 2 Rat 8.1 pEC50 = 8.1 Functional
Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatumInhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44276551 96927 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL26965 96927 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44276552 99418 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL285924 99418 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
10497993 167909 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL43514 167909 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
44276572 96200 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL26365 96200 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
75201961 169063 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
CHEMBL4437012 169063 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
146192955 170960 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 409 4 1 4 3.8 C[C@H]1c2cccc(-c3cnn(C)c3)c2C[C@H](CO)N1C(=O)Cc1ccccc1Cl 10.1021/acsmedchemlett.9b00547
CHEMBL4464215 170960 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assayPositive allosteric modulation of human D1 receptor expressed in HEK293 assessed as cAMP production incubated for 60 mins by HTRF assay
ChEMBL 409 4 1 4 3.8 C[C@H]1c2cccc(-c3cnn(C)c3)c2C[C@H](CO)N1C(=O)Cc1ccccc1Cl 10.1021/acsmedchemlett.9b00547
10519436 11122 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1178784 11122 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL41238 11122 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
118445551 166761 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
CHEMBL4294009 166761 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
13851595 173933 2 None -489 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3098131 173933 2 None -489 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL455497 173933 2 None -489 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
85090338 180179 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4756163 180179 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in HEK293 cells assessed as potentiation of dopamine-induced cAMP accumulation by measuring dopamine EC50 at 50 uM measured after 30 mins by HitHunter assay (Rvb = 214 nM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
14809026 204073 2 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL83080 204073 2 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
14809026 204073 2 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL83080 204073 2 None -2 2 Human 5.1 pEC50 = 5.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10684714 99846 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115372 99846 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL289283 99846 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
146025817 175444 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 175444 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025817 175444 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 175444 0 None 66 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
6603820 95330 13 None -6 7 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL25856 95330 13 None -6 7 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
10592479 99801 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL288846 99801 0 None - 1 Goldfish 7.1 pEC50 = 7.1 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
146025705 170047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4450916 170047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
44554982 103785 0 None -58 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
CHEMBL3099230 103785 0 None -58 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 minsAgonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins
ChEMBL 327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21 10.1016/j.bmc.2013.11.012
44320257 204455 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86325 204455 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Concentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retinaConcentration required to inhibit 50% dopamine receptor D1 activity using cell free homogenate of carp retina
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
146025705 170047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4450916 170047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assayAgonist activity at recombinant human D1 receptor expressed in HEK29T cells assessed as induction of stimulatory G-protein-mediated cAMP accumulation measured after 15 mins by Glosensor-based FLIPR assay
ChEMBL 369 3 0 6 4.9 Cc1cc(N(C)c2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
90142280 166743 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4293757 166743 1 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assayAgonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
9841398 99058 3 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL28338 99058 3 None 2 3 Human 8.1 pEC50 = 8.1 Functional
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
10546131 99943 0 None - 1 Goldfish 7.0 pEC50 = 7.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290149 99943 0 None - 1 Goldfish 7.0 pEC50 = 7.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
6852376 91167 11 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL1467585 91167 11 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL24077 91167 11 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL503958 91167 11 None -16 4 Goldfish 6.0 pEC50 = 6.0 Functional
Ability to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissueAbility to stimulate the Dopamine receptor D1 like was assayed by measuring cAMP production in cell free homogenates of goldfish retinal tissue
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
155558060 174112 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 414 4 1 6 3.0 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1ncccc1OC(F)F 10.1021/acsmedchemlett.9b00050
CHEMBL4559240 174112 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay
ChEMBL 414 4 1 6 3.0 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1ncccc1OC(F)F 10.1021/acsmedchemlett.9b00050
146025822 173219 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4537900 173219 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025822 173219 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4537900 173219 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAgonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 393 3 0 5 4.4 CC(=O)Oc1c(C(C)C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
107930 1500 20 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
3304 1500 20 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
CHEMBL298406 1500 20 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
DB12273 1500 20 None 10471 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127305
3036864 201066 16 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1256645 201066 16 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1814790 201066 16 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL62 201066 16 None -6 6 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulationAntagonist activity at human recombinant at D1 receptor assessed as inhibition of dopamine-induced cAMP accumulation
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
155561845 175145 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL4582377 175145 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
15061351 86052 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 367 2 0 6 3.0 COc1ccc2c(c1OC(C)=O)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL2314734 86052 0 None -2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 367 2 0 6 3.0 COc1ccc2c(c1OC(C)=O)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
71453989 83115 0 None -1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 298 0 0 4 4.0 Cn1c2cnc1OCC/C=C\CCCCOc1ccccc1-2 10.1021/jm1012374
CHEMBL2203622 83115 0 None -1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
ChEMBL 298 0 0 4 4.0 Cn1c2cnc1OCC/C=C\CCCCOc1ccccc1-2 10.1021/jm1012374
70682088 75715 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057446 75715 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
46931072 200360 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL608530 200360 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
3246545 200787 1 None -3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 200787 1 None -3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 200787 1 None -3 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
70690500 75720 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057455 75720 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
155538443 171816 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL4476383 171816 0 None -2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.bmc.2019.04.014
146025811 171195 0 None -416 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171195 0 None -416 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
1353 1880 85 None -199 27 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
3559 1880 85 None -199 27 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
86 1880 85 None -199 27 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
CHEMBL54 1880 85 None -199 27 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
DB00502 1880 85 None -199 27 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
72301 185536 72 None -3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2019.04.014
CHEMBL487182 185536 72 None -3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2019.04.014
44299467 195879 0 None -30 2 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
CHEMBL57029 195879 0 None -30 2 Rat 5.8 pIC50 = 5.8 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
3246443 37453 2 None -16 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 37453 2 None -16 3 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
44537919 196459 0 None -60 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574700 196459 0 None -60 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
72699716 114691 0 None -12 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344459 114691 0 None -12 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
161665 172016 33 None -28 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 172016 33 None -28 3 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
70690498 75714 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057445 75714 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
13869636 101235 0 None -83 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 397 8 0 4 4.7 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1021/jm00393a037
CHEMBL299471 101235 0 None -83 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 397 8 0 4 4.7 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1021/jm00393a037
44299213 100166 0 None -77 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@@H]1C 10.1021/jm00393a037
CHEMBL292006 100166 0 None -77 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@@H]1C 10.1021/jm00393a037
44299579 196042 0 None -33 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
CHEMBL57140 196042 0 None -33 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 355 6 1 3 4.0 C[C@@H]1CN(CCCC(=O)c2ccc(F)cc2)CCC1(O)c1ccccc1 10.1021/jm00393a037
18367 193274 24 None -60 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 341 6 1 3 3.8 O=C(CCCN1CCC(O)(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
CHEMBL54206 193274 24 None -60 2 Rat 5.6 pIC50 = 5.6 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 341 6 1 3 3.8 O=C(CCCN1CCC(O)(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
3036864 201066 16 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
CHEMBL1256645 201066 16 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
CHEMBL1814790 201066 16 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
CHEMBL62 201066 16 None -6 6 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2019.04.014
3036864 201066 16 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
CHEMBL1256645 201066 16 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
CHEMBL1814790 201066 16 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
CHEMBL62 201066 16 None -6 6 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2014.09.024
44299566 195103 0 None -67 2 Rat 5.5 pIC50 = 5.5 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@H]1C 10.1021/jm00393a037
CHEMBL56547 195103 0 None -67 2 Rat 5.5 pIC50 = 5.5 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 411 8 0 4 5.0 CCC(=O)OC1(c2ccccc2)CCN(CCCC(=O)c2ccc(F)cc2)C[C@H]1C 10.1021/jm00393a037
44537925 197067 0 None -162 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL582945 197067 0 None -162 3 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393Antagonist activity at dopamine D1 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay in presence of SKF-38393
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
129103318 166760 0 None -39 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assayAntagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 166760 0 None -39 6 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assayAntagonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced cAMP accumulation preincubated for 15 mins followed by dopamine induction and measured after 30 mins by HTRF assay
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
228 441 26 None -131 8 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
33 441 26 None -131 8 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
6005 441 26 None -131 8 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
CHEMBL53 441 26 None -131 8 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
DB00714 441 26 None -131 8 Rat 6.4 pIC50 = 6.4 Functional
Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.Affinity of the Compound for Dopamine D1 receptor in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]SCH-23390 as ligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(00)80249-8
146025812 174319 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 174319 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025812 174319 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 174319 0 None -1 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90899701 169168 0 None -5 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 313 1 3 5 2.5 COc1ccc2c(c1O)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
CHEMBL4438471 169168 0 None -5 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 313 1 3 5 2.5 COc1ccc2c(c1O)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
453215 86054 3 None 7 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)C1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2019.04.014
CHEMBL2314745 86054 3 None 7 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)C1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2019.04.014
3246545 200787 1 None -3 3 Human 6.3 pIC50 = 6.3 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 200787 1 None -3 3 Human 6.3 pIC50 = 6.3 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 200787 1 None -3 3 Human 6.3 pIC50 = 6.3 Functional
Antagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assayAntagonism of D1 dopamine receptor of human was determined in C6D1 low-density cells by using cyclic AMP assay
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
146025813 175014 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175014 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025813 175014 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175014 0 None -2 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
3036864 201066 16 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1256645 201066 16 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1814790 201066 16 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL62 201066 16 None -6 6 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assayAntagonist activity at dopamine D1 receptor assessed as inhibition of [35S]GTPgammaS binding in cell-based assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
1353 1880 85 None -199 27 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
3559 1880 85 None -199 27 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
86 1880 85 None -199 27 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
CHEMBL54 1880 85 None -199 27 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
DB00502 1880 85 None -199 27 Rat 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00393a037
3036864 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
3036864 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 201066 16 None -6 6 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
72699817 114690 0 None 1 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344458 114690 0 None 1 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393Antagonist activity at D1 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay in presence of SKF38393
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
5018 3493 8 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
943 3493 8 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
946 3493 8 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
CHEMBL13668 3493 8 None -42 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity at dopamine D1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
12269810 86055 5 None -15 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 327 2 2 5 2.8 COc1ccc2c(c1OC)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
CHEMBL2314747 86055 5 None -15 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 327 2 2 5 2.8 COc1ccc2c(c1OC)CN1CCc3cc(O)c(O)cc3C1C2 10.1016/j.bmc.2019.04.014
24837531 174202 1 None -4 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 311 2 1 4 3.1 COc1cc2c(cc1OC)C1Cc3ccc(O)cc3CN1CC2 10.1016/j.bmc.2019.04.014
CHEMBL4561303 174202 1 None -4 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 311 2 1 4 3.1 COc1cc2c(cc1OC)C1Cc3ccc(O)cc3CN1CC2 10.1016/j.bmc.2019.04.014
9549058 172579 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.bmc.2019.04.014
CHEMBL4521450 172579 0 None 3 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.bmc.2019.04.014
146025814 172210 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 172210 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
155552483 173487 0 None -6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 2 1 6 2.8 COc1cc2c(c(OC)c1O)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
CHEMBL4544045 173487 0 None -6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 minsAntagonist activity at D1 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of SKF38393-induced cAMP accumulation measured after 30 mins
ChEMBL 355 2 1 6 2.8 COc1cc2c(c(OC)c1O)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2019.04.014
146025814 172210 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 172210 0 None 6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
13869644 195576 0 None -109 2 Rat 5.1 pIC50 = 5.1 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 325 6 0 2 4.7 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
CHEMBL56843 195576 0 None -109 2 Rat 5.1 pIC50 = 5.1 Functional
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
ChEMBL 325 6 0 2 4.7 O=C(CCCN1CCC(c2ccccc2)CC1)c1ccc(F)cc1 10.1021/jm00393a037
146025815 169212 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 169212 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
146025815 169212 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 169212 0 None -33 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assayAntagonist activity at D1R (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
156017431 177203 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643069 177203 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assayAntagonist activity at human dopamine D1 receptor expressed in CHO-K1 cells by cAMP Hunter assay
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
11681599 74823 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 74823 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
133538 3562 17 None - 1 Human 8.9 pKi = 8.9 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
8443 3562 17 None - 1 Human 8.9 pKi = 8.9 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
CHEMBL574558 3562 17 None - 1 Human 8.9 pKi = 8.9 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
11558055 72805 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL1204122 72805 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 72805 1 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11573628 74350 0 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 74350 0 None - 0 Human 8.0 pKi = 8.0 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
9992499 73039 0 None - 0 Human 6.0 pKi = 6 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 73039 0 None - 0 Human 6.0 pKi = 6 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
11716449 140684 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 140684 0 None - 0 Human 6.8 pKi = 6.8 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
10071501 9786 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL114228 9786 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
1242 3556 23 None 1 3 Human 6.7 pKi = 6.7 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 3556 23 None 1 3 Human 6.7 pKi = 6.7 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 3556 23 None 1 3 Human 6.7 pKi = 6.7 Functional
Agonist activity at dopamine D1 receptorAgonist activity at dopamine D1 receptor
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
11716438 140351 1 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 140351 1 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
16090814 81169 0 None - 0 Human 8.6 pKi = 8.6 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 81169 0 None - 0 Human 8.6 pKi = 8.6 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
11566745 74345 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 74345 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 74345 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
11558247 75071 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 75071 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
11637457 72740 1 None - 0 Human 6.7 pKi = 6.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 72740 1 None - 0 Human 6.7 pKi = 6.7 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
9952858 7473 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
CHEMBL108764 7473 0 None - 0 Rat 7.7 pKi = 7.7 Functional
Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudateDopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
44408818 139635 1 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
CHEMBL380330 139635 1 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
11573806 75066 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 75066 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
10467946 48205 3 None - 0 Human 8.5 pKi = 8.5 Functional
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1016/j.ejmech.2022.114378
CHEMBL155596 48205 3 None - 0 Human 8.5 pKi = 8.5 Functional
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1016/j.ejmech.2022.114378
11623343 140311 1 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 140311 1 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11493746 140792 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL383451 140792 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
16090821 81421 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 81421 0 None - 0 Human 6.5 pKi = 6.5 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
11718008 74941 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL203734 74941 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
137284323 184270 0 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 341 1 1 3 4.9 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4852403 184270 0 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 341 1 1 3 4.9 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CC1 10.1016/j.bmcl.2021.127911
11536995 139025 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL379662 139025 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
147230103 179573 0 None - 2 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
CHEMBL4748915 179573 0 None - 2 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2021.127911
5249956 73048 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 73048 1 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
135398737 944 89 None -77 36 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
38 944 89 None -77 36 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
722 944 89 None -77 36 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
CHEMBL42 944 89 None -77 36 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
DB00363 944 89 None -77 36 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2021.127911
11500677 140317 1 None - 0 Human 6.3 pKi = 6.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL381946 140317 1 None - 0 Human 6.3 pKi = 6.3 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
147200197 185132 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 317 1 1 3 4.7 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4865663 185132 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 317 1 1 3 4.7 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
11595240 139658 0 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 139658 0 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
11558055 72805 1 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 72805 1 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 72805 1 None - 0 Human 8.2 pKi = 8.2 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
4350931 168747 39 None - 1 Human 7.2 pKi = 7.2 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 168747 39 None - 1 Human 7.2 pKi = 7.2 Functional
Activity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D1 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
4350931 168747 39 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 168747 39 None - 1 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
11522339 74902 1 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
CHEMBL203689 74902 1 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D1 dopamine receptor in HEK 293 cells by intracellular calcium assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
5249952 73061 7 None - 0 Human 6.1 pKi = 6.1 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
CHEMBL201584 73061 7 None - 0 Human 6.1 pKi = 6.1 Functional
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by functional calcium assay
ChEMBL 304 1 1 1 4.4 CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 10.1021/jm050846j
135409468 2004 63 None - 5 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
333 2004 63 None - 5 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
CHEMBL845 2004 63 None - 5 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 10.1016/j.bmcl.2021.127911
164623328 185294 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 331 2 1 3 5.0 CCc1ccc2c(c1)C(C1=CCN(C)CC1)=Nc1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4868181 185294 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 331 2 1 3 5.0 CCc1ccc2c(c1)C(C1=CCN(C)CC1)=Nc1cc(C)ccc1N2 10.1016/j.bmcl.2021.127911
149505732 185649 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 321 1 1 3 4.6 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2021.127911
CHEMBL4873426 185649 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulationAntagonist activity at human D1 receptor expressed in CHO cells assessed as inhibition of dopamine-induced calcium accumulation
ChEMBL 321 1 1 3 4.6 Cc1ccc2c(c1)N=C(C1=CCN(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2021.127911
1225 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
3958 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
667477 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
CHEMBL860 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
DB01142 1443 24 None -3 11 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 279 3 0 2 4.0 CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C None
133538 3562 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.
Guide to Pharmacology 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 25660762
8443 3562 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.
Guide to Pharmacology 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 25660762
CHEMBL574558 3562 17 None - 1 Human 9.7 pEC50 = 9.7 Functional
Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.Biased towards G-protein signalling in a cellular assay expressing only D<sub>1</sub> receptor.
Guide to Pharmacology 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 25660762
12170 3847 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Ligand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamineLigand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamine
Guide to Pharmacology 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 36044544
137364063 3847 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Ligand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamineLigand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamine
Guide to Pharmacology 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 36044544
CHEMBL5172089 3847 6 None - 1 Human 7.2 pEC50 = 7.2 Functional
Ligand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamineLigand-induced elevation of cAMP production in the presence of EC<sub>70</sub> dopamine
Guide to Pharmacology 279 4 1 3 3.7 N=S(=O)(c1ccc(c2ccccc2OCF)cc1)C 36044544
10506 2488 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
86290953 2488 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
CHEMBL3421729 2488 15 None 20 3 Human 8.6 pEC50 = 8.6 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing human D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
10506 2488 15 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
86290953 2488 15 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
CHEMBL3421729 2488 15 None -20 3 Mouse 7.2 pEC50 = 7.2 Functional
Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.Potentiator potency: Increase of cAMP by LY3154207 in the presence of an EC<sub>20</sub> concentration of dopamine in HEK293 cells transiently expressing mouse D<sub>1</sub> receptors.
Guide to Pharmacology 449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C 31532644
122324 203 17 None -4 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
6077 203 17 None -4 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
CHEMBL86931 203 17 None -4 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 16318870
11938 2379 5 None 11 4 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 35175768
146192952 2379 5 None 11 4 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 35175768
CHEMBL4468760 2379 5 None 11 4 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 35175768
100 3745 52 None -7 28 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -7 28 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -7 28 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -7 28 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -7 28 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
146025821 169104 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169104 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025821 169104 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4437552 169104 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 3 0 5 3.9 CCc1cc2c(c(OC(C)=O)c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025817 175444 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 175444 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025817 175444 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 175444 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146192964 174138 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4559891 174138 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
681 1437 65 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
940 1437 65 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
947 1437 65 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
CHEMBL59 1437 65 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
DB00988 1437 65 None -154 38 Human 7.0 pEC50 = 7 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
6852376 91167 11 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
CHEMBL1467585 91167 11 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
CHEMBL24077 91167 11 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
CHEMBL503958 91167 11 None -4 5 Rat 7.0 pEC50 = 7 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00041a025
11938 2379 5 None - 0 Human 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 2379 5 None - 0 Human 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 2379 5 None - 0 Human 7.9 pEC50 = 7.9 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
75201901 165872 14 None -1 24 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None -1 24 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442471 175510 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 175510 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
75201961 169063 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
CHEMBL4437012 169063 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 331 3 0 5 5.0 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnnc1C 10.1021/acsmedchemlett.9b00050
130442471 175510 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
CHEMBL4591207 175510 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 331 3 1 5 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1cc(N)cnc1C 10.1021/acs.jmedchem.9b00351
75201901 165872 14 None -1 24 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None -1 24 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
4901726 180217 9 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4756486 180217 9 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
12668019 10143 6 None 204 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
CHEMBL1160787 10143 6 None 204 3 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/acs.jmedchem.8b00435
6603820 95330 13 None -4 13 Human 7.9 pEC50 = 7.9 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
CHEMBL25856 95330 13 None -4 13 Human 7.9 pEC50 = 7.9 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
146025820 172651 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4523054 172651 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 365 2 0 5 3.6 CC(=O)Oc1c(C)cc2c(c1OC(C)=O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
681 1437 65 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
940 1437 65 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
947 1437 65 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
CHEMBL59 1437 65 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
DB00988 1437 65 None -154 38 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acsmedchemlett.9b00050
85090318 178865 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740497 178865 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
146192966 174744 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acs.jmedchem.1c01887
CHEMBL4573538 174744 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1 10.1021/acs.jmedchem.1c01887
85090319 180028 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4754602 180028 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090338 180179 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4756163 180179 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090320 181981 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4787728 181981 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090337 182699 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796761 182699 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
11938 2379 5 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146192952 2379 5 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4468760 2379 5 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of mouse D1 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
85090325 179169 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4744261 179169 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
85090334 180043 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4754761 180043 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
132016545 172507 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 333 2 0 1 4.7 C[C@H]1c2ccccc2CCN1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4519818 172507 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 333 2 0 1 4.7 C[C@H]1c2ccccc2CCN1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
9796958 146045 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL2115374 146045 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL39230 146045 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL544814 146045 0 None -28 4 Human 5.8 pEC50 = 5.8 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
130442473 166783 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 166783 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442473 166783 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4294397 166783 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
85090335 180532 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
CHEMBL4760355 180532 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 10.1016/j.bmcl.2020.127696
85090330 180491 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4759814 180491 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
167715 2832 12 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2832 12 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2832 12 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
24133757 171034 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 340 1 1 2 5.2 CC1c2ccsc2CCN1C(=O)Nc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
CHEMBL4465320 171034 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
ChEMBL 340 1 1 2 5.2 CC1c2ccsc2CCN1C(=O)Nc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.8b01767
167715 2832 12 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
969 2832 12 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL225230 2832 12 None -194 5 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
133642 171385 9 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 171385 9 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
133642 171385 9 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
CHEMBL4470553 171385 9 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 307 2 0 3 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/acsmedchemlett.9b00575
10742 3560 27 None -2 7 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
1225 3560 27 None -2 7 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
CHEMBL35354 3560 27 None -2 7 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/acs.jmedchem.8b00435
10020353 13776 13 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL1196161 13776 13 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
CHEMBL556024 13776 13 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 343 3 2 3 4.2 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2cccc(C)c2)C1 10.1021/acs.jmedchem.8b00435
85090328 180453 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4759339 180453 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
146025701 170004 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 170004 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025713 171045 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 171045 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
146025701 170004 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
CHEMBL4450338 170004 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 357 3 1 7 4.2 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1N 10.1021/acs.jmedchem.9b00351
146025713 171045 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4465393 171045 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 372 3 0 6 5.4 Cc1cc(Oc2nccc3ccsc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442480 174698 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
130442480 174698 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -1 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
146025816 169411 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 169411 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
1242 3556 23 None -5 17 Human 6.6 pEC50 = 6.6 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 nan
935 3556 23 None -5 17 Human 6.6 pEC50 = 6.6 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 nan
CHEMBL286080 3556 23 None -5 17 Human 6.6 pEC50 = 6.6 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 nan
146192967 190518 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 485 5 1 5 4.5 C[C@H]1c2cccc(-c3cnn(C4COC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL5187909 190518 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 485 5 1 5 4.5 C[C@H]1c2cccc(-c3cnn(C4COC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
146025816 169411 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 169411 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
130442590 169232 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 169232 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
130442590 169232 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4439333 169232 0 None - 0 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)nc2cnccn12 10.1021/acs.jmedchem.9b00351
130442572 171342 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 171342 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None -3 24 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
6603703 206 7 None -1 5 Human 8.5 pEC50 = 8.5 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
9637 206 7 None -1 5 Human 8.5 pEC50 = 8.5 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
CHEMBL291143 206 7 None -1 5 Human 8.5 pEC50 = 8.5 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
1153 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
12668023 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026874 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
30026875 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
3341 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
6603851 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
933 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
939 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
985 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1160786 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL1161520 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
CHEMBL588 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
DB00800 1598 53 None -32 10 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assayAgonist activity at human dopamine D1 receptor expressed in CHOK1 cells assessed as assessed as increase in beta-arrestin-2 recruitment after 60 mins by luminescence assay
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/acs.jmedchem.8b00435
75201901 165872 14 None -1 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
CHEMBL4277264 165872 14 None -1 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acsmedchemlett.9b00050
2030130 20779 13 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL1311333 20779 13 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090324 180110 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4755481 180110 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
76284418 181736 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4784295 181736 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
75202022 170243 2 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 170243 2 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
146025815 169212 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 169212 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
1218 3559 24 None -11 7 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 3559 24 None -11 7 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 3559 24 None -11 7 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
146025815 169212 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 169212 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
85090321 182231 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4790909 182231 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090323 181340 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4779641 181340 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2020.127696
146266 100231 7 None -2 4 Human 7.4 pEC50 = 7.4 Binding
Antagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL292418 100231 7 None -2 4 Human 7.4 pEC50 = 7.4 Binding
Antagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL540857 100231 7 None -2 4 Human 7.4 pEC50 = 7.4 Binding
Antagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assayAntagonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as inhibition of SKF81297-induced beta arrestin2 recruitment preincubated for 30 mins followed by SKF81297 addition and measured after 90 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
146025823 169010 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 169010 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
146025823 169010 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
CHEMBL4435882 169010 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 457 4 0 6 5.0 COc1cccc(-c2cc3c(c(OC(C)=O)c2OC(C)=O)-c2cccc4c2[C@@H](C3)N(C)CC4)c1 10.1021/acsmedchemlett.9b00575
85090322 178879 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4740678 178879 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
75201899 171350 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 171350 0 None - 1 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assayAgonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
228 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
3033200 173955 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173955 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
85090333 180719 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
CHEMBL4762375 180719 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 10.1016/j.bmcl.2020.127696
85090326 182191 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4790277 182191 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
228 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
33 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
6005 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
CHEMBL53 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
DB00714 441 26 None -35 24 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/acsmedchemlett.9b00575
3033200 173955 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
CHEMBL4555547 173955 5 None - 0 Human 5.3 pEC50 = 5.3 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 4 0 5 4.1 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(OC(C)=O)c(OC(C)=O)c1-3 10.1021/acsmedchemlett.9b00575
85090332 180137 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4755709 180137 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
6852376 91167 11 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL1467585 91167 11 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL24077 91167 11 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL503958 91167 11 None -3 5 Human 7.2 pEC50 = 7.2 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
146192960 170953 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
CHEMBL4464150 170953 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Positive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assayPositive allosteric modulation of human D1 receptor in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins in presence of dopamine by HTRF assay
ChEMBL 429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.1c01887
85090339 181723 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
CHEMBL4784143 181723 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1 10.1016/j.bmcl.2020.127696
136326241 178848 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4740312 178848 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21 10.1016/j.bmcl.2020.127696
92044504 171161 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 171161 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
92044504 171161 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4467080 171161 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 3 0 6 4.5 Cc1cc(Oc2nccn3cccc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
3045992 175501 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4591021 175501 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
90134269 173634 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 173634 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
90134269 173634 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4548284 173634 1 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assayAgonist activity at recombinant C-terminal RLuc8-fused human D1 receptor expressed in HEK29T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 15 mins in presence of coelenterazine H by BRET assay
ChEMBL 342 3 1 6 4.5 Nc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
3045992 175501 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4591021 175501 1 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 355 6 0 5 3.4 COCOc1ccc2c(c1OCOC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
85090329 182100 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4789255 182100 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21 10.1016/j.bmcl.2020.127696
85090331 180871 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
CHEMBL4764398 180871 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl 10.1016/j.bmcl.2020.127696
76284419 182666 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
CHEMBL4796389 182666 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)Positive allosteric modulator activity at human dopamine D1 receptor expressed in CHO-K1 cells assessed as potentiation of dopamine-induced beta-arrestin2 recruitment by measuring dopamine EC50 at 50 uM incubated for 90 mins by PathHunter assay (Rvb = 1.4 uM)
ChEMBL 343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21 10.1016/j.bmcl.2020.127696
9841398 99058 3 None -3 4 Human 8.1 pEC50 = 8.1 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
CHEMBL28338 99058 3 None -3 4 Human 8.1 pEC50 = 8.1 Binding
Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
1218 3559 24 None -11 7 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
938 3559 24 None -11 7 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
CHEMBL353335 3559 24 None -11 7 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D1 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acs.jmedchem.9b00412
72548703 161019 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161019 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysisDisplacement of [3H]-SCH 23390 from human recombinant dopamine D1 receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
3036864 201066 16 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL1256645 201066 16 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL1814790 201066 16 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
CHEMBL62 201066 16 None -2 27 Human 9.7 pIC50 = 9.7 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2013.03.016
3036864 201066 16 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1256645 201066 16 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1814790 201066 16 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL62 201066 16 None -2 27 Human 9.6 pIC50 = 9.6 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
5281878 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
5281881 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
948 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
968 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
CHEMBL42055 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
CHEMBL54661 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
DB00875 1630 33 None -11 16 Rat 9.5 pIC50 = 9.5 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2003.08.063
5018 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
943 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
946 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
CHEMBL13668 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting methodDisplacement of [3H]SCH 23390 from human recombinant dopamine D1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.11.014
5018 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
943 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
946 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
CHEMBL13668 3493 8 None 2 9 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant Dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2016.03.006
44358126 26474 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 315 1 1 2 4.2 C[C@H]1N(C)CCc2cc(Cl)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm00022a004
CHEMBL136190 26474 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 315 1 1 2 4.2 C[C@H]1N(C)CCc2cc(Cl)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm00022a004
3036864 201066 16 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
CHEMBL1256645 201066 16 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
CHEMBL1814790 201066 16 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
CHEMBL62 201066 16 None -2 27 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00002a013
11795296 26562 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136260 26562 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
3036864 201066 16 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
CHEMBL1256645 201066 16 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
CHEMBL1814790 201066 16 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
CHEMBL62 201066 16 None -2 27 Human 9.2 pIC50 = 9.2 Binding
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm058018d
10809333 26984 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136630 26984 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
10522247 26526 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136235 26526 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
3036864 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
CHEMBL1256645 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
CHEMBL1814790 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
CHEMBL62 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm701575k
10784787 26516 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 360 2 0 3 5.0 CN1CCN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136226 26516 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 360 2 0 3 5.0 CN1CCN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
11795296 26562 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136260 26562 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
3036864 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
CHEMBL1256645 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
CHEMBL1814790 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
CHEMBL62 201066 16 None -2 27 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2010.07.034
10712649 118702 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL343282 118702 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
10810927 118791 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL343922 118791 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
10522247 26526 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136235 26526 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
11794473 118825 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCC2 10.1021/jm00022a004
CHEMBL344206 118825 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCC2 10.1021/jm00022a004
10810927 118791 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL343922 118791 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
3036864 201066 16 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1256645 201066 16 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1814790 201066 16 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL62 201066 16 None -2 27 Human 9.0 pIC50 = 9.0 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
10787324 26650 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 402 4 1 3 4.4 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCO 10.1021/jm00022a004
CHEMBL136340 26650 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 402 4 1 3 4.4 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCO 10.1021/jm00022a004
10574585 27218 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL136822 27218 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
3036864 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
CHEMBL1256645 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
CHEMBL1814790 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
CHEMBL62 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00168a034
3036864 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
CHEMBL1256645 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
CHEMBL1814790 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
CHEMBL62 201066 16 None -2 27 Rat 9.0 pIC50 = 9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00041a025
10043978 27041 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL136683 27041 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
10525990 27365 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 5 1 3 4.8 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCCO 10.1021/jm00022a004
CHEMBL136932 27365 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 5 1 3 4.8 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCCO 10.1021/jm00022a004
10247592 28691 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL137960 28691 1 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
6603950 201633 9 None -6 9 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL64875 201633 9 None -6 9 Rat 8.9 pIC50 = 8.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
6603950 201633 9 None -6 9 Rat 8.9 pIC50 = 8.9 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
CHEMBL64875 201633 9 None -6 9 Rat 8.9 pIC50 = 8.9 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
107995 96678 17 None - 5 Rat 8.9 pIC50 = 8.9 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmcl.2003.08.063
29982233 96678 17 None - 5 Rat 8.9 pIC50 = 8.9 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmcl.2003.08.063
CHEMBL267723 96678 17 None - 5 Rat 8.9 pIC50 = 8.9 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmcl.2003.08.063
10809333 26984 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136630 26984 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
3036864 201066 16 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
CHEMBL1256645 201066 16 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
CHEMBL1814790 201066 16 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
CHEMBL62 201066 16 None -2 27 Rat 8.9 pIC50 = 8.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a022
10712649 118702 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL343282 118702 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
3036864 201066 16 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1256645 201066 16 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1814790 201066 16 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL62 201066 16 None -2 27 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
10835172 118674 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 406 2 0 2 5.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL343078 118674 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 406 2 0 2 5.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1(C)C 10.1021/jm00022a004
10247592 28691 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL137960 28691 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
10525999 27156 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Br)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136776 27156 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 416 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Br)cc32)CC1(C)C 10.1021/jm00022a004
10574585 27218 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL136822 27218 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
5016 108682 8 None - 2 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL32145 108682 8 None - 2 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL544114 108682 8 None - 2 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00086a016
146025812 174319 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 174319 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10049758 202939 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL73589 202939 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
177725 172695 1 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)C[C@H]1c3c(ccc(O)c3O2)CCN1C 10.1021/jm060959i
CHEMBL452510 172695 1 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)C[C@H]1c3c(ccc(O)c3O2)CCN1C 10.1021/jm060959i
159034 172696 2 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1ccc2c(c1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL452512 172696 2 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1ccc2c(c1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
15657216 12887 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1189682 12887 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL539274 12887 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
15657214 13127 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1191339 13127 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL542419 13127 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1 10.1021/jm00069a013
10252000 98095 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27650 98095 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50188 98095 0 None - 1 Bovine 5.0 pIC50 = 5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
15065270 111864 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 249 2 1 4 2.5 CCCN1CCC2=C(CCc3sc(N)nc32)C1 10.1021/jm00113a010
CHEMBL329444 111864 0 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 249 2 1 4 2.5 CCCN1CCC2=C(CCc3sc(N)nc32)C1 10.1021/jm00113a010
194775 205588 22 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 223 3 1 4 2.2 CCCN1CCC=C(c2csc(N)n2)C1 10.1021/jm00113a010
CHEMBL93428 205588 22 None - 0 Rat 5.0 pIC50 = 5 Binding
In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390In vitro binding affinity towards dopamine receptor D1 in rat striatal membrane using [3H]-SCH- 23390
ChEMBL 223 3 1 4 2.2 CCCN1CCC=C(c2csc(N)n2)C1 10.1021/jm00113a010
10008463 11145 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178971 11145 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51985 11145 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
11743327 98249 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27763 98249 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
131001 98536 7 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27995 98536 7 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1 10.1021/jm00038a007
10364722 98628 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 98628 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 98628 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 99098 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99098 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9975915 99275 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL284912 99275 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10338595 161949 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL416747 161949 0 None - 1 Bovine 4.0 pIC50 = 4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10707563 28143 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
CHEMBL137478 28143 0 None - 0 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
3082597 99098 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL283606 99098 8 None - 1 Bovine 4.0 pIC50 = 4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm950861w
14138285 144622 4 None - 1 Human 6.0 pIC50 = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
CHEMBL3912178 144622 4 None - 1 Human 6.0 pIC50 = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
71109989 153241 0 None 6 2 Human 7.0 pIC50 = 7.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3982119 153241 0 None 6 2 Human 7.0 pIC50 = 7.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
9992356 9664 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
CHEMBL113477 9664 1 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
440585 12582 14 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 596 8 3 8 6.2 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3O)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL1187468 12582 14 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 596 8 3 8 6.2 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3O)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL503882 12582 14 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 596 8 3 8 6.2 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3O)cc1)N(C)CC2 10.1021/np50087a016
135221 144686 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3912606 144686 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
135398737 944 89 None -44 91 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 944 89 None -44 91 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 944 89 None -44 91 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 944 89 None -44 91 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 944 89 None -44 91 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
10015045 13541 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
CHEMBL119455 13541 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
6603799 99253 12 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL284746 99253 12 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@H](c1ccccc1)CNCC2 10.1021/jm00086a016
150 2473 18 None -43 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2473 18 None -43 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2473 18 None -43 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2473 18 None -43 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2473 18 None -43 15 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
14901831 13273 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1192581 13273 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL543838 13273 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
3168 9172 84 None -89 21 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9172 84 None -89 21 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
16104 161368 15 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
CHEMBL415300 161368 15 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm991005d
16104 161368 15 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm9704457
CHEMBL415300 161368 15 None -1 5 Rat 8.0 pIC50 = 8.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm9704457
6603820 95330 13 None 1 13 Rat 7.9 pIC50 = 7.9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
CHEMBL25856 95330 13 None 1 13 Rat 7.9 pIC50 = 7.9 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
1353 1880 85 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1880 85 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1880 85 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1880 85 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1880 85 None -38 85 Human 7.0 pIC50 = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
10015045 13541 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL119455 13541 1 None -2 6 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
146025812 174319 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4564103 174319 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
10043978 27041 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL136683 27041 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
14901827 12942 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1190039 12942 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL540036 12942 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
44584684 12336 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@H](Cc1ccc(OC)c(c1)-c1cc(ccc1O)C(=O)[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL1186001 12336 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@H](Cc1ccc(OC)c(c1)-c1cc(ccc1O)C(=O)[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL445011 12336 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@H](Cc1ccc(OC)c(c1)-c1cc(ccc1O)C(=O)[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
2801 161325 56 None -10 28 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161325 56 None -10 28 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161325 56 None -10 28 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
44317479 204031 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.
ChEMBL 243 4 3 3 2.4 NCC(Cc1ccccc1)c1ccc(O)c(O)c1 10.1021/jm00013a015
CHEMBL82706 204031 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.Binding affinity to the dopamine receptor D1 by displacing [3H]-SCH- 23390 radio-ligand in rat striatal membranes by using radioligand competition assay.
ChEMBL 243 4 3 3 2.4 NCC(Cc1ccccc1)c1ccc(O)c(O)c1 10.1021/jm00013a015
10885636 110527 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL326263 110527 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
10024827 13026 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1190552 13026 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL541096 13026 2 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
70684206 75712 0 None 11 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057442 75712 0 None 11 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692652 75711 0 None 8 2 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
CHEMBL2057441 75711 0 None 8 2 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
10547041 23610 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.8 Oc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
CHEMBL133615 23610 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.8 Oc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
14901829 13032 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1190633 13032 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL541304 13032 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
10264849 9277 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 265 0 1 2 3.3 CN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
CHEMBL111348 9277 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 265 0 1 2 3.3 CN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
107715 199260 18 None -144 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199260 18 None -144 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199260 18 None -144 20 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
8447 188362 80 None -8 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188362 80 None -8 13 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
3191 102385 93 None -12 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -12 25 Human 5.9 pIC50 = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
13154762 102636 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL307717 102636 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
15648961 106917 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 341 2 0 1 5.4 CN1CCC(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL317982 106917 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 341 2 0 1 5.4 CN1CCC(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
6603820 95330 13 None 1 13 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00168a034
CHEMBL25856 95330 13 None 1 13 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00168a034
6917970 3635 54 None -1 34 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
8370 3635 54 None -1 34 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
CHEMBL487387 3635 54 None -1 34 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
6604005 156575 2 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm00168a034
CHEMBL407489 156575 2 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O 10.1021/jm00168a034
10361722 22020 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.5 Oc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
CHEMBL132304 22020 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 369 2 1 2 3.5 Oc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
10333742 59088 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 277 2 0 1 4.1 c1ccc(CN2CCCC3Cc4ccccc4CC32)cc1 10.1016/s0960-894x(01)00076-2
CHEMBL170974 59088 1 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 277 2 0 1 4.1 c1ccc(CN2CCCC3Cc4ccccc4CC32)cc1 10.1016/s0960-894x(01)00076-2
42 2032 50 None - 17 Bovine 4.9 pIC50 = 4.9 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
56971 2032 50 None - 17 Bovine 4.9 pIC50 = 4.9 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL8412 2032 50 None - 17 Bovine 4.9 pIC50 = 4.9 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
42 2032 50 None - 17 Bovine 4.9 pIC50 = 4.9 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
56971 2032 50 None - 17 Bovine 4.9 pIC50 = 4.9 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
CHEMBL8412 2032 50 None - 17 Bovine 4.9 pIC50 = 4.9 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
44370646 47951 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/jm00164a022
CHEMBL155246 47951 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@H](C2)N(C)CC3 10.1021/jm00164a022
44269133 33713 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 356 2 3 3 2.1 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL14239 33713 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 356 2 3 3 2.1 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
72329 95204 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 337 2 2 5 4.0 COc1c(O)c2c3c(nccc3c1OC)C(C)(C)c1cc(O)ccc1-2 10.1021/jm060959i
CHEMBL257958 95204 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 337 2 2 5 4.0 COc1c(O)c2c3c(nccc3c1OC)C(C)(C)c1cc(O)ccc1-2 10.1021/jm060959i
64143 197186 57 None -1 8 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
CHEMBL584 197186 57 None -1 8 Human 4.9 pIC50 = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
10523361 29611 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC(C)N1C 10.1021/jm00022a004
CHEMBL138745 29611 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC(C)N1C 10.1021/jm00022a004
10567738 118901 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 320 2 0 2 4.3 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL344680 118901 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 320 2 0 2 4.3 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
71109797 145363 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
CHEMBL3917753 145363 0 None - 1 Human 7.9 pIC50 = 7.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
135398737 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
38 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
722 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
CHEMBL42 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
DB00363 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00022a004
15653096 206154 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1 10.1021/jm00022a004
CHEMBL1788129 206154 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1 10.1021/jm00022a004
CHEMBL96618 206154 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1 10.1021/jm00022a004
135398737 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
38 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
722 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
CHEMBL42 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
DB00363 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm991005d
135398737 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
38 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
722 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
CHEMBL42 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
DB00363 944 89 None -83 91 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9704457
100 3745 52 None -16 55 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
2637 3745 52 None -16 55 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
5452 3745 52 None -16 55 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
CHEMBL479 3745 52 None -16 55 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
DB00679 3745 52 None -16 55 Rat 5.9 pIC50 = 5.9 Binding
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
131213 5230 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL106622 5230 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
131213 5230 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL106622 5230 1 None - 2 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
44312870 202871 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
CHEMBL73082 202871 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
44285576 141719 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C/c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
CHEMBL38848 141719 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C/c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
12545 47395 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 281 1 1 3 3.2 COc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
CHEMBL154709 47395 9 None - 0 Rat 4.9 pIC50 = 4.9 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 281 1 1 3 3.2 COc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
195158 42905 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
CHEMBL150550 42905 1 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
44267161 162492 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL417608 162492 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
70690498 75714 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057445 75714 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
71109805 87077 0 None 27 3 Human 7.8 pIC50 = 7.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
CHEMBL2334881 87077 0 None 27 3 Human 7.8 pIC50 = 7.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
70690500 75720 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 75720 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
70692653 75713 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057443 75713 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
70692653 75713 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL2057443 75713 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
146025817 175444 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 175444 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
22857296 28937 0 None - 4 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13816 28937 0 None - 4 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
146025817 175444 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4589737 175444 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 309 2 0 3 3.8 COc1ccc2c(c1OC)-c1ccc(C)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
15720219 68323 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranesCompound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranes
ChEMBL 220 5 0 2 2.9 CCCN(CCC)[C@H]1CCn2cccc2C1 10.1016/S0960-894X(00)80003-7
CHEMBL192037 68323 1 None - 1 Rat 4.8 pIC50 = 4.8 Binding
Compound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranesCompound was evaluated for binding affinity to Dopamine receptor D1 labeled with [3H]-SCH- 23390 (0.3 nM) in rat striatal membranes
ChEMBL 220 5 0 2 2.9 CCCN(CCC)[C@H]1CCn2cccc2C1 10.1016/S0960-894X(00)80003-7
146025813 175014 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175014 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
6603820 95330 13 None 1 13 Rat 6.8 pIC50 = 6.8 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
CHEMBL25856 95330 13 None 1 13 Rat 6.8 pIC50 = 6.8 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
2585 790 100 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 790 100 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 790 100 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 790 100 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 790 100 None -112 22 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
71474024 143935 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3906676 143935 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
10247592 28691 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL137960 28691 1 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
146025816 169411 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 169411 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
146025816 169411 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4442011 169411 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
44190762 176306 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
CHEMBL461571 176306 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
ChEMBL 531 8 1 5 6.6 Cc1c(C(=O)c2ccc(Cl)cc2)c2ccc(OC(F)(F)F)cc2n1Cc1cccc(O[C@H](C)C(=O)O)c1 10.1016/j.bmcl.2008.07.103
26987 936 29 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 936 29 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 936 29 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 936 29 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 936 29 None -245 21 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
9851833 12334 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 608 3 1 8 6.9 COc1ccc2cc1Oc1ccc(cc1)C[C@@H]1c3c(cc(OC)c(O)c3Oc3cc4c(cc3OC)CCN(C)[C@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL1185978 12334 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 608 3 1 8 6.9 COc1ccc2cc1Oc1ccc(cc1)C[C@@H]1c3c(cc(OC)c(O)c3Oc3cc4c(cc3OC)CCN(C)[C@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL443953 12334 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 608 3 1 8 6.9 COc1ccc2cc1Oc1ccc(cc1)C[C@@H]1c3c(cc(OC)c(O)c3Oc3cc4c(cc3OC)CCN(C)[C@H]4C2)CCN1C 10.1021/np50087a016
2274 3124 53 None -16 32 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -16 32 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -16 32 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -16 32 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -16 32 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44284723 137593 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C/C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL37661 137593 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C/C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
277 1274 55 None -47 45 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1274 55 None -47 45 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1274 55 None -47 45 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1274 55 None -47 45 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1274 55 None -47 45 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
146025815 169212 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 169212 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
15115476 26899 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 2 0 2 4.2 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
CHEMBL136553 26899 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 326 2 0 2 4.2 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
10320519 26908 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 4 1 3 3.2 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL136562 26908 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 4 1 3 3.2 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
146025815 169212 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
CHEMBL4439029 169212 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 323 3 0 3 4.0 CCc1ccc2c3c1CCN(C)[C@@H]3Cc1ccc(OC)c(OC)c1-2 10.1021/acsmedchemlett.9b00575
10732779 187687 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 297 4 2 3 3.7 CCCN1CCc2cc(O)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm001128u
CHEMBL49995 187687 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 297 4 2 3 3.7 CCCN1CCc2cc(O)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm001128u
10264176 110838 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
CHEMBL326781 110838 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1ccc2c(c1)[C@@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
10048240 13283 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 347 9 2 3 4.6 CCCN(CCCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1192639 13283 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 347 9 2 3 4.6 CCCN(CCCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL543914 13283 1 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 347 9 2 3 4.6 CCCN(CCCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
44358170 28076 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 378 2 0 2 4.7 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
CHEMBL137430 28076 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 378 2 0 2 4.7 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
100 3745 52 None -16 55 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
2637 3745 52 None -16 55 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
5452 3745 52 None -16 55 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
CHEMBL479 3745 52 None -16 55 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
DB00679 3745 52 None -16 55 Rat 7.8 pIC50 = 7.8 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00393a021
44370644 48537 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm060959i
CHEMBL155884 48537 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm060959i
240 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
2769 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
44279790 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
660 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL1729 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
CHEMBL560739 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
DB00604 931 39 None - 25 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm0509501
44370644 48537 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
CHEMBL155884 48537 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
6603798 99717 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL1613539 99717 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL288096 99717 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
6603798 99717 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL1613539 99717 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL288096 99717 5 None -17378 2 Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
14140118 95152 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 1 4 3.2 COc1c(O)c2c3c(c1OC)CCN(C)C3Cc1ccccc1-2 10.1021/jm060959i
CHEMBL257747 95152 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 1 4 3.2 COc1c(O)c2c3c(c1OC)CCN(C)C3Cc1ccccc1-2 10.1021/jm060959i
1043 1552 13 None -9549 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1552 13 None -9549 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1552 13 None -9549 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1552 13 None -9549 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1552 13 None -9549 28 Human 5.8 pIC50 = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
1588 2294 24 None -190 43 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2294 24 None -190 43 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2294 24 None -190 43 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2294 24 None -190 43 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2294 24 None -190 43 Human 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
15653097 205463 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
CHEMBL2111567 205463 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
CHEMBL92560 205463 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
9979207 13726 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1195842 13726 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL555427 13726 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 333 8 2 3 4.2 CCCN(CCc1ccc(O)cc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
44370749 48475 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
CHEMBL155833 48475 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
70692652 75711 0 None 8 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057441 75711 0 None 8 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
6603729 99494 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL286424 99494 2 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@H](c2ccccc2)C1 10.1021/jm00086a016
192611 13458 7 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 301 2 1 2 4.1 CN(C)[C@H]1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1193985 13458 7 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 301 2 1 2 4.1 CN(C)[C@H]1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL545477 13458 7 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 301 2 1 2 4.1 CN(C)[C@H]1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
10595484 118585 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)C(C)CN1C 10.1021/jm00022a004
CHEMBL342698 118585 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)C(C)CN1C 10.1021/jm00022a004
71240 205983 10 None - 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00072a006
CHEMBL95636 205983 10 None - 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 408 4 1 3 4.0 OCCN1CCN([C@@H]2C[C@@H](c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00072a006
1241 99716 19 None -1 7 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL288090 99716 19 None -1 7 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00086a016
CHEMBL552611 99716 19 None -1 7 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00086a016
1242 3556 23 None 1 17 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00086a016
935 3556 23 None 1 17 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00086a016
CHEMBL286080 3556 23 None 1 17 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00086a016
44269117 96864 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 352 2 2 4 3.2 CN1C[C@H](C(=O)Nc2nccs2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL269160 96864 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 352 2 2 4 3.2 CN1C[C@H](C(=O)Nc2nccs2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
10831881 115972 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 4.1 I/C=C/CN1CCC[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm980284m
CHEMBL336128 115972 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 4.1 I/C=C/CN1CCC[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm980284m
71474025 144794 0 None 131 2 Human 5.7 pIC50 = 5.7 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 144794 0 None 131 2 Human 5.7 pIC50 = 5.7 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
135398737 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
38 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
722 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
CHEMBL42 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
DB00363 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00130a006
135398737 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
38 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
722 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
CHEMBL42 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
DB00363 944 89 None -83 91 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00164a053
100 3745 52 None -47 55 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -47 55 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -47 55 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -47 55 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -47 55 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
129503 161119 9 None - 5 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
CHEMBL413105 161119 9 None - 5 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
2750 202363 69 None -5 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 202363 69 None -5 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
10043978 27041 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL136683 27041 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
10641744 31113 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 352 2 0 2 4.7 Cc1ccc2c(c1)C(N1CCN(C)C(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL140189 31113 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 352 2 0 2 4.7 Cc1ccc2c(c1)C(N1CCN(C)C(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
10810109 114996 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 Fc1ccc(C2CC(N3CCN4CCCCC4C3)c3cc(Cl)ccc32)cc1 10.1021/jm00022a004
CHEMBL335155 114996 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 384 2 0 2 5.2 Fc1ccc(C2CC(N3CCN4CCCCC4C3)c3cc(Cl)ccc32)cc1 10.1021/jm00022a004
9819535 98490 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.
ChEMBL 344 2 1 4 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(N=C=S)c2)C1 10.1016/0960-894X(96)00186-2
CHEMBL279634 98490 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.Compound was tested for binding affinity against Dopamine receptor D1 using 1 nM [3H]SCH-23390 as the radioligand.
ChEMBL 344 2 1 4 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(N=C=S)c2)C1 10.1016/0960-894X(96)00186-2
2726 906 64 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
621 906 64 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
83 906 64 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
CHEMBL71 906 64 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
DB00477 906 64 None -18 72 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00002a013
12765746 101810 3 None -18 10 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
CHEMBL303313 101810 3 None -18 10 Rat 8.7 pIC50 = 8.7 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm020938y
12765746 101810 3 None -18 10 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
CHEMBL303313 101810 3 None -18 10 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
1238 201484 21 None -5 16 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
CHEMBL64249 201484 21 None -5 16 Rat 8.7 pIC50 = 8.7 Binding
Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranesAbility to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00111a015
12765746 101810 3 None -18 10 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL303313 101810 3 None -18 10 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00072a006
10666149 118827 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 0 2 4.7 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
CHEMBL344216 118827 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 358 2 0 2 4.7 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
10246528 27085 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136722 27085 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
3036864 201066 16 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1256645 201066 16 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1814790 201066 16 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL62 201066 16 None -2 27 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
5018 3493 8 None 2 9 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
943 3493 8 None 2 9 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
946 3493 8 None 2 9 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
CHEMBL13668 3493 8 None 2 9 Human 8.6 pIC50 = 8.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
10810514 27009 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 392 2 1 2 5.1 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CCN1 10.1021/jm00022a004
CHEMBL136648 27009 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 392 2 1 2 5.1 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CCN1 10.1021/jm00022a004
135514603 202414 13 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL70319 202414 13 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 474 2 1 7 4.0 CN1CCN(C2=Nc3cc(Cl)ccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
681 1437 65 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
940 1437 65 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
947 1437 65 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
CHEMBL59 1437 65 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
DB00988 1437 65 None -23 38 Bovine 6.7 pIC50 = 6.7 Binding
In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/S0960-894X(00)80265-6
15653098 205517 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1 10.1021/jm00022a004
CHEMBL92896 205517 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1 10.1021/jm00022a004
121852 10071 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10071 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10071 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9978353 11149 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL1178987 11149 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL52785 11149 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
9981024 95651 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 95651 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 95651 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10319624 98530 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27991 98530 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL298534 98530 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9980269 98626 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280586 98626 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54266 98626 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10321248 98967 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28287 98967 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50722 98967 0 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
121852 10071 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 10071 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 10071 7 None - 1 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
10333685 88116 3 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 276 1 1 1 3.8 CN1CCc2c([nH]c3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
CHEMBL23529 88116 3 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 276 1 1 1 3.8 CN1CCc2c([nH]c3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
14233815 205278 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CCC21 10.1021/jm00113a010
CHEMBL91453 205278 1 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CCC21 10.1021/jm00113a010
71109993 142715 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
CHEMBL3896617 142715 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
14547414 101814 1 None - 5 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
CHEMBL303339 101814 1 None - 5 Rat 4.7 pIC50 = 4.7 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
28417 39799 48 None -1 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 39799 48 None -1 12 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
10480509 141799 0 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 483 2 2 5 4.4 COc1cc2c(c(Br)c1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL388564 141799 0 None - 2 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 483 2 2 5 4.4 COc1cc2c(c(Br)c1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
44312605 202730 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL72162 202730 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
44323851 205246 0 None 3 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL91310 205246 0 None 3 4 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
13154801 27244 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 370 5 1 4 3.0 COc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL136841 27244 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 370 5 1 4 3.0 COc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
24121307 102569 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(C)(=O)=O)cc32)CC1 10.1021/jm991005d
CHEMBL307163 102569 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(C)(=O)=O)cc32)CC1 10.1021/jm991005d
3117 206106 100 None -2 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -2 16 Human 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
147080 204259 4 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.
ChEMBL 365 6 0 6 2.8 O=c1ccoc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1021/jm00105a039
CHEMBL84639 204259 4 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.Compound was tested for its inhibitory effect on the binding profile in Dopamine receptor D1 using [3H]flupenthixol in rat brain.
ChEMBL 365 6 0 6 2.8 O=c1ccoc2cc(OCCCN3CCN(c4ccccn4)CC3)ccc12 10.1021/jm00105a039
44354812 24925 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 3.8 I/C=C/CN1CCCC2Cc3ccccc3CC21 10.1021/jm980284m
CHEMBL134746 24925 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 353 2 0 1 3.8 I/C=C/CN1CCCC2Cc3ccccc3CC21 10.1021/jm980284m
44285034 149235 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C\C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL39483 149235 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 305 6 0 1 5.0 C(=C\C1CCCN(CCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
135493554 202459 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3cc(OS(C)(=O)=O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL70609 202459 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 386 2 1 7 2.4 CN1CCN(C2=Nc3cc(OS(C)(=O)=O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
125720 26110 5 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 338 2 2 3 1.7 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13588 26110 5 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 338 2 2 3 1.7 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
9911120 9532 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 9532 0 None - 0 Bovine 4.7 pIC50 = 4.7 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
2726 906 64 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -36 72 Human 6.7 pIC50 = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
4913274 17816 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 408 4 1 3 4.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
CHEMBL12628 17816 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 408 4 1 3 4.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1 10.1021/jm00022a004
15648962 107866 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 339 2 0 1 5.3 CN1CC=C(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL319810 107866 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 339 2 0 1 5.3 CN1CC=C(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
1212 1632 45 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -51 65 Human 7.6 pIC50 = 7.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
146025814 172210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 172210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
9911120 9532 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 9532 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
11744707 164357 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL422283 164357 0 None - 0 Bovine 4.6 pIC50 = 4.6 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
228 441 26 None -30 24 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
33 441 26 None -30 24 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
6005 441 26 None -30 24 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
CHEMBL53 441 26 None -30 24 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
DB00714 441 26 None -30 24 Rat 6.6 pIC50 = 6.6 Binding
In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1In vitro antagonist binding affinity was determined by displacing the [3H]-SCH- in rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)81245-2
10400783 193216 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 267 2 1 3 2.8 c1ccc(C[C@@H]2NCCc3cc4c(cc32)OCO4)cc1 10.1021/jm001128u
CHEMBL54051 193216 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 267 2 1 3 2.8 c1ccc(C[C@@H]2NCCc3cc4c(cc32)OCO4)cc1 10.1021/jm001128u
10531 1392 18 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1392 18 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1392 18 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1392 18 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1392 18 None -218 24 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
440989 94856 23 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 285 3 3 4 2.5 COc1cc2c(cc1O)[C@@H](Cc1ccc(O)cc1)NCC2 10.1021/np980008a
CHEMBL256448 94856 23 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 285 3 3 4 2.5 COc1cc2c(cc1O)[C@@H](Cc1ccc(O)cc1)NCC2 10.1021/np980008a
10408602 13584 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 317 8 1 2 4.5 CCCN(CCc1ccccc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1194852 13584 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 317 8 1 2 4.5 CCCN(CCc1ccccc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL553399 13584 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 317 8 1 2 4.5 CCCN(CCc1ccccc1)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
2284 3133 27 None -36 28 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3133 27 None -36 28 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3133 27 None -36 28 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3133 27 None -36 28 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3133 27 None -36 28 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
10246528 27085 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136722 27085 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
22179 185683 36 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 3 5 2.5 COc1cc2c(cc1O)C[C@@H]1NCCc3cc(O)c(OC)c-2c31 10.1021/jm060959i
CHEMBL487388 185683 36 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 2 3 5 2.5 COc1cc2c(cc1O)C[C@@H]1NCCc3cc(O)c(OC)c-2c31 10.1021/jm060959i
11035765 9795 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
CHEMBL114280 9795 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 359 6 2 6 3.3 Oc1nc2ccccc2n1CCCNCc1cc2c(cc1Cl)OCO2 10.1021/jm010878g
49836496 18369 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1 10.1021/jm100515z
CHEMBL1275791 18369 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1 10.1021/jm100515z
146025814 172210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4513262 172210 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
197505 13579 16 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 171 2 2 2 1.5 NCCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1194829 13579 16 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 171 2 2 2 1.5 NCCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL553361 13579 16 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 171 2 2 2 1.5 NCCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
441383 20133 54 None -12 17 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20133 54 None -12 17 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
2600 3720 73 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3720 73 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3720 73 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3720 73 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3720 73 None -7 13 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
10762505 164305 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 4.1 COc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
CHEMBL421914 164305 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 4.1 COc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I 10.1021/jm980284m
2477 734 54 None -28 28 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
36 734 54 None -28 28 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
437 734 54 None -28 28 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL49 734 54 None -28 28 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
DB00490 734 54 None -28 28 Bovine 4.6 pIC50 = 4.6 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
44342270 9837 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 9837 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
2286 3134 48 None -30 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3134 48 None -30 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3134 48 None -30 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3134 48 None -30 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3134 48 None -30 29 Human 5.6 pIC50 = 5.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
11730467 10925 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
CHEMBL117537 10925 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 476 10 0 2 6.0 O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1021/jm010878g
11080 28872 74 None -5 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 28872 74 None -5 6 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
5352624 66903 40 None -3 5 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
CHEMBL18797 66903 40 None -3 5 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
2662 11279 124 None -3 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
CHEMBL118 11279 124 None -3 31 Human 4.6 pIC50 = 4.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
13154762 102636 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL307717 102636 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
6603997 99448 8 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL286120 99448 8 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00086a016
15723883 204399 1 None - 1 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 294 6 0 2 3.8 c1ccc(CCCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm00116a003
CHEMBL85879 204399 1 None - 1 Rat 5.6 pIC50 = 5.6 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 294 6 0 2 3.8 c1ccc(CCCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm00116a003
31101 720 39 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 720 39 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 720 39 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 720 39 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 720 39 None -436 35 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10264175 108114 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@@H]21 10.1021/jm00002a013
CHEMBL320481 108114 1 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@@H]21 10.1021/jm00002a013
196129 67456 12 None -1819 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67456 12 None -1819 15 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
70684207 75717 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057452 75717 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70684207 75717 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057452 75717 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
14547415 100204 1 None - 4 Rat 4.5 pIC50 = 4.5 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
CHEMBL292274 100204 1 None - 4 Rat 4.5 pIC50 = 4.5 Binding
In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.In vitro binding activity against dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand.
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00130a008
73453 29403 22 None -208 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29403 22 None -208 17 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
195158 42905 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
CHEMBL150550 42905 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Compound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPACompound was tested in vitro for binding affinity against dopamine receptor D1 in rat striatal membrane by using DA antagonist [3H]NPA
ChEMBL 249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21 10.1021/jm00113a010
21589014 143540 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3903297 143540 0 None 1 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
10246528 27085 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136722 27085 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 0 2 4.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccccc32)CC1(C)C 10.1021/jm00022a004
10004036 94785 0 None 33 2 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL256075 94785 0 None 33 2 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
10570260 28229 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(F)c32)CC1(C)C 10.1021/jm00022a004
CHEMBL137536 28229 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(F)c32)CC1(C)C 10.1021/jm00022a004
70692655 75721 0 None 8 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057456 75721 0 None 8 2 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
15723897 9403 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 330 5 0 2 4.6 c1ccc(N2CCN(CCCc3ccc4ccccc4c3)CC2)cc1 10.1021/jm00116a003
CHEMBL112037 9403 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 330 5 0 2 4.6 c1ccc(N2CCN(CCCc3ccc4ccccc4c3)CC2)cc1 10.1021/jm00116a003
228 441 26 None -30 24 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
33 441 26 None -30 24 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
6005 441 26 None -30 24 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
CHEMBL53 441 26 None -30 24 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
DB00714 441 26 None -30 24 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00171a014
681 1437 65 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
940 1437 65 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
947 1437 65 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
CHEMBL59 1437 65 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
DB00988 1437 65 None -97 38 Rat 5.5 pIC50 = 5.5 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00171a014
9861399 33078 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 307 2 0 2 4.9 CCN1CCc2c(sc3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
CHEMBL141863 33078 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 307 2 0 2 4.9 CCN1CCc2c(sc3ccccc23)C(c2ccccc2)C1 10.1021/jm980156y
10251234 11141 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11141 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11141 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10429859 11937 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL1183429 11937 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL296395 11937 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
10476735 13619 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1195096 13619 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL553833 13619 0 None - 0 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9981024 95651 0 None - 1 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 95651 0 None - 1 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 95651 0 None - 1 Bovine 4.5 pIC50 = 4.5 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
44312603 103297 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 350 1 0 2 4.9 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL308843 103297 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 350 1 0 2 4.9 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
14728694 5277 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 2 0 3 4.1 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/jm00174a002
CHEMBL106886 5277 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 2 0 3 4.1 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc2c(c1-3)OCO2 10.1021/jm00174a002
44319215 13093 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 265 2 0 1 4.1 CN(C)[C@@]1(C)Cc2ccccc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL1191117 13093 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 265 2 0 1 4.1 CN(C)[C@@]1(C)Cc2ccccc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
CHEMBL542167 13093 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23390 as radioligand.
ChEMBL 265 2 0 1 4.1 CN(C)[C@@]1(C)Cc2ccccc2[C@H](c2ccccc2)C1 10.1021/jm00069a013
11057 175575 19 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 175575 19 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 175575 19 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 175575 19 None -2 20 Human 5.5 pIC50 = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
10809334 26641 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1(C)C 10.1021/jm00022a004
CHEMBL136334 26641 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1(C)C 10.1021/jm00022a004
6761 67457 17 None -5 18 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67457 17 None -5 18 Human 7.5 pIC50 = 7.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44285043 154272 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C\c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
CHEMBL40031 154272 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C\c2ccccc2)C1 10.1016/S0960-894X(97)00253-9
10043093 202161 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(Br)cc3CC[C@H]21 10.1021/jm00002a013
CHEMBL68680 202161 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(Br)cc3CC[C@H]21 10.1021/jm00002a013
70690497 75710 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057438 75710 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
70690497 75710 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL2057438 75710 0 None 3 2 Human 6.5 pIC50 = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
13994412 11060 1 None -117 3 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
CHEMBL117841 11060 1 None -117 3 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00164a022
7055406 188754 3 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 299 4 2 4 2.8 COc1ccc(C[C@H]2NCCc3cc(O)c(OC)cc32)cc1 10.1021/np980008a
CHEMBL512542 188754 3 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH-23390 from rat striatal dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat striatal dopamine D1 receptor
ChEMBL 299 4 2 4 2.8 COc1ccc(C[C@H]2NCCc3cc(O)c(OC)cc32)cc1 10.1021/np980008a
9816455 16612 6 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@H]2CNC3 10.1021/jm0101545
CHEMBL124561 16612 6 None - 0 Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@H]2CNC3 10.1021/jm0101545
130907 193017 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL53294 193017 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
10091430 9788 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1 10.1016/0960-894X(96)00174-6
CHEMBL11425 9788 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1 10.1016/0960-894X(96)00174-6
457825 172085 37 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3cc(c(OC)cc3CCN1C)Oc1c(OC)c(OC)cc3c1[C@@H](C2)N(C)CC3 10.1021/np50087a016
CHEMBL449690 172085 37 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3cc(c(OC)cc3CCN1C)Oc1c(OC)c(OC)cc3c1[C@@H](C2)N(C)CC3 10.1021/np50087a016
CHEMBL506025 172085 37 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3cc(c(OC)cc3CCN1C)Oc1c(OC)c(OC)cc3c1[C@@H](C2)N(C)CC3 10.1021/np50087a016
130907 193017 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL53294 193017 5 None -3311 4 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
44370718 119035 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
CHEMBL345822 119035 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(Br)c(O)c1-3 10.1021/jm00164a022
1353 1880 85 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
3559 1880 85 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
86 1880 85 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
CHEMBL54 1880 85 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
DB00502 1880 85 None -74 85 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligandBinding affinity towards Dopamine receptor D1 in rat membranes using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00116a003
10548369 30231 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 388 2 0 2 5.6 CN1CCN(C2CC(c3ccc(Cl)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL139258 30231 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 388 2 0 2 5.6 CN1CCN(C2CC(c3ccc(Cl)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
9979258 97665 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 415 3 2 2 4.9 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL273526 97665 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 415 3 2 2 4.9 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
44267181 9520 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.
ChEMBL 277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL11262 9520 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.Compound was evaluated for the binding affinity towards Dopamine receptor D1 by displacement of [3H]raclopride.
ChEMBL 277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
6852376 91167 11 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
CHEMBL1467585 91167 11 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
CHEMBL24077 91167 11 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
CHEMBL503958 91167 11 None -4 5 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00168a034
44269085 24785 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13464 24785 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
180 397 50 None -109 38 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -109 38 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -109 38 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -109 38 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -109 38 Human 6.5 pIC50 = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
1353 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
3559 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
86 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
CHEMBL54 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
DB00502 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991005d
1353 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
3559 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
86 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
CHEMBL54 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
DB00502 1880 85 None -74 85 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9704457
164710 95151 6 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 4 2.5 Oc1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
CHEMBL257746 95151 6 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 4 2.5 Oc1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
736083 161665 15 None -50 2 Rat 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00164a022
CHEMBL416288 161665 15 None -50 2 Rat 5.4 pIC50 = 5.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00164a022
10619325 27302 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136891 27302 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1(C)C 10.1021/jm00022a004
71110290 146627 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3927835 146627 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
681 1437 65 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
940 1437 65 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
947 1437 65 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
CHEMBL59 1437 65 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
DB00988 1437 65 None -97 38 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00101a018
4011 81996 43 None -64 23 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81996 43 None -64 23 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
11005810 10367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10367 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
44358128 26807 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 324 2 0 2 4.0 Cc1ccc2c(c1)C(N1CCN(C)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL136480 26807 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 324 2 0 2 4.0 Cc1ccc2c(c1)C(N1CCN(C)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
14901835 12806 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(O)c(F)c1 10.1021/jm00171a014
CHEMBL1189074 12806 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(O)c(F)c1 10.1021/jm00171a014
CHEMBL538012 12806 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(O)c(F)c1 10.1021/jm00171a014
10527884 28162 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2 10.1021/jm950861w
CHEMBL137486 28162 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2 10.1021/jm950861w
44269075 28407 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13770 28407 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
10550367 114708 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2 10.1021/jm950861w
CHEMBL334498 114708 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2 10.1021/jm950861w
228 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
33 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
6005 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
CHEMBL53 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
DB00714 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Compound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligandCompound was tested in vitro for binding affinity towards Dopamine receptor D1 in rat striatal membrane by using [3H]-SCH- 23390 as radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00113a010
228 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
33 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
6005 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
CHEMBL53 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
DB00714 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390In vitro binding affinity to Dopamine receptor D1 in rat striatal membranes using D1 antagonist [3H]SCH-23390
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/S0960-894X(01)80462-5
228 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
33 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
6005 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
CHEMBL53 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
DB00714 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determinedInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 was determined
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a051
2351 3234 60 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3234 60 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3234 60 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3234 60 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3234 60 None -16 21 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
12488 1627 51 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1627 51 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1627 51 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1627 51 None -19 23 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
13154803 116249 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 386 5 1 4 3.7 CSc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL337542 116249 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 386 5 1 4 3.7 CSc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
100231 177344 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3c(cc(OC)c(OC)c3Oc3cc4c(cc3OC)CCN(C)[C@@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL451211 177344 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3c(cc(OC)c(OC)c3Oc3cc4c(cc3OC)CCN(C)[C@@H]4C2)CCN1C 10.1021/np50087a016
CHEMBL464525 177344 5 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 4 0 8 7.2 COc1ccc2cc1Oc1ccc(cc1)C[C@H]1c3c(cc(OC)c(OC)c3Oc3cc4c(cc3OC)CCN(C)[C@@H]4C2)CCN1C 10.1021/np50087a016
191 399 92 None -26 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -26 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -26 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -26 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -26 28 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
121852 10071 7 None - 1 Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL11592 10071 7 None - 1 Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL301060 10071 7 None - 1 Human 4.4 pIC50 = 4.4 Binding
Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.Compound was evaluated for the Dopamine receptor D1 by displacement of [3H]SCH-23390.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
10452020 117772 2 None - 3 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL34095 117772 2 None - 3 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm00086a016
3036864 201066 16 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
CHEMBL1256645 201066 16 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
CHEMBL1814790 201066 16 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
CHEMBL62 201066 16 None -2 27 Rat 8.4 pIC50 = 8.4 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm980156y
3036864 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
3036864 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1256645 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL1814790 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
CHEMBL62 201066 16 None -2 27 Human 8.4 pIC50 = 8.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/acsmedchemlett.9b00575
10809335 26793 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccccc3F)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136468 26793 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccccc3F)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
70690500 75720 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057455 75720 0 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
3496768 95296 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 0 1 4 2.9 CN1CCc2cc3c(c4c2C1Cc1cccc(O)c1-4)OCO3 10.1021/jm060959i
CHEMBL258370 95296 3 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 0 1 4 2.9 CN1CCc2cc3c(c4c2C1Cc1cccc(O)c1-4)OCO3 10.1021/jm060959i
10154 141597 54 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL388342 141597 54 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
10154 141597 54 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL388342 141597 54 None -58 4 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/np990433j
9981671 14372 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
CHEMBL12028 14372 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
121852 10071 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10071 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10071 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251234 11141 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11141 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11141 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10047322 96692 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL26783 96692 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL50993 96692 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
10251673 99030 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283207 99030 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52396 99030 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10070029 164865 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL423841 164865 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54089 164865 0 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10265863 192721 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
CHEMBL52438 192721 0 None - 0 Bovine 4.4 pIC50 = 4.4 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
121852 10071 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 10071 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 10071 7 None - 1 Bovine 4.4 pIC50 = 4.4 Binding
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
2247 502 77 None -61 41 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -61 41 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -61 41 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -61 41 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -61 41 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
134551 355 25 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 355 25 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 355 25 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 355 25 None -28 21 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
146025811 171195 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171195 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
146025811 171195 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4467483 171195 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1c(Br)ccc3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
5353853 17803 41 None -19 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17803 41 None -19 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17803 41 None -19 15 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10498684 31424 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 359 3 2 2 3.6 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL14048 31424 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 359 3 2 2 3.6 CN1C[C@H](CNC(=O)c2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
71474079 142732 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3896731 142732 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
2337 3205 72 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3205 72 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3205 72 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3205 72 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3205 72 None -53 62 Human 6.4 pIC50 = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
11016 201913 31 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 173 3 0 1 0.0 O=P(N1CC1)(N1CC1)N1CC1 10.1021/jm980284m
CHEMBL670 201913 31 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 173 3 0 1 0.0 O=P(N1CC1)(N1CC1)N1CC1 10.1021/jm980284m
228 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
33 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
6005 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
CHEMBL53 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
DB00714 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/s0960-894x(01)00076-2
228 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
33 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
6005 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
CHEMBL53 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
DB00714 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00164a022
332915 29505 3 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 240 0 1 1 3.1 C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL13866 29505 3 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 240 0 1 1 3.1 C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
10712649 118702 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
CHEMBL343282 118702 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1 10.1021/jm00022a004
5353432 97046 84 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97046 84 None -1 3 Human 5.4 pIC50 = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
44323870 111102 0 None 3 4 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL328246 111102 0 None 3 4 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
228 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
33 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
6005 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
CHEMBL53 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
DB00714 441 26 None -30 24 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
9864292 29894 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1(C)C 10.1021/jm00022a004
CHEMBL138964 29894 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3c(Cl)cccc32)CC1(C)C 10.1021/jm00022a004
70682088 75715 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057446 75715 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
14004813 58972 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 307 3 0 2 4.1 COc1cccc2c1CC1CCCN(Cc3ccccc3)C1C2 10.1016/s0960-894x(01)00076-2
CHEMBL170475 58972 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranesInhibition of binding of [3H]SCH-23390 to Dopamine receptor D1 in rat striatal membranes
ChEMBL 307 3 0 2 4.1 COc1cccc2c1CC1CCCN(Cc3ccccc3)C1C2 10.1016/s0960-894x(01)00076-2
CHEMBL1200633 206858 3 None -7 8 Human 5.3 pIC50 = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
44269057 31128 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 412 2 3 3 3.4 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL14020 31128 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 412 2 3 3 3.4 CC(=O)NC(=S)NC[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
71110293 142847 0 None 6 3 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 142847 0 None 6 3 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
2389 3279 114 None -467 67 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3279 114 None -467 67 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3279 114 None -467 67 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3279 114 None -467 67 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3279 114 None -467 67 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
44358098 118779 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 292 2 0 2 3.5 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
CHEMBL343820 118779 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 292 2 0 2 3.5 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
133381 95150 8 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 4 2.8 COc1c2c3c(c4c1OCO4)-c1ccccc1C[C@H]3NCC2 10.1021/jm060959i
CHEMBL257745 95150 8 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 4 2.8 COc1c2c3c(c4c1OCO4)-c1ccccc1C[C@H]3NCC2 10.1021/jm060959i
71110293 142847 0 None 6 3 Human 6.3 pIC50 = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 142847 0 None 6 3 Human 6.3 pIC50 = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
71474026 153765 0 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
CHEMBL3986624 153765 0 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
45482789 197247 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
CHEMBL584554 197247 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 428 4 2 2 4.5 CCN(CC)C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C(=O)Nc2ccccc2)C1 10.1016/j.bmcl.2009.09.002
5024 118745 22 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 297 3 0 3 3.3 COc1cc2c(cc1OC)C(c1ccccc1)CN(C)CC2 10.1021/jm980156y
CHEMBL343569 118745 22 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 297 3 0 3 3.3 COc1cc2c(cc1OC)C(c1ccccc1)CN(C)CC2 10.1021/jm980156y
10742 3560 27 None 2 7 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00086a016
1225 3560 27 None 2 7 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00086a016
CHEMBL35354 3560 27 None 2 7 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00086a016
13154762 102636 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
CHEMBL307717 102636 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1 10.1021/jm00022a004
6603820 95330 13 None 1 13 Rat 8.3 pIC50 = 8.3 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
CHEMBL25856 95330 13 None 1 13 Rat 8.3 pIC50 = 8.3 Binding
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00041a025
10617001 30940 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 1 2 4.4 Cc1ccc2c(c1)C(N1CCNC(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL140032 30940 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 338 2 1 2 4.4 Cc1ccc2c(c1)C(N1CCNC(C)(C)C1)CC2c1ccc(F)cc1 10.1021/jm00022a004
6852376 91167 11 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL1467585 91167 11 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL24077 91167 11 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
CHEMBL503958 91167 11 None -4 5 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00086a016
11794523 30024 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 385 2 0 2 5.7 CCN1CCc2c(sc3ccccc23)C(c2cccc(Br)c2)C1 10.1021/jm980156y
CHEMBL139081 30024 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 385 2 0 2 5.7 CCN1CCc2c(sc3ccccc23)C(c2cccc(Br)c2)C1 10.1021/jm980156y
10712993 118243 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 352 3 0 4 4.8 CCN1CCc2c(sc3ccccc23)C(c2cccc([N+](=O)[O-])c2)C1 10.1021/jm980156y
CHEMBL341805 118243 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 352 3 0 4 4.8 CCN1CCc2c(sc3ccccc23)C(c2cccc([N+](=O)[O-])c2)C1 10.1021/jm980156y
10251234 11141 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11141 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11141 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10364722 98628 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 98628 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 98628 0 None - 1 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10072866 195799 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51561 195799 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL56990 195799 0 None - 0 Bovine 4.3 pIC50 = 4.3 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
11099480 188556 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1ccc2c(c1O)Oc1c(OC)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL510777 188556 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1ccc2c(c1O)Oc1c(OC)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
44370629 50786 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
CHEMBL157879 50786 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00164a022
10246432 13689 2 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 255 7 1 2 3.7 CCCN(CCC)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL1195595 13689 2 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 255 7 1 2 3.7 CCCN(CCC)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
CHEMBL554950 13689 2 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 255 7 1 2 3.7 CCCN(CCC)CCc1ccc(Cl)c(O)c1 10.1021/jm00101a018
44379650 120244 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL355107 120244 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
10574585 27218 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL136822 27218 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
13154795 28687 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 4 1 3 3.3 Cc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL137954 28687 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 354 4 1 3 3.3 Cc1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
10582557 193062 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 309 4 0 3 4.0 CCCN1CCc2cc3c(cc2[C@@H]1Cc1ccccc1)OCO3 10.1021/jm001128u
CHEMBL53520 193062 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]-SCH- 23390 binding to the rat striatal membranesInhibition of [3H]-SCH- 23390 binding to the rat striatal membranes
ChEMBL 309 4 0 3 4.0 CCCN1CCc2cc3c(cc2[C@@H]1Cc1ccccc1)OCO3 10.1021/jm001128u
11795296 26562 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136260 26562 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
10424479 108381 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 293 2 1 2 4.1 CCCN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
CHEMBL321040 108381 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 293 2 1 2 4.1 CCCN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21 10.1021/jm00002a013
10923047 16332 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@@H]2CNC3 10.1021/jm0101545
CHEMBL123642 16332 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1[C@@H]2CNC3 10.1021/jm0101545
4543 169982 36 None -5 29 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169982 36 None -5 29 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169982 36 None -5 29 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
44312870 202871 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL73082 202871 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
44323876 204856 0 None 2 4 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
CHEMBL88870 204856 0 None 2 4 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00164a053
135 2496 38 None -91 57 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2496 38 None -91 57 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2496 38 None -91 57 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2496 38 None -91 57 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2496 38 None -91 57 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
10828627 102689 18 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm991005d
CHEMBL308090 102689 18 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm991005d
15521599 202833 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm991005d
CHEMBL72794 202833 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm991005d
10828627 102689 18 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm9704457
CHEMBL308090 102689 18 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3ccccc3Nc3ccc(O)cc32)CC1 10.1021/jm9704457
15521599 202833 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm9704457
CHEMBL72794 202833 6 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1ccccc1N2 10.1021/jm9704457
10264174 9596 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@H]21 10.1021/jm00002a013
CHEMBL113053 9596 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 251 0 2 2 2.9 Oc1cccc2c1CC[C@H]1NCc3ccccc3[C@H]21 10.1021/jm00002a013
70692656 75722 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057457 75722 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692656 75722 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057457 75722 0 None 5 2 Human 7.3 pIC50 = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
10031670 12358 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 610 9 2 8 6.5 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3OC)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL1186148 12358 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 610 9 2 8 6.5 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3OC)cc1)N(C)CC2 10.1021/np50087a016
CHEMBL451734 12358 1 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 610 9 2 8 6.5 COc1cc2c(cc1O)[C@H](Cc1ccc(Oc3cc(C[C@@H]4c5cc(O)c(OC)cc5CCN4C)ccc3OC)cc1)N(C)CC2 10.1021/np50087a016
44370651 46487 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1c(Cl)ccc(O)c1-3 10.1021/jm00164a022
CHEMBL153960 46487 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1c(Cl)ccc(O)c1-3 10.1021/jm00164a022
3561 18886 34 None -1 11 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 18886 34 None -1 11 Human 6.3 pIC50 = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
14137099 172122 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 638 11 0 8 7.1 COc1cc2c(cc1OC)[C@H](Cc1ccc(OC)c(Oc3ccc(C[C@@H]4c5cc(OC)c(OC)cc5CCN4C)cc3)c1)N(C)CC2 10.1021/np50087a016
CHEMBL450147 172122 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 638 11 0 8 7.1 COc1cc2c(cc1OC)[C@H](Cc1ccc(OC)c(Oc3ccc(C[C@@H]4c5cc(OC)c(OC)cc5CCN4C)cc3)c1)N(C)CC2 10.1021/np50087a016
CHEMBL507970 172122 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 638 11 0 8 7.1 COc1cc2c(cc1OC)[C@H](Cc1ccc(OC)c(Oc3ccc(C[C@@H]4c5cc(OC)c(OC)cc5CCN4C)cc3)c1)N(C)CC2 10.1021/np50087a016
44269131 30695 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 381 2 2 4 3.2 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL13979 30695 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 381 2 2 4 3.2 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
71041800 162191 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 290 7 3 6 2.2 CCC[C@@H](CCO)Nc1nc(N)nc2cc(OC)ccc12 10.1021/acs.jmedchem.8b00643
CHEMBL4171368 162191 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 290 7 3 6 2.2 CCC[C@@H](CCO)Nc1nc(N)nc2cc(OC)ccc12 10.1021/acs.jmedchem.8b00643
44285013 153206 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 319 7 0 1 5.4 C(=C\C1CCCN(CCCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL39818 153206 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 319 7 0 1 5.4 C(=C\C1CCCN(CCCCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
1042 1551 20 None -204 16 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1551 20 None -204 16 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1551 20 None -204 16 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1551 20 None -204 16 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1551 20 None -204 16 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
10693049 118863 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 412 2 0 2 6.0 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCCC2 10.1021/jm00022a004
CHEMBL344426 118863 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 412 2 0 2 6.0 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCCC2 10.1021/jm00022a004
10810927 118791 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
CHEMBL343922 118791 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2 10.1021/jm00022a004
146299 172805 7 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL452776 172805 7 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 313 1 2 5 3.0 COc1cc2c(cc1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
44267790 15348 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 431 6 1 10 1.9 Cc1sc2nc(SCCCN3CCN(c4ncccn4)CC3)n(N)c(=O)c2c1C 10.1021/jm950866t
CHEMBL12177 15348 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
In vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]SCH-23390 binding to Dopamine receptor D1 in rat striatal membrane
ChEMBL 431 6 1 10 1.9 Cc1sc2nc(SCCCN3CCN(c4ncccn4)CC3)n(N)c(=O)c2c1C 10.1021/jm950866t
118731187 117676 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 613 10 3 7 6.1 CCOc1nc(NC(=O)C(C)(C)NC(=O)c2ccc3c(C4CCCC4)c(-c4ccc(F)cn4)n(C)c3c2)ccc1/C=C/C(=O)O 10.1016/j.bmcl.2014.12.078
CHEMBL3408841 117676 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 613 10 3 7 6.1 CCOc1nc(NC(=O)C(C)(C)NC(=O)c2ccc3c(C4CCCC4)c(-c4ccc(F)cn4)n(C)c3c2)ccc1/C=C/C(=O)O 10.1016/j.bmcl.2014.12.078
10092409 11941 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1183479 11941 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL299561 11941 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10095594 12262 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1185501 12262 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL417550 12262 0 None - 0 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10364722 98628 0 None - 1 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280608 98628 0 None - 1 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51888 98628 0 None - 1 Bovine 4.2 pIC50 = 4.2 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL3215298 209485 12 None -6 2 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(C=C[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(C=C[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
14901811 13426 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 155 2 2 2 1.0 NCCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1193777 13426 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 155 2 2 2 1.0 NCCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL545240 13426 6 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 155 2 2 2 1.0 NCCc1ccc(F)c(O)c1 10.1021/jm00171a014
10809333 26984 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136630 26984 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
4189 205195 91 None -25 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -25 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -25 34 Human 5.2 pIC50 = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
16104 161368 15 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00130a006
CHEMBL415300 161368 15 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00130a006
16104 161368 15 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00164a053
CHEMBL415300 161368 15 None -1 5 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00164a053
44285030 131969 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 291 5 0 1 4.7 C(=C\C1CCCN(CCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
CHEMBL36979 131969 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.Binding affinity at dopamine D1 receptor in rat striatum by [3H]SCH-22390 displacement.
ChEMBL 291 5 0 1 4.7 C(=C\C1CCCN(CCc2ccccc2)C1)\c1ccccc1 10.1016/S0960-894X(97)00253-9
23930365 95203 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c3c(c1OC)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1021/jm060959i
CHEMBL257957 95203 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c3c(c1OC)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1021/jm060959i
44370725 119047 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(Cl)c(O)c1-3 10.1021/jm00164a022
CHEMBL345907 119047 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 285 0 1 2 3.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(Cl)c(O)c1-3 10.1021/jm00164a022
9954899 202758 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL72292 202758 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
9954899 202758 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm9704457
CHEMBL72292 202758 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3ccccc3Nc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm9704457
167715 2832 12 None -954 5 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
969 2832 12 None -954 5 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
CHEMBL225230 2832 12 None -954 5 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00174a002
71109986 150100 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
CHEMBL3955446 150100 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
9904738 101186 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 309 2 2 3 3.8 CCCN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
CHEMBL299161 101186 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 309 2 2 3 3.8 CCCN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
13154798 26565 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 382 5 1 3 4.1 CC(C)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL136262 26565 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 382 5 1 3 4.1 CC(C)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
10026300 167271 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
CHEMBL430798 167271 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 441 2 0 7 3.3 CN1CCN(C2=Nc3ccccc3Oc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1 10.1021/jm991005d
10409038 84818 0 None -41 4 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL225853 84818 0 None -41 4 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
3081681 98062 4 None - 0 Rat 5.2 pIC50 = 5.2 Binding
compound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissuecompound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissue
ChEMBL 442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm00107a028
CHEMBL276175 98062 4 None - 0 Rat 5.2 pIC50 = 5.2 Binding
compound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissuecompound was measured as affinity for dopamine receptor D1 labeled with [3H]-SCH- 23390 radioligand in striatum tissue
ChEMBL 442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm00107a028
5249490 14989 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1C2CNC3 10.1021/jm0101545
CHEMBL120995 14989 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membraneIn vitro inhibition of [125I]SCH-23982 binding to Dopamine receptor D1 of rat striatal membrane
ChEMBL 253 0 3 3 2.2 Oc1ccc2c(c1O)Cc1cccc3c1C2CNC3 10.1021/jm0101545
2105 3005 34 None -537 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3005 34 None -537 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3005 34 None -537 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3005 34 None -537 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3005 34 None -537 33 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
70690499 75718 0 None 9 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057453 75718 0 None 9 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
160597 154536 23 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 3 2.8 c1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
CHEMBL401798 154536 23 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 3 2.8 c1ccc2c(c1)C[C@H]1NCCc3cc4c(c-2c31)OCO4 10.1021/jm060959i
70682090 75716 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057451 75716 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70682090 75716 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057451 75716 0 None -1 2 Human 6.2 pIC50 = 6.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
3158 55974 21 None -2398 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55974 21 None -2398 20 Human 6.2 pIC50 = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
2601 3721 30 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
443951 3721 30 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
56 3721 30 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
CHEMBL73151 3721 30 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
DB13399 3721 30 None - 21 Rat 7.2 pIC50 = 7.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm00130a008
13154822 30276 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 418 5 1 5 2.4 CS(=O)(=O)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
CHEMBL139304 30276 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 418 5 1 5 2.4 CS(=O)(=O)c1ccc2c(c1)C(N1CCN(CCO)CC1)CC2c1ccc(F)cc1 10.1021/jm00022a004
6603820 95330 13 None 1 13 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
CHEMBL25856 95330 13 None 1 13 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00002a013
71474025 144794 0 None 131 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 144794 0 None 131 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
11539632 70217 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70217 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
44354823 24370 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 241 1 1 2 2.2 C#CCN1CCCC2Cc3c(O)cccc3CC21 10.1021/jm980284m
CHEMBL134273 24370 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 241 1 1 2 2.2 C#CCN1CCCC2Cc3c(O)cccc3CC21 10.1021/jm980284m
16038374 93911 88 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptorDisplacement of [3H]SCH-23390 from dopamine D1 receptor
ChEMBL 357 5 1 4 4.9 COc1cc(NC(=O)c2ccc(-c3ccc(Cl)cc3)o2)cc(OC)c1 10.1073/pnas.0611364104
CHEMBL250699 93911 88 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptorDisplacement of [3H]SCH-23390 from dopamine D1 receptor
ChEMBL 357 5 1 4 4.9 COc1cc(NC(=O)c2ccc(-c3ccc(Cl)cc3)o2)cc(OC)c1 10.1073/pnas.0611364104
10571551 116067 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 375 2 0 2 6.2 CCN1CCc2c(sc3ccccc23)C(c2ccc(Cl)c(Cl)c2)C1 10.1021/jm980156y
CHEMBL336437 116067 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390Relative affinity for Dopamine receptor D1 in striatum using [3H]SCH-23390
ChEMBL 375 2 0 2 6.2 CCN1CCc2c(sc3ccccc23)C(c2ccc(Cl)c(Cl)c2)C1 10.1021/jm980156y
135398745 2869 108 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2869 108 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2869 108 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2869 108 None -26 65 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
49836386 18364 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
CHEMBL1275709 18364 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity to dopamine D1Binding affinity to dopamine D1
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
44269142 31913 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL14089 31913 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 437 2 2 4 4.5 CN1C[C@H](C(=O)Nc2ccc(Cl)nn2)C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
15115475 26639 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 322 4 1 3 2.9 OCCN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
CHEMBL136333 26639 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 322 4 1 3 2.9 OCCN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1 10.1021/jm00022a004
12441 50818 19 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm00164a022
CHEMBL157912 50818 19 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm00164a022
44269091 97969 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
CHEMBL275539 97969 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 394 2 2 3 3.0 CN1C[C@H](CN2CC(=O)NC2=O)C[C@@H]2c3cc(C(C)(C)C)cc4[nH]cc(c34)C[C@H]21 10.1016/s0960-894x(98)00166-8
44312604 202746 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 338 1 0 2 4.6 CC1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
CHEMBL72220 202746 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against Dopamine receptor D1 in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 338 1 0 2 4.6 CC1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00130a006
133 2460 48 None -30 42 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2460 48 None -30 42 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2460 48 None -30 42 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2460 48 None -30 42 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2460 48 None -30 42 Human 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
12441 50818 19 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm060959i
CHEMBL157912 50818 19 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 1 1 5 2.9 COc1ccc2c(c1O)-c1c3c(cc4c1[C@H](C2)N(C)CC4)OCO3 10.1021/jm060959i
5018 3493 8 None 2 9 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
943 3493 8 None 2 9 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
946 3493 8 None 2 9 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
CHEMBL13668 3493 8 None 2 9 Human 6.1 pIC50 = 6.1 Binding
[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.[35S]GTPγS Binding Assay: For detecting the agonism action of the compounds, the [35S]GTPγS binding assay was performed at 30° C. for 40 mins in reaction buffer containing 50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, 100 mM NaCl and 1 mM (DL)-dithiothreitol (DTT). The assay mixture (200 μL) contained 30 μg of membraneprotein, 0.1 nM [35S]GTPγS, and 40 μM guanosine triphosphate (GDP) with various concentration of the compound. The D1 receptor agonist SKF38393 and sntagonist SCH23390 were used for reference. Non specific binding was measured in the presence of 100 μM 50-guanylimidodiphosphate (Gpp(NH)p). The reaction was terminated by adding 3 mL of ice-cold washing buffer (50 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EDTA, and 100 mM NaCl) and was rapidly filtered with GF/C glass fiber filters (Whatman) and rinsed for three times.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
135686415 202870 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm991005d
CHEMBL73074 202870 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm991005d
135686415 202870 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm9704457
CHEMBL73074 202870 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 322 1 1 5 3.1 COc1ccc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm9704457
3294 1975 106 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
71360 1975 106 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
87 1975 106 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
CHEMBL14376 1975 106 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
DB04946 1975 106 None - 44 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1021/jm00007a009
10144 137882 39 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 275 0 0 4 3.2 O=C1c2ccccc2-c2c3c(cc4ccnc1c24)OCO3 10.1021/jm060959i
CHEMBL37736 137882 39 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 275 0 0 4 3.2 O=C1c2ccccc2-c2c3c(cc4ccnc1c24)OCO3 10.1021/jm060959i
44269092 28873 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 296 0 1 1 4.4 C[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL13811 28873 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 296 0 1 1 4.4 C[C@@H]1C[C@@H]2c3ccc(C(C)(C)C)c4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
11059058 9996 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
CHEMBL115444 9996 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
71110287 145792 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3921127 145792 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
448537 159703 86 None -28 25 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159703 86 None -28 25 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
44312605 202730 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
CHEMBL72162 202730 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 336 1 0 2 4.5 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1021/jm00164a053
13720693 99212 2 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00086a016
CHEMBL284473 99212 2 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatumDisplacement of [3H]-SCH- 23390 (0.3 nM) from dopamine receptor D1 in crude membrane fraction of rat brain corpus striatum
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00086a016
71109897 87085 0 None 7 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
CHEMBL2334893 87085 0 None 7 2 Human 8.1 pIC50 = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
10478809 164326 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
CHEMBL422067 164326 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.The compound was tested for the binding affinity against Dopamine receptor D1 activity is expressed as IC50 values.
ChEMBL 374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00022a004
10787201 28519 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 4 0 2 5.9 CCC1(CC)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
CHEMBL137805 28519 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 400 4 0 2 5.9 CCC1(CC)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1C 10.1021/jm00022a004
44354809 116042 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 3.8 COc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
CHEMBL336274 116042 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranesDisplacement of [3H]-SCH- 23390 from Dopamine receptor D1 of rat striatal membranes
ChEMBL 383 3 0 2 3.8 COc1cccc2c1CC1CCCN(C/C=C/I)C1C2 10.1021/jm980284m
100 3745 52 None -16 55 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
2637 3745 52 None -16 55 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
5452 3745 52 None -16 55 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
CHEMBL479 3745 52 None -16 55 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
DB00679 3745 52 None -16 55 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brainDisplacement of [3H]cis-flupenthixol from Dopamine receptor D1 in rat brain
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1021/jm00397a032
681 1437 65 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
940 1437 65 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
947 1437 65 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
CHEMBL59 1437 65 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
DB00988 1437 65 None -97 38 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00168a034
442203 173986 3 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1cc2c(cc1OC)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL455633 173986 3 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 1 5 3.3 COc1cc2c(cc1OC)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
10504100 47476 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane
ChEMBL 458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
CHEMBL154787 47476 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]spiperone binding to Dopamine receptor D2 in rat striatal membrane
ChEMBL 458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
14901825 12977 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 287 7 1 2 3.6 CCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL1190275 12977 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 287 7 1 2 3.6 CCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
CHEMBL540546 12977 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranesCompound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes
ChEMBL 287 7 1 2 3.6 CCN(CCc1ccccc1)CCc1ccc(F)c(O)c1 10.1021/jm00171a014
10024943 96940 0 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26975 96940 0 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52485 96940 0 None - 1 Bovine 4.1 pIC50 = 4.1 Binding
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10406315 192722 0 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 361 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
CHEMBL524439 192722 0 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membraneDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane
ChEMBL 361 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C 10.1021/np990433j
146025813 175014 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
CHEMBL4579687 175014 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAntagonist activity at C-terminal RLuc8-fused D1R (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 373 2 0 3 4.2 COc1ccc2c(c1OC)-c1ccc(Br)c3c1[C@@H](C2)N(C)CC3 10.1021/acsmedchemlett.9b00575
44370706 47708 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1cc(Br)cc(O)c1-3 10.1021/jm00164a022
CHEMBL154989 47708 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@H]1Cc1cc(Br)cc(O)c1-3 10.1021/jm00164a022
10409556 161822 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
CHEMBL416523 161822 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390Binding affinity towards Dopamine receptor D1 by displacement of [3H]SCH-23,390
ChEMBL 414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
15657207 204614 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 287 2 2 2 3.7 CNC1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00069a013
CHEMBL87321 204614 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligandBinding affinity against dopamine receptor D1 from rat striatal homogenates, using [3H]SCH-23,390 as radioligand
ChEMBL 287 2 2 2 3.7 CNC1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00069a013
44269058 31151 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
CHEMBL14022 31151 0 None - 1 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
ChEMBL 425 6 2 4 2.6 CCNC(=O)N(CCCN(C)C)C(=O)[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 10.1016/s0960-894x(98)00166-8
1016 3690 75 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -29 35 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44370645 119057 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
CHEMBL346017 119057 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.In vitro binding affinity towards rat Dopamine receptor D1 by [3H]SCH-23390 displacement.
ChEMBL 329 0 1 2 3.9 CN1CCc2cccc3c2[C@@H]1Cc1c(Br)ccc(O)c1-3 10.1021/jm00164a022
1530 2151 44 None -53 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -53 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -53 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -53 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -53 20 Human 6.1 pIC50 = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
10522247 26526 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136235 26526 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C 10.1021/jm00022a004
16103 202932 37 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00130a006
CHEMBL73538 202932 37 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligandBinding activity against dopamine D1 receptor in rat brain, using [3H]SCH-23390 as the radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00130a006
16103 202932 37 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00164a053
CHEMBL73538 202932 37 None -2 4 Rat 6.1 pIC50 = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brainBinding affinity against Dopamine receptor D1 using [3H]-SCN 23390 in rat brain
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00164a053
71454427 78111 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
CHEMBL2111937 78111 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3cc(Cl)ccc32)CC1 10.1021/jm00022a004
44329358 107038 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
CHEMBL318714 107038 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 344 2 0 2 4.3 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1 10.1021/jm00072a006
10833129 27283 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3cccc(F)c3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
CHEMBL136873 27283 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
ChEMBL 372 2 0 2 5.1 CN1CCN(C2CC(c3cccc(F)c3)c3ccc(Cl)cc32)CC1(C)C 10.1021/jm00022a004
15648963 16714 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 340 2 0 2 5.1 CN1CC=C(c2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/jm00072a006
CHEMBL12507 16714 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranesBinding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes
ChEMBL 340 2 0 2 5.1 CN1CC=C(c2cn(-c3ccc(F)cc3)c3ccc(Cl)cc23)CC1 10.1021/jm00072a006
70690500 75720 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 75720 0 None - 1 Human 8.0 pIC50 = 8.0 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
9804849 67117 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67117 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against dopamine receptor D1Inhibitory concentration against dopamine receptor D1
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
2812 4711 96 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -32 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
44584686 12583 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@@H](C(=O)c1ccc(O)c(c1)-c1cc(ccc1OC)C[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL1187479 12583 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@@H](C(=O)c1ccc(O)c(c1)-c1cc(ccc1OC)C[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
CHEMBL504303 12583 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 622 3 2 9 6.1 COc1cc2c3cc1Oc1c(O)c(OC)cc4c1[C@@H](C(=O)c1ccc(O)c(c1)-c1cc(ccc1OC)C[C@H]3N(C)CC2)N(C)CC4 10.1021/np50087a016
11543723 188510 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
CHEMBL51017 188510 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1021/jm00168a034
176 394 63 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -4 31 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
3198 203802 73 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -31 34 Human 5.0 pIC50 = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
114876 12684 4 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm00101a018
CHEMBL1188090 12684 4 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm00101a018
CHEMBL545783 12684 4 None - 5 Rat 4.0 pIC50 = 4.0 Binding
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
ChEMBL 283 8 1 2 3.9 CCCN(CCc1ccccc1)CCc1cccc(O)c1 10.1021/jm00101a018
135515198 104271 6 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL310712 104271 6 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
135515198 104271 6 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
CHEMBL310712 104271 6 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 440 2 1 7 3.3 CN1CCN(C2=Nc3cc(OS(=O)(=O)C(F)(F)F)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
134 2478 19 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2478 19 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2478 19 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2478 19 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2478 19 None -263 67 Human 6.0 pIC50 = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
11778475 162744 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3ccc(O)c(O)c3CC[C@H]21 10.1021/jm00002a013
CHEMBL418791 162744 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 by using [3H]SCH-23390 as radioligand
ChEMBL 281 0 2 3 3.0 CN1Cc2ccccc2[C@@H]2c3ccc(O)c(O)c3CC[C@H]21 10.1021/jm00002a013
66572162 75343 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 363 6 1 3 5.2 OC(CCN1CC=C(Cc2ccccc2)CC1)c1cc2ccccc2s1 10.1016/j.ejmech.2012.04.030
CHEMBL2047561 75343 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 363 6 1 3 5.2 OC(CCN1CC=C(Cc2ccccc2)CC1)c1cc2ccccc2s1 10.1016/j.ejmech.2012.04.030
10907460 9735 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL113956 9735 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
ChEMBL 521 11 1 3 5.8 CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
25053021 109184 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
CHEMBL322574 109184 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00174a002
25053021 109184 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL322574 109184 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 373 2 2 3 4.4 CCCN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
70686343 75719 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057454 75719 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
135508767 202425 18 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
CHEMBL70377 202425 18 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Binding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligandBinding affinity towards D1 CNS receptor of rat corpus striatum using [3H]SCH-23390 as radioligand
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm991005d
13891896 188344 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 297 2 2 4 2.8 COc1c(O)c2c3c(c1OC)CCN[C@@H]3Cc1ccccc1-2 10.1021/jm060959i
CHEMBL508011 188344 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 297 2 2 4 2.8 COc1c(O)c2c3c(c1OC)CCN[C@@H]3Cc1ccccc1-2 10.1021/jm060959i
135508767 202425 18 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
CHEMBL70377 202425 18 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Inhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatumInhibitory binding of [3H]SCH-23390 to Dopamine receptor D1 in membranes from rat corpus striatum
ChEMBL 308 0 2 5 2.8 CN1CCN(C2=Nc3cc(O)ccc3Nc3ccccc32)CC1 10.1021/jm9704457
3082777 167759 10 None - 1 Human 9.8 pKd = 9.8 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2C(c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00119a003
CHEMBL434215 167759 10 None - 1 Human 9.8 pKd = 9.8 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2C(c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00119a003
164612037 184795 0 None -144 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184795 0 None -144 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
168290235 192366 0 None -1513 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192366 0 None -1513 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192366 0 None -1513 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
168294767 192417 0 None -457 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192417 0 None -457 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192417 0 None -457 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
168295528 192429 0 None -338 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192429 0 None -338 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192429 0 None -338 20 Human 9.6 pKd = 9.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
44366049 43209 0 None - 1 Human 9.6 pKd = 9.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
CHEMBL150800 43209 0 None - 1 Human 9.6 pKd = 9.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
2869 4088 85 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60 4088 85 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60857 4088 85 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
CHEMBL1185 4088 85 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
DB00315 4088 85 None -2 7 Rat 9.5 pKd = 9.5 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
3036864 201066 16 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
CHEMBL1256645 201066 16 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
CHEMBL1814790 201066 16 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
CHEMBL62 201066 16 None -2 27 Human 9.4 pKd = 9.4 Binding
Ability to inhibit the binding of [3H]-SCH- 23390 to canine striatal membraneAbility to inhibit the binding of [3H]-SCH- 23390 to canine striatal membrane
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00119a003
129244 118166 7 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL2114388 118166 7 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL34170 118166 7 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity to the rat striatal homogenateIn vitro binding affinity to the rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
118736406 118451 0 None 3 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 673 16 7 7 2.7 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423404 118451 0 None 3 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 673 16 7 7 2.7 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
16731521 85030 0 None - 1 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 630 10 4 5 3.5 CC(C)[C@H](NC(=O)[C@H](CCC1CCCCC1)NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL226639 85030 0 None - 1 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 630 10 4 5 3.5 CC(C)[C@H](NC(=O)[C@H](CCC1CCCCC1)NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
118736409 118454 0 None -1 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 693 16 6 6 3.3 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423407 118454 0 None -1 3 Human 5.9 pKd = 5.9 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 693 16 6 6 3.3 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)c(F)c1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
6852376 91167 11 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
CHEMBL1467585 91167 11 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
CHEMBL24077 91167 11 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
CHEMBL503958 91167 11 None -3 5 Human 6.8 pKd = 6.8 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm950447w
118736412 118458 0 None -6 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423410 118458 0 None -6 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736405 118450 0 None -9 3 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423403 118450 0 None -9 3 Human 4.8 pKd = 4.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736413 118459 0 None -2 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423411 118459 0 None -2 2 Human 5.8 pKd = 5.8 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as high affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
167715 2832 12 None -194 5 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
969 2832 12 None -194 5 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
CHEMBL225230 2832 12 None -194 5 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
1153 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
12668023 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026874 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026875 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
3341 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
6603851 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
933 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
939 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
985 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1160786 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1161520 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL588 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
DB00800 1598 53 None -32 10 Human 5.7 pKd = 5.7 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
118736408 118453 0 None 1 3 Human 5.7 pKd = 5.7 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 696 16 7 6 3.5 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423406 118453 0 None 1 3 Human 5.7 pKd = 5.7 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 696 16 7 6 3.5 CCCC[C@H](NC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
5311428 99645 7 None -32 2 Rat 6.7 pKd = 6.7 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1744078 99645 7 None -32 2 Rat 6.7 pKd = 6.7 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL287504 99645 7 None -32 2 Rat 6.7 pKd = 6.7 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
10088113 161727 5 None -4 2 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1744079 161727 5 None -4 2 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL416401 161727 5 None -4 2 Rat 8.6 pKd = 8.6 Binding
In vitro binding affinity to the rat striatal homogenate.In vitro binding affinity to the rat striatal homogenate.
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
118736412 118458 0 None -6 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423410 118458 0 None -6 2 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
681 1437 65 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
940 1437 65 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
947 1437 65 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
CHEMBL59 1437 65 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
DB00988 1437 65 None -154 38 Human 5.6 pKd = 5.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm950447w
118736402 118447 0 None -5 4 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 659 11 5 6 2.4 CCCC[C@H](NC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423400 118447 0 None -5 4 Human 4.6 pKd = 4.6 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 659 11 5 6 2.4 CCCC[C@H](NC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
1153 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
12668023 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026874 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
30026875 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
3341 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
6603851 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
933 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
939 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
985 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1160786 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL1161520 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
CHEMBL588 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
DB00800 1598 53 None -32 10 Human 7.6 pKd = 7.6 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm950447w
118736404 118449 0 None -2 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 18 7 7 3.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423402 118449 0 None -2 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 18 7 7 3.5 NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCCN1C(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736413 118459 0 None -2 2 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423411 118459 0 None -2 2 Human 4.5 pKd = 4.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes assessed as low affinity constant after 1.5 hrs by scintillation counting analysis
ChEMBL 790 18 6 7 3.3 NCCCC[C@H](NC(=O)[C@H](Cc1ccc(F)c(F)c1)NC(=O)[C@H]1CCCN1C(=O)CCCCCNC(=O)[C@@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(N)=O 10.1016/j.ejmech.2015.04.052
118736411 118456 0 None -1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 788 22 7 7 3.8 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423409 118456 0 None -1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 788 22 7 7 3.8 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
118736407 118452 0 None 1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 17 7 7 3.5 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423405 118452 0 None 1 3 Human 5.5 pKd = 5.5 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 793 17 7 7 3.5 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
118736403 118448 0 None -6 3 Human 4.4 pKd = 4.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 786 22 8 8 3.4 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423401 118448 0 None -6 3 Human 4.4 pKd = 4.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 786 22 8 8 3.4 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2015.04.052
10452020 117772 2 None 10 3 Human 6.4 pKd = 6.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm950447w
CHEMBL34095 117772 2 None 10 3 Human 6.4 pKd = 6.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm950447w
118736410 118455 0 None -1 3 Human 5.4 pKd = 5.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 772 17 6 7 3.1 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
CHEMBL3423408 118455 0 None -1 3 Human 5.4 pKd = 5.4 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysisDisplacement of [3H]-SCH23390 from dopamine D1 receptor (unknown origin) expressed in sheep striatum membranes after 1.5 hrs by scintillation counting analysis
ChEMBL 772 17 6 7 3.1 CCCC[C@H](NC(=O)CCCCCNC(=O)[C@H]1CC[C@@H]2c3[nH]c4ccccc4c3CCN2C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1C[C@@H](N)C[C@H]1C(N)=O 10.1016/j.ejmech.2015.04.052
122132 200877 14 None -87 4 Human 5.3 pKd = 5.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm950447w
CHEMBL611801 200877 14 None -87 4 Human 5.3 pKd = 5.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm950447w
1960 2815 64 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
439260 2815 64 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
505 2815 64 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
CHEMBL1437 2815 64 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
DB00368 2815 64 None -95 26 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
1028 287 69 None -91 29 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
139148732 287 69 None -91 29 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
479 287 69 None -91 29 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
5816 287 69 None -91 29 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
CHEMBL679 287 69 None -91 29 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
DB00668 287 69 None -91 29 Human 4.3 pKd = 4.3 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm950447w
16731518 141750 0 None 26 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 628 9 4 5 2.5 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL388509 141750 0 None 26 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 628 9 4 5 2.5 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
228 441 26 None -35 24 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
33 441 26 None -35 24 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
6005 441 26 None -35 24 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
CHEMBL53 441 26 None -35 24 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
DB00714 441 26 None -35 24 Human 6.2 pKd = 6.2 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm950447w
16732431 143499 0 None -34 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 735 11 4 7 3.3 CN1C[C@H](C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCCC(C(N)=O)C2)C=C2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm060947x
CHEMBL390299 143499 0 None -34 2 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 735 11 4 7 3.3 CN1C[C@H](C(=O)N[C@@H](Cc2ccc([N+](=O)[O-])cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N2CCCC(C(N)=O)C2)C=C2c3cccc4[nH]cc(c34)C[C@H]21 10.1021/jm060947x
16732899 168140 0 None - 1 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL436797 168140 0 None - 1 Human 6.2 pKd = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
16731520 141819 0 None - 1 Human 5.1 pKd = 5.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
CHEMBL388732 141819 0 None - 1 Human 5.1 pKd = 5.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hrDisplacement of [3H]SCH 23390 from dopamine D1 receptor in lamb striatum membrane after 1 hr
ChEMBL 655 10 4 7 2.3 CC(C)[C@H](NC(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm060947x
5 139 66 None -23442 54 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
5202 139 66 None -23442 54 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
CHEMBL39 139 66 None -23442 54 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
DB08839 139 66 None -23442 54 Human 5.0 pKd = 5.0 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950447w
4350931 168747 39 None 63 7 Rat 10.1 pKi = 10.1 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
CHEMBL441618 168747 39 None 63 7 Rat 10.1 pKi = 10.1 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
127026236 137590 0 None 1 3 Rat 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3763331 137590 0 None 1 3 Rat 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3765893 137590 0 None 1 3 Rat 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 450 8 1 4 3.9 O=C(NCCCN1CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
3036864 201066 16 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 201066 16 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 201066 16 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 201066 16 None -26 27 Bovine 10.0 pKi = 10 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
3036864 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
CHEMBL1256645 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
CHEMBL1814790 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
CHEMBL62 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2014.12.045
3036864 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1256645 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL1814790 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
CHEMBL62 201066 16 None -2 27 Human 10.0 pKi = 10 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm401895u
3036864 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1256645 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL1814790 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
CHEMBL62 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2013.01.044
3036864 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
CHEMBL1256645 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
CHEMBL1814790 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
CHEMBL62 201066 16 None -2 27 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm2006782
3036864 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL1256645 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL1814790 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL62 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/s0960-894x(00)00185-2
11465618 101926 18 None 1 19 Human 9.9 pKi = 9.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2020.127563
CHEMBL3039528 101926 18 None 1 19 Human 9.9 pKi = 9.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2020.127563
CHEMBL5191141 101926 18 None 1 19 Human 9.9 pKi = 9.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2020.127563
3036864 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
CHEMBL1256645 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
CHEMBL1814790 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
CHEMBL62 201066 16 None -2 27 Rat 9.9 pKi = 9.9 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00391a028
3036864 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
3036864 201066 16 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 201066 16 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 201066 16 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 201066 16 None -26 27 Bovine 9.8 pKi = 9.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
3036864 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1256645 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1814790 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL62 201066 16 None -2 27 Human 9.8 pKi = 9.8 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
3036864 201066 16 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL1256645 201066 16 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL1814790 201066 16 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
CHEMBL62 201066 16 None -2 27 Human 9.7 pKi = 9.7 Binding
Antagonist activity at dopamine D1 receptor (unknown origin)Antagonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2020.127305
11154178 198542 0 None 64 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
CHEMBL596824 198542 0 None 64 3 Human 9.7 pKi = 9.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 412 4 1 3 4.6 CC(=O)N(Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1)C1CCC1 10.1016/j.bmcl.2009.12.100
162657549 180402 0 None 630 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 355 1 1 3 5.3 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4758723 180402 0 None 630 2 Human 9.7 pKi = 9.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 355 1 1 3 5.3 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
46231926 198895 0 None 12 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599135 198895 0 None 12 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 446 4 1 4 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/OCc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231992 198959 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 389 1 1 2 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599528 198959 0 None 398 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 389 1 1 2 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 201066 16 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
CHEMBL1256645 201066 16 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
CHEMBL1814790 201066 16 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
CHEMBL62 201066 16 None -2 27 Rat 9.7 pKi = 9.7 Binding
The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.The compound was tested for binding affinity against Dopamine receptor D1 from rat striatal membranes, using [3H]-SCH- 23390 as radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00021a018
14896355 26627 0 None 10 3 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(Br)c2)C1 10.1016/s0960-894x(00)00185-2
CHEMBL13632 26627 0 None 10 3 Rat 9.6 pKi = 9.6 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2cccc(Br)c2)C1 10.1016/s0960-894x(00)00185-2
1243 3561 26 None 3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1021/jm00115a012
944 3561 26 None 3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1021/jm00115a012
CHEMBL324017 3561 26 None 3 5 Human 9.5 pKi = 9.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 10.1021/jm00115a012
3038603 101395 6 None 2 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL300647 101395 6 None 2 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
3036864 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1256645 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1814790 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL62 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
3036864 201066 16 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL1256645 201066 16 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL1814790 201066 16 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL62 201066 16 None -2 27 Rat 9.5 pKi = 9.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/S0960-894X(00)80155-9
3036864 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
CHEMBL1256645 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
CHEMBL1814790 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
CHEMBL62 201066 16 None -2 27 Human 9.5 pKi = 9.5 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00081a010
11269330 199808 0 None 34 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605127 199808 0 None 34 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 390 1 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccncc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3039881 173685 6 None 4 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL45491 173685 6 None 4 3 Human 9.5 pKi = 9.5 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
11558055 72805 1 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL1204122 72805 1 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL201170 72805 1 None -1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
3036864 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1256645 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL1814790 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
CHEMBL62 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm8007618
11558055 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL1204122 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL201170 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
11558055 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL1204122 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201170 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2006.11.093
11558055 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL1204122 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
CHEMBL201170 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmc.2009.08.028
3036864 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1256645 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL1814790 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL62 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
11558055 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL1204122 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
CHEMBL201170 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm050846j
14787973 102194 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1cccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)c1 10.1021/jm00170a025
CHEMBL304535 102194 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1cccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)c1 10.1021/jm00170a025
3036864 201066 16 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1256645 201066 16 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL1814790 201066 16 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
CHEMBL62 201066 16 None 2 27 Mouse 9.4 pKi = 9.4 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00170a025
3036864 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1256645 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1814790 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL62 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
11558055 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL1204122 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
CHEMBL201170 72805 1 None -1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1039/C5MD00258C
46231993 198723 0 None 562 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 407 1 1 2 5.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598104 198723 0 None 562 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 407 1 1 2 5.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
CHEMBL1256645 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
CHEMBL1814790 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
CHEMBL62 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00128a038
3036864 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1256645 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1814790 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL62 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
3036864 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL1256645 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL1814790 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL62 201066 16 None -2 27 Human 9.4 pKi = 9.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00129a006
3036864 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
CHEMBL1256645 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
CHEMBL1814790 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
CHEMBL62 201066 16 None -2 27 Rat 9.4 pKi = 9.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00118a012
11595240 139658 0 None -5 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
CHEMBL380464 139658 0 None -5 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 10.1021/jm051237e
162655154 180191 0 None 204 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4756254 180191 0 None 204 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
44320357 204673 0 None 1202 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87734 204673 0 None 1202 2 Rat 9.3 pKi = 9.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
11235174 198697 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NS(C)(=O)=O)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL597909 198697 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NS(C)(=O)=O)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11374299 198924 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 448 5 1 4 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C3CCC3)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599282 198924 0 None 11 3 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 448 5 1 4 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C3CCC3)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
46231588 199576 0 None 12022 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 408 4 1 4 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL603901 199576 0 None 12022 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 408 4 1 4 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(C)(=O)=O)cc2)C1 10.1016/j.bmcl.2009.12.100
3036864 201066 16 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
CHEMBL1256645 201066 16 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
CHEMBL1814790 201066 16 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
CHEMBL62 201066 16 None -2 27 Pig 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm0604979
44439943 92934 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245570 92934 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2006.11.093
11465618 101926 18 None 1 19 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 101926 18 None 1 19 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 101926 18 None 1 19 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
44439943 92934 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL245570 92934 0 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 306 0 2 2 3.5 CN1CCc2ccccc2Cc2[nH]c3ccc(O)cc3c2CC1 10.1016/j.bmcl.2008.04.081
86346162 131918 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 433 3 1 4 4.2 Cc1cc(Oc2ncccc2I)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697581 131918 0 None - 1 Human 9.2 pKi = 9.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 433 3 1 4 4.2 Cc1cc(Oc2ncccc2I)ccc1-c1c(C)n[nH]c(=O)c1C nan
10088113 161727 5 None 4 2 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1744079 161727 5 None 4 2 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL416401 161727 5 None 4 2 Human 9.2 pKi = 9.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 331 1 1 2 3.8 CN1CCc2cc(Br)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
11488247 198955 0 None 1 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL599487 198955 0 None 1 4 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 470 5 1 4 4.5 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(C)S(=O)(=O)c3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
46232135 198640 0 None 85 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 428 1 2 2 6.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc5[nH]ccc5c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597503 198640 0 None 85 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 428 1 2 2 6.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc5[nH]ccc5c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231994 198724 0 None 5 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598105 198724 0 None 5 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 414 1 1 3 5.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(C#N)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231784 199653 0 None 2 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604314 199653 0 None 2 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 329 0 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46231995 199849 0 None 7 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605339 199849 0 None 7 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 434 2 1 4 5.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc([N+](=O)[O-])c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
44268809 97813 0 None 46 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
CHEMBL274577 97813 0 None 46 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
24873463 147511 0 None 3467 2 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 557 10 0 5 6.0 O=C(CCCN1CCN2CC3C(CC2C1)c1ccccc1N3CCCC(=O)c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
CHEMBL393466 147511 0 None 3467 2 Rat 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 557 10 0 5 6.0 O=C(CCCN1CCN2CC3C(CC2C1)c1ccccc1N3CCCC(=O)c1ccc(F)cc1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
46231645 198667 0 None 776 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 518 6 1 3 7.2 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(Cc3ccccc3)c3ccc(F)cc3F)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL597702 198667 0 None 776 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 518 6 1 3 7.2 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CN(Cc3ccccc3)c3ccc(F)cc3F)cc2)C1 10.1016/j.bmcl.2009.12.100
46231709 199023 0 None 1548 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)Nc4c(Cl)cccc4Cl)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL599977 199023 0 None 1548 2 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)Nc4c(Cl)cccc4Cl)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11452916 199145 0 None 7 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL600986 199145 0 None 7 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
44268693 23146 0 None 16 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2ccccc2Br)C1 10.1016/s0960-894x(00)00185-2
CHEMBL13325 23146 0 None 16 3 Rat 9.2 pKi = 9.2 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL 365 1 1 2 4.4 CN1CCc2cc(Cl)c(O)cc2C(c2ccccc2Br)C1 10.1016/s0960-894x(00)00185-2
3036864 201066 16 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1256645 201066 16 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL1814790 201066 16 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
CHEMBL62 201066 16 None -2 27 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrsDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in CHO cells after 2 hrs
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2013.01.025
46232067 198605 0 None 16 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 2 1 3 5.7 CN(C)c1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL597310 198605 0 None 16 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 2 1 3 5.7 CN(C)c1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
46232066 199571 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
CHEMBL603872 199571 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 1 3 5.7 COc1ccc(-c2cccc3c2CC[C@H]2[C@H]3c3cc(O)c(Cl)cc3CCN2C)cc1 10.1016/j.bmcl.2009.12.094
46232134 199631 0 None 125 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 2 3 5.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc(CO)cc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604176 199631 0 None 125 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 419 2 2 3 5.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4ccc(CO)cc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
CHEMBL1256645 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
CHEMBL1814790 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
CHEMBL62 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm960318v
3036864 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
CHEMBL1256645 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
CHEMBL1814790 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
CHEMBL62 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm991034o
10516818 25447 0 None 2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135197 25447 0 None 2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
14787971 169505 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccccc1[C@H]1CN(C)CCc2cc(Cl)c(O)cc21 10.1021/jm00170a025
CHEMBL444321 169505 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccccc1[C@H]1CN(C)CCc2cc(Cl)c(O)cc21 10.1021/jm00170a025
3036864 201066 16 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
CHEMBL1256645 201066 16 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
CHEMBL1814790 201066 16 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
CHEMBL62 201066 16 None -2 27 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2008.05.077
242 467 117 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
34 467 117 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
60795 467 117 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
CHEMBL1112 467 117 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
DB01238 467 117 None -74 51 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm100294b
11681599 74823 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL203637 74823 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1016/j.bmcl.2008.04.081
44439942 151333 0 None 4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2[nH]c3c(c2c1)CCN(C)CCc1ccccc1C3 10.1016/j.bmcl.2006.11.093
CHEMBL396560 151333 0 None 4 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2[nH]c3c(c2c1)CCN(C)CCc1ccccc1C3 10.1016/j.bmcl.2006.11.093
11681599 74823 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL203637 74823 0 None -12 6 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 10.1021/jm051237e
10802788 167675 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL433652 167675 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
10802788 167675 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL433652 167675 0 None -2 2 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 281 4 1 2 3.8 CCCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
3036864 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1256645 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1814790 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL62 201066 16 None -2 27 Rat 9.1 pKi = 9.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
46231541 198504 0 None 4 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 370 4 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNC3CCC3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL596622 198504 0 None 4 3 Human 9.1 pKi = 9.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 370 4 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNC3CCC3)cc2)C1 10.1016/j.bmcl.2009.12.100
107930 1500 20 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
3304 1500 20 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
CHEMBL298406 1500 20 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
DB12273 1500 20 None 1 6 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2020.127563
149506840 182566 0 None 120 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 371 1 1 3 5.8 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4795230 182566 0 None 120 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 371 1 1 3 5.8 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
46232065 198575 0 None 346 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 425 1 1 2 5.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cc(F)cc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597100 198575 0 None 346 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 425 1 1 2 5.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cc(F)cc(F)c4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
46216855 198694 0 None 2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL597900 198694 0 None 2 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 395 1 1 3 5.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccs4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
15111050 13237 0 None 707 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 357 3 1 2 4.3 C=CCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1192259 13237 0 None 707 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 357 3 1 2 4.3 C=CCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL543473 13237 0 None 707 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 357 3 1 2 4.3 C=CCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
130844 13091 13 None 512 2 Human 9.1 pKi = 9.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL1191103 13091 13 None 512 2 Human 9.1 pKi = 9.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL543398 13091 13 None 512 2 Human 9.1 pKi = 9.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 303 1 2 3 3.4 CN1CCc2c(cc(O)c(O)c2Cl)C(c2ccccc2)C1 10.1021/jm00116a004
71451380 80825 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 435 3 5 6 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1.O=C(O)/C(O)=C(/O)C(=O)O 10.1016/j.bmc.2012.08.058
CHEMBL2158641 80825 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 435 3 5 6 3.1 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1.O=C(O)/C(O)=C(/O)C(=O)O 10.1016/j.bmc.2012.08.058
6852376 91167 11 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL1467585 91167 11 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL24077 91167 11 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL503958 91167 11 None -3 5 Human 9.0 pKi = 9 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
167715 2832 12 None -194 5 Human 9.0 pKi = 9 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
969 2832 12 None -194 5 Human 9.0 pKi = 9 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL225230 2832 12 None -194 5 Human 9.0 pKi = 9 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
11393666 192384 0 None -2 19 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192384 0 None -2 19 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192384 0 None -2 19 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysisDisplacement of [3H]SCH 23390 from recombinant human D1 receptor measured after 60 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
46231927 199851 0 None 2 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL605354 199851 0 None 2 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 432 3 1 4 5.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/Oc4ccccc4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
13805900 43759 0 None -2 6 Bovine 9.0 pKi = 9.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@@H]1Cc2cccc(O)c2C[C@H]1C 10.1021/jm020990u
CHEMBL15136 43759 0 None -2 6 Bovine 9.0 pKi = 9.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 261 5 1 2 3.6 CCCN(CCC)[C@@H]1Cc2cccc(O)c2C[C@H]1C 10.1021/jm020990u
162646534 179003 0 None 123 2 Human 9.0 pKi = 9.0 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 362 1 1 4 5.0 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(C#N)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4742056 179003 0 None 123 2 Human 9.0 pKi = 9.0 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 362 1 1 4 5.0 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(C#N)cc32)CCN1C 10.1016/j.bmcl.2020.127563
1242 3556 23 None -5 17 Human 9.0 pKi = 9.0 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
935 3556 23 None -5 17 Human 9.0 pKi = 9.0 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
CHEMBL286080 3556 23 None -5 17 Human 9.0 pKi = 9.0 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
133538 3562 17 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2008.09.049
8443 3562 17 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2008.09.049
CHEMBL574558 3562 17 None -1 5 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2008.09.049
107930 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
3304 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
CHEMBL298406 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
DB12273 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.100
5018 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
943 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
946 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
CHEMBL13668 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 10.1016/j.bmc.2012.12.016
107930 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
3304 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
CHEMBL298406 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
DB12273 1500 20 None 1 6 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1016/j.bmcl.2009.12.094
15111051 13259 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 313 3 1 2 4.2 C=CCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1192465 13259 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 313 3 1 2 4.2 C=CCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL543704 13259 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 313 3 1 2 4.2 C=CCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
13697621 13629 0 None 1148 2 Human 8.9 pKi = 8.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 347 1 2 3 3.5 CN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL1195188 13629 0 None 1148 2 Human 8.9 pKi = 8.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 347 1 2 3 3.5 CN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL554009 13629 0 None 1148 2 Human 8.9 pKi = 8.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 347 1 2 3 3.5 CN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
1153 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
12668023 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
30026874 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
30026875 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
3341 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
6603851 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
933 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
939 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
985 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL1160786 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL1161520 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL588 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
DB00800 1598 53 None -1 10 Rat 8.9 pKi = 8.9 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
3036864 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1256645 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL1814790 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
CHEMBL62 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmc.2012.05.057
5018 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
943 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
946 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
CHEMBL13668 3493 8 None 2 9 Human 8.9 pKi = 8.9 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O nan
134139606 145815 0 None 288 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 419 3 2 5 3.9 CCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3921278 145815 0 None 288 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 419 3 2 5 3.9 CCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
3036864 201066 16 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1256645 201066 16 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL1814790 201066 16 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
CHEMBL62 201066 16 None -5 27 Goldfish 8.9 pKi = 8.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00114a002
10638646 26010 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135735 26010 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
11486421 199509 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 400 2 2 4 4.5 CCOC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL603485 199509 0 None 2 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 400 2 2 4 4.5 CCOC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
3036864 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL1256645 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL1814790 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL62 201066 16 None -2 27 Human 8.9 pKi = 8.9 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2009.12.100
142405815 180582 0 None -10 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 365 2 1 3 5.7 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4760903 180582 0 None -10 3 Human 8.9 pKi = 8.9 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 365 2 1 3 5.7 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
11223303 199146 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL600987 199146 0 None 4 3 Human 8.8 pKi = 8.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1ccc2c(c1)CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
14787975 101762 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1 10.1021/jm00170a025
CHEMBL303012 101762 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 301 1 1 2 4.0 Cc1ccc([C@H]2CN(C)CCc3cc(Cl)c(O)cc32)cc1 10.1021/jm00170a025
162646218 178896 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4740880 178896 0 None 77 2 Human 8.8 pKi = 8.8 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CCN1C 10.1016/j.bmcl.2020.127563
122324 203 17 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
6077 203 17 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
CHEMBL86931 203 17 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00112a034
122324 203 17 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None 323 3 Rat 8.8 pKi = 8.8 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
44415569 165381 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL425069 165381 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
44415569 165381 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL425069 165381 0 None 8 6 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
46231849 199733 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604732 199733 0 None 2 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 356 1 2 4 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(/C=N/O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3036864 201066 16 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
CHEMBL1256645 201066 16 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
CHEMBL1814790 201066 16 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
CHEMBL62 201066 16 None -2 27 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometryDisplacement of [3H]-SCH-23390 from dopamine D1 receptor (unknown origin) expressed in HEK293 cell membranes incubated for 15 mins by liquid scintillation spectrometry
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2015.07.030
129244 118166 7 None - 1 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL2114388 118166 7 None - 1 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
CHEMBL34170 118166 7 None - 1 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 413 1 1 2 4.3 CN1CCc2cc(Cl)c(O)cc2C(c2ccc(I)cc2)C1 10.1021/jm00127a005
10638646 26010 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135735 26010 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
37461 16953 10 None -2 8 Rat 8.7 pKi = 8.7 Binding
Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/jm9911478
CHEMBL1255588 16953 10 None -2 8 Rat 8.7 pKi = 8.7 Binding
Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 rat striatal receptor using [3H]SCH-23390
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/jm9911478
46231925 199693 0 None 5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL604525 199693 0 None 5 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 384 3 1 4 4.4 CCO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
73671785 128899 0 None - 1 Human 8.7 pKi = 8.7 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 3 2 6 2.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3671278 128899 0 None - 1 Human 8.7 pKi = 8.7 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 3 2 6 2.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
4350931 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL441618 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
10656804 116059 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL336366 116059 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
107930 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
3304 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
CHEMBL298406 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
DB12273 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00170a025
107930 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
3304 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
CHEMBL298406 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
DB12273 1500 20 None 1 6 Human 8.7 pKi = 8.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
4350931 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
CHEMBL441618 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm051237e
4350931 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL441618 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
4350931 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL441618 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
4350931 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL441618 168747 39 None -63 7 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1039/C5MD00258C
12765746 101810 3 None -18 10 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL303313 101810 3 None -18 10 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
12765746 101810 3 None -18 10 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL303313 101810 3 None -18 10 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
9797664 165684 1 None -4 3 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 331 1 0 4 3.8 CN1CCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL426763 165684 1 None -4 3 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 331 1 0 4 3.8 CN1CCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
107930 1500 20 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
3304 1500 20 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
CHEMBL298406 1500 20 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
DB12273 1500 20 None -1 6 Rat 8.7 pKi = 8.7 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 10.1021/jm00128a038
133538 3562 17 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
8443 3562 17 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
CHEMBL574558 3562 17 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O 10.1016/j.bmc.2009.06.019
12765746 101810 3 None -18 10 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL303313 101810 3 None -18 10 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
4106 2466 16 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
5358812 2466 16 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
89 2466 16 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
CHEMBL93240 2466 16 None -5 33 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10.1021/jm010982y
44348383 16127 0 None -10 2 Rat 8.7 pKi = 8.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 205 3 1 2 2.7 CSc1ccc2c(c1)C(CCN)=CC2 10.1021/jm9706832
CHEMBL122536 16127 0 None -10 2 Rat 8.7 pKi = 8.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 205 3 1 2 2.7 CSc1ccc2c(c1)C(CCN)=CC2 10.1021/jm9706832
135398745 2869 108 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
47 2869 108 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
CHEMBL715 2869 108 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
DB00334 2869 108 None -26 65 Human 8.0 pKi = 8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0002432
15937726 164597 0 None 177 2 Rat 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 293 1 1 2 4.2 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL422796 164597 0 None 177 2 Rat 8.0 pKi = 8 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 293 1 1 2 4.2 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
44579030 189089 0 None 10 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 377 7 0 3 5.7 CCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL515342 189089 0 None 10 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 377 7 0 3 5.7 CCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415558 79752 0 None 93 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4n3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213443 79752 0 None 93 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4n3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415657 168176 0 None 17 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 4 1 7 4.9 CCOc1csc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
CHEMBL437112 168176 0 None 17 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 4 1 7 4.9 CCOc1csc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
117773683 131920 0 None - 1 Human 8.0 pKi = 8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 403 5 1 6 3.5 Cc1cc(Oc2nccc(C)c2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697583 131920 0 None - 1 Human 8.0 pKi = 8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 403 5 1 6 3.5 Cc1cc(Oc2nccc(C)c2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
56594534 70256 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
CHEMBL1949728 70256 0 None 1 5 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@@H]1CO 10.1021/jm200676f
90140327 128890 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]c(C)c23)cc1 nan
CHEMBL3671269 128890 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]c(C)c23)cc1 nan
74223724 128895 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671274 128895 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
74223826 128915 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671293 128915 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
11637457 72740 1 None 1 5 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
CHEMBL201093 72740 1 None 1 5 Human 8.0 pKi = 8.0 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1021/jm050846j
86764102 131957 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1ccnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)cc2)c1Cl nan
CHEMBL3697619 131957 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1ccnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)cc2)c1Cl nan
135398745 2869 108 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2869 108 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2869 108 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2869 108 None -26 65 Human 7.0 pKi = 7 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
11271099 202951 0 None -501 4 Rat 7.0 pKi = 7 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 458 9 2 5 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(N)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL73665 202951 0 None -501 4 Rat 7.0 pKi = 7 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 458 9 2 5 4.3 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(N)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
15937722 114725 0 None - 1 Rat 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 294 1 1 3 3.1 CN1CCc2cc(Cl)c(O)cc2C(N2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL334650 114725 0 None - 1 Rat 7.0 pKi = 7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 294 1 1 3 3.1 CN1CCc2cc(Cl)c(O)cc2C(N2CCCCC2)C1 10.1016/S0960-894X(00)80155-9
49782398 17270 0 None -138 5 Pig 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1257688 17270 0 None -138 5 Pig 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 471 6 1 3 5.7 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
6603820 95330 13 None 1 13 Rat 7.0 pKi = 7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL25856 95330 13 None 1 13 Rat 7.0 pKi = 7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm970038v
15711850 13128 0 None -1 5 Goldfish 7.0 pKi = 7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1191350 13128 0 None -1 5 Goldfish 7.0 pKi = 7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL542436 13128 0 None -1 5 Goldfish 7.0 pKi = 7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
242 467 117 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 467 117 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 467 117 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 467 117 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 467 117 None -281 51 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
135398737 944 89 None -44 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 944 89 None -44 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 944 89 None -44 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 944 89 None -44 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 944 89 None -44 91 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
2337 3205 72 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
50 3205 72 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
5002 3205 72 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
CHEMBL716 3205 72 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
DB01224 3205 72 None -53 62 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1039/C2MD00311B
2389 3279 114 None -467 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3279 114 None -467 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3279 114 None -467 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3279 114 None -467 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3279 114 None -467 67 Human 6.0 pKi = 6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
17449900 139012 12 None -3548 6 Pig 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139012 12 None -3548 6 Pig 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
137633863 156084 0 None -436 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156084 0 None -436 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
44372154 53940 0 None -11 4 Bovine 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160749 53940 0 None -11 4 Bovine 6.0 pKi = 6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 434 4 0 4 5.4 Cc1nn2c(-c3ccc(F)cc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
9864676 127286 0 None -58 5 Bovine 6.0 pKi = 6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL366388 127286 0 None -58 5 Bovine 6.0 pKi = 6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 380 6 0 3 4.5 O=C(CCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
15115530 12809 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 659 3 7 9 6.4 O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N/C(S)=N\c3ccc(C4CNCCc5cc(O)c(O)cc54)cc3)cc21 10.1021/jm00115a012
CHEMBL1189085 12809 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 659 3 7 9 6.4 O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N/C(S)=N\c3ccc(C4CNCCc5cc(O)c(O)cc54)cc3)cc21 10.1021/jm00115a012
CHEMBL538023 12809 0 None - 1 Human 5.0 pKi = 5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 659 3 7 9 6.4 O=C1OC2(c3ccc(O)cc3Oc3cc(O)ccc32)c2ccc(N/C(S)=N\c3ccc(C4CNCCc5cc(O)c(O)cc54)cc3)cc21 10.1021/jm00115a012
44339879 171716 0 None -186 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 171716 0 None -186 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
10357869 4815 0 None -158 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL104453 4815 0 None -158 4 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3cccc3-c3cnco3)CC2)cc1 10.1016/s0960-894x(99)00540-5
44412458 138764 3 None -3090 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL379177 138764 3 None -3090 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 316 4 0 4 3.6 C1=C(c2ccccc2)CCN(Cc2cn(-c3ccccc3)nn2)C1 10.1016/j.bmcl.2006.02.075
45112568 197128 0 None -229 3 Rat 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
CHEMBL583422 197128 0 None -229 3 Rat 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
145980271 165939 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4278465 165939 0 None -19 16 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 538 8 1 3 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
145986752 166723 0 None -23 17 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
CHEMBL4293307 166723 0 None -23 17 Human 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 562 10 1 5 7.3 COc1ccc(N(CCCCN2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)c2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.10.036
10633305 35765 0 None -28 2 Bovine 4.0 pKi = 4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2ccc(C)cc2C)C1 10.1021/jm9708700
CHEMBL144302 35765 0 None -28 2 Bovine 4.0 pKi = 4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2ccc(C)cc2C)C1 10.1021/jm9708700
44329093 205978 0 None -309 3 Bovine 4.0 pKi = 4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@@H]1CCn2ccc(CO)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL95618 205978 0 None -309 3 Bovine 4.0 pKi = 4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@@H]1CCn2ccc(CO)c2C1 10.1016/s0960-894x(01)00564-9
44304814 201183 0 None -16 4 Bovine 4.0 pKi = 4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
CHEMBL62601 201183 0 None -16 4 Bovine 4.0 pKi = 4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 505 8 1 5 5.9 COc1c(-c2nc(CNC[C@@H]3CCN(Cc4ccccc4)C3)co2)cc(Br)c2ccccc12 10.1016/s0960-894x(00)00405-4
71109993 142715 0 None - 1 Human 6.0 pKi = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
CHEMBL3896617 142715 0 None - 1 Human 6.0 pKi = 6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1ccc2c(c1)CCN1Cc3c(cc(OC)c(OC)c3OC)CC21 nan
228 441 26 None -4 24 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
33 441 26 None -4 24 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
6005 441 26 None -4 24 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
CHEMBL53 441 26 None -4 24 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
DB00714 441 26 None -4 24 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.02.038
228 441 26 None -30 24 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
33 441 26 None -30 24 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
6005 441 26 None -30 24 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
CHEMBL53 441 26 None -30 24 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
DB00714 441 26 None -30 24 Rat 6.0 pKi = 6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
74223776 128910 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1C#N nan
CHEMBL3671289 128910 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1C#N nan
28417 39799 48 None -1 12 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
CHEMBL1479 39799 48 None -1 12 Human 5.0 pKi = 5.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C nan
15711865 13064 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL1190906 13064 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL541838 13064 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
3246545 200787 1 None -7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 200787 1 None -7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 200787 1 None -7 5 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
44415394 141301 0 None 15 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 471 3 1 5 4.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)/C=C/c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL386424 141301 0 None 15 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 471 3 1 5 4.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)/C=C/c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
13864380 204706 1 None 4 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87958 204706 1 None 4 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O 10.1021/jm00112a034
13864381 206603 3 None 4 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL542683 206603 3 None 4 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL99361 206603 3 None 4 4 Rat 6.0 pKi = 6.0 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O 10.1021/jm00173a005
10637496 112385 0 None -58 3 Rat 6.0 pKi = 6.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 2 0 2 4.0 CCc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL331005 112385 0 None -58 3 Rat 6.0 pKi = 6.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 2 0 2 4.0 CCc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
44405995 72650 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
CHEMBL200802 72650 0 None -1 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
56593482 3878 1 None -954 9 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7650 3878 1 None -954 9 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165119 3878 1 None -954 9 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 462 7 1 5 4.6 O=C1CCc2c(N1)nc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
156018236 177338 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 377 4 1 3 4.9 C=CCN1CCc2cc(OC)c(O)cc2C(c2c(Cl)cccc2Cl)C1 10.1016/j.bmcl.2020.127305
CHEMBL4645139 177338 0 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 377 4 1 3 4.9 C=CCN1CCc2cc(OC)c(O)cc2C(c2c(Cl)cccc2Cl)C1 10.1016/j.bmcl.2020.127305
154706030 175971 1 None -50 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4580817 175971 1 None -50 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597188 175971 1 None -50 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
76325156 105909 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 105909 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 105909 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
12050197 100407 0 None -79 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL293645 100407 0 None -79 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 457 6 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
10570422 164353 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 6 2 3 4.0 CNCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL422267 164353 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 6 2 3 4.0 CNCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
15627832 98082 0 None -6 3 Rat 7.0 pKi = 7.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 345 0 2 3 3.6 CN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL276326 98082 0 None -6 3 Rat 7.0 pKi = 7.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 345 0 2 3 3.6 CN1CCc2cc(Br)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
13646434 124134 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL1743799 124134 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL36416 124134 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
70692652 75711 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057441 75711 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
72708059 91764 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425369 91764 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
161665 172016 33 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL448891 172016 33 None 1 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
1353 1880 85 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
3559 1880 85 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
86 1880 85 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
CHEMBL54 1880 85 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
DB00502 1880 85 None -38 85 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm1013693
72708059 91764 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425369 91764 0 None 1 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 301 0 2 3 3.4 Oc1ccc2c(c1)CC1c3cc(O)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
45112462 195291 0 None -831 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
CHEMBL566533 195291 0 None -831 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 in rat striatum by liquid scintillation counting
ChEMBL 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 10.1016/j.ejmech.2009.11.023
154706123 175714 1 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4593394 175714 1 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595145 175714 1 None -134 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
11724078 41465 1 None -2 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cccnc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL149240 41465 1 None -2 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cccnc3Oc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
154706513 176012 1 None -16 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4440698 176012 1 None -16 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4597532 176012 1 None -16 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 480 12 0 6 5.6 COc1ccc(F)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
3117 206106 100 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 206106 100 None -2 16 Human 6.0 pKi = 6.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44448066 94434 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL253948 94434 0 None -1 2 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 10.1021/jm060959i
154704141 176105 1 None -46 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4561808 176105 1 None -46 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598299 176105 1 None -46 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 3 5.0 CCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
117774721 131923 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 5 1 6 2.8 Cc1c(-c2ccc(Oc3ncccc3OC(F)F)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697586 131923 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 5 1 6 2.8 Cc1c(-c2ccc(Oc3ncccc3OC(F)F)cc2)n(C)c(=O)[nH]c1=O nan
112500032 131948 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697610 131948 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)cnc(=O)n1C nan
10333842 97979 1 None -50 8 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
CHEMBL27559 97979 1 None -50 8 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
76325156 105909 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3115585 105909 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
CHEMBL3139393 105909 1 None -15135 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 263 7 2 3 3.3 CCCCCCNC[C@H]1CCc2ccc(O)cc2O1 10.1021/jm401384w
9951964 204635 0 None -22 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87458 204635 0 None -22 4 Rat 6.0 pKi = 6.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 383 5 0 3 4.3 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3cc(F)ccc3C2=O)CC1 10.1021/jm00042a009
44415644 141289 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 583 4 1 5 7.3 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4N(NC(=O)c4ccccc4Cl)c4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
CHEMBL386336 141289 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 583 4 1 5 7.3 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4N(NC(=O)c4ccccc4Cl)c4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
10490043 113222 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960189i
CHEMBL332332 113222 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960189i
44386623 60730 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 376 3 0 4 4.2 COc1c(Cl)c2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
CHEMBL176356 60730 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 376 3 0 4 4.2 COc1c(Cl)c2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
1212 1632 45 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1632 45 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1632 45 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1632 45 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1632 45 None -51 65 Human 8.0 pKi = 8.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44415633 79597 0 None 8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 7 5.1 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL212807 79597 0 None 8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 7 5.1 COc1cccc(OC)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
44415578 140971 0 None 57 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL384500 140971 0 None 57 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
134151737 152441 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 5 2 5 3.9 CCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3975220 152441 0 None 12 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 5 2 5 3.9 CCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
127031424 138340 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 6 1 5 4.2 CCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3781840 138340 0 None 5 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 6 1 5 4.2 CCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
75201901 165872 14 None -1 24 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165872 14 None -1 24 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
44370173 48221 0 None -18 2 Bovine 7.0 pKi = 7.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 331 6 2 4 4.0 CCCN(CCc1cccs1)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
CHEMBL155613 48221 0 None -18 2 Bovine 7.0 pKi = 7.0 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 331 6 2 4 4.0 CCCN(CCc1cccs1)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
75201901 165872 14 None -1 24 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 165872 14 None -1 24 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
122189393 122732 0 None -20 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613879 122732 0 None -20 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 455 6 0 7 4.0 Clc1cccc(N2CCN(CCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
122189394 122733 0 None -354 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613880 122733 0 None -354 5 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 7 0 7 4.4 Clc1cccc(N2CCN(CCCCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
21302486 109312 0 None -117 4 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 379 5 1 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCN3)c1ccc(F)cc1 10.1021/jm401958n
CHEMBL3233143 109312 0 None -117 4 Human 7.0 pKi = 7.0 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 379 5 1 4 3.9 O=C(CCCN1CC[C@H]2[C@@H](C1)c1cccc3c1N2CCN3)c1ccc(F)cc1 10.1021/jm401958n
10092819 16594 0 None -1412 12 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 16594 0 None -1412 12 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
11133602 30559 0 None -63 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL139600 30559 0 None -63 5 Human 6.0 pKi = 6.0 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44276404 98621 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL28054 98621 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
44276557 98858 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL282136 98858 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
11761412 116451 0 None -2290 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
CHEMBL338606 116451 0 None -2290 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 411 9 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)/C=C/c2ccc(F)cc2)CC1 10.1016/j.bmcl.2010.09.142
10490043 113222 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm060959i
CHEMBL332332 113222 0 None -190 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 237 0 2 2 2.8 Oc1cccc2c1-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm060959i
71459761 83666 0 None -181 7 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207642 83666 0 None -181 7 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 540 7 0 5 6.1 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
137635685 155464 0 None -38 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
CHEMBL4061986 155464 0 None -38 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 417 7 1 7 3.6 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2cccnc12 10.1021/acs.jmedchem.7b00363
25072633 158675 0 None -1584 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 158675 0 None -1584 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
118709166 112913 0 None -19 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318838 112913 0 None -19 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 25 0 8 12.9 O=C(CCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
164615845 184607 0 None -1 6 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
CHEMBL4857492 184607 0 None -1 6 Human 6.0 pKi = 6.0 Binding
Inhibition of dopamine D1 receptor (unknown origin)Inhibition of dopamine D1 receptor (unknown origin)
ChEMBL 389 2 1 4 3.7 O=C(O)c1ccc(C#Cc2ccc3c(c2)C=C([N+](=O)[O-])C(C(F)(F)F)O3)cc1 10.1016/j.bmcl.2021.128008
10833953 30909 0 None -1445 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140006 30909 0 None -1445 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cc2c1 10.1021/jm0009989
44380697 57787 0 None -61 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167414 57787 0 None -61 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44380685 58427 0 None -77 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168566 58427 0 None -77 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 373 6 2 4 3.2 COc1cc(N)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44380815 58701 0 None -234 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169193 58701 0 None -234 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
44264682 96869 0 None -2754 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
CHEMBL269202 96869 0 None -2754 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)c1 10.1016/s0960-894x(98)00692-1
15508243 5231 20 None -7 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL106635 5231 20 None -7 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 366 3 0 2 3.9 Ic1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
25099153 186670 0 None -257039 3 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 436 9 2 5 4.7 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL492664 186670 0 None -257039 3 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 436 9 2 5 4.7 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
45270021 193494 0 None -158 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL550392 193494 0 None -158 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 335 3 0 5 3.0 Cc1cc2nc(C)c(CN3CCN(c4ccccc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
45272580 194782 0 None -165 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563109 194782 0 None -165 4 Bovine 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cnc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
102262219 139529 0 None -22908 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800400 139529 0 None -22908 6 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137655029 158400 0 None -2691 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4095881 158400 0 None -2691 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 452 8 1 9 2.6 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc12 10.1016/j.bmc.2017.08.037
137657427 159012 0 None -9772 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4102628 159012 0 None -9772 5 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 476 7 3 6 3.5 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
10361512 54154 0 None -4786 5 Bovine 5.0 pKi = 5.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160932 54154 0 None -4786 5 Bovine 5.0 pKi = 5.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 365 3 0 5 3.5 Cc1nn2c(C#N)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
154706590 175735 1 None -58 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4590839 175735 1 None -58 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4595264 175735 1 None -58 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
71110301 91766 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425371 91766 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
44415368 79193 0 None 17 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 465 4 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCC3CCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL211461 79193 0 None 17 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 465 4 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCC3CCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
14198586 200148 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL60706 200148 0 None 2 2 Rat 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1016/j.bmc.2009.05.079
156013666 176705 0 None -10 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 3 1 4 3.6 COc1cc2c3c(c1OC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4636318 176705 0 None -10 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 3 1 4 3.6 COc1cc2c3c(c1OC1CC1)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
2726 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
154704536 175873 1 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4467528 175873 1 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4596340 175873 1 None -2 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCOc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
154703875 175874 1 None -87 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 175874 1 None -87 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 175874 1 None -87 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
11335419 66764 1 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL187367 66764 1 None -11 6 Human 7.0 pKi = 7.0 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 7 0 2 4.1 c1ccc(Cc2ccccc2OCCCN2CCCC2)cc1 10.1021/jm049720x
74223726 128897 13 None - 1 Human 7.0 pKi = 7.0 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C 10.1021/acs.jmedchem.8b01767
CHEMBL3671276 128897 13 None - 1 Human 7.0 pKi = 7.0 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C 10.1021/acs.jmedchem.8b01767
74223726 128897 13 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
CHEMBL3671276 128897 13 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 331 3 1 5 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
10497993 167909 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL43514 167909 0 None 2 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2 10.1021/jm970038v
3038495 700 30 None -616 19 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
7625 700 30 None -616 19 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
CHEMBL25236 700 30 None -616 19 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/acs.jmedchem.9b01835
136074293 201368 0 None -3 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1cnc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm00067a009
CHEMBL63590 201368 0 None -3 2 Rat 6.0 pKi = 6.0 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1cnc2c(c1)N=C(N1CCN(C)CC1)c1ccccc1N2 10.1021/jm00067a009
45481842 196384 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 3 1 2 3.8 CCCCC1c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
CHEMBL574112 196384 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 3 1 2 3.8 CCCCC1c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
56589561 70257 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
CHEMBL1949729 70257 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 320 1 2 2 3.2 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2C[C@H]1CO 10.1021/jm200676f
135398737 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
38 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
722 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
CHEMBL42 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
DB00363 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00030a011
242 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
242 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
34 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
60795 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL1112 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB01238 467 117 None -281 51 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
76325154 105925 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3115580 105925 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3139475 105925 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
154703647 175791 1 None -20 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4450429 175791 1 None -20 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595728 175791 1 None -20 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCOc1ccc(F)cc1C1CC1CN(CC)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
135398737 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
38 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
722 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
CHEMBL42 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
DB00363 944 89 None -83 91 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00067a009
156016177 177080 0 None -114 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
CHEMBL4641502 177080 0 None -114 7 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 307 0 1 4 3.6 CN1CCc2cccc3c2C1Cc1ccc2nc(N)sc2c1-3 10.1016/j.bmc.2020.115578
12049520 100596 6 None -45 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL294780 100596 6 None -45 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 319 4 0 4 3.7 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)co2)cc1 10.1016/s0960-894x(00)00405-4
44593524 183474 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmc.2008.05.077
CHEMBL482276 183474 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmc.2008.05.077
76325154 105925 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3115580 105925 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
CHEMBL3139475 105925 0 None -35 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1OCCCCF)CC2 10.1021/jm401384w
44448062 94407 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253737 94407 0 None 1 2 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
117774133 131896 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 5 4.1 Cc1cc(Oc2ncc(Cl)cc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697559 131896 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 5 4.1 Cc1cc(Oc2ncc(Cl)cc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
90644065 111170 0 None -8 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3286429 111170 0 None -8 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 5 0 4 4.2 Clc1ccc(N2CCN(CCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
53318565 58293 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684134 58293 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
10000788 47729 0 None -41 3 Rat 5.9 pKi = 5.9 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 395 6 1 4 3.9 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCN(c3ccccc3OC)CC1)CC2 10.1016/0960-894X(95)00076-6
CHEMBL155006 47729 0 None -41 3 Rat 5.9 pKi = 5.9 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 395 6 1 4 3.9 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCN(c3ccccc3OC)CC1)CC2 10.1016/0960-894X(95)00076-6
10832461 50990 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)c2c(c1)CCN(C)C2Cc1ccccc1O 10.1021/jm991034o
CHEMBL158067 50990 0 None -1 2 Rat 4.9 pKi = 4.9 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)c2c(c1)CCN(C)C2Cc1ccccc1O 10.1021/jm991034o
86763998 131952 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697614 131952 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
135398745 2869 108 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
47 2869 108 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
CHEMBL715 2869 108 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
DB00334 2869 108 None -23 65 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049632c
91899760 128925 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 1 5 4.3 Cc1cc(Oc2nccc3n[nH]cc23)c(F)cc1-c1c(C)ncnc1C nan
CHEMBL3671302 128925 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 1 5 4.3 Cc1cc(Oc2nccc3n[nH]cc23)c(F)cc1-c1c(C)ncnc1C nan
12304090 87080 30 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@H]21 10.1016/j.bmc.2012.12.016
CHEMBL2334886 87080 30 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@H]21 10.1016/j.bmc.2012.12.016
135398745 2869 108 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
47 2869 108 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
CHEMBL715 2869 108 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
DB00334 2869 108 None -26 65 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/S0960-894X(96)00567-7
168289523 190903 0 None -5 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
CHEMBL5193761 190903 0 None -5 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysisDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cell membrane by competitive inhibition based analysis
ChEMBL 422 5 1 2 6.0 FC(F)(F)c1cccc(COC2CCN(Cc3cc4ccc(Cl)cc4[nH]3)CC2)c1 10.1016/j.bmcl.2022.128615
10276451 198601 33 None -12022 10 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL2112910 198601 33 None -12022 10 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL59725 198601 33 None -12022 10 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
10531 1392 18 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1392 18 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1392 18 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1392 18 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1392 18 None -218 24 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
2435 3533 78 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 3533 78 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 3533 78 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 3533 78 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 3533 78 None -43 48 Rat 7.9 pKi = 7.9 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
25141414 181899 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 5 0 3 4.9 CCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL478671 181899 0 None -1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 5 0 3 4.9 CCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415721 79632 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 605 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212936 79632 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 605 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415703 79411 0 None 537 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)c(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212077 79411 0 None 537 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)c(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415688 79761 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213477 79761 0 None 30 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
134143833 149982 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 355 4 2 5 3.6 CCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3954556 149982 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 355 4 2 5 3.6 CCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
127031403 138205 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 381 5 1 5 3.9 COc1cc2c(cc1O)C1Cc3ccc(OCC4CC4)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780184 138205 0 None 4 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 381 5 1 5 3.9 COc1cc2c(cc1O)C1Cc3ccc(OCC4CC4)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
10733562 146481 0 None 25 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL39266 146481 0 None 25 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2 10.1021/jm970038v
9819042 13046 1 None 23 2 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 333 1 3 3 3.1 Oc1cc2c(c(Br)c1O)CCNCC2c1ccccc1 10.1021/jm00116a004
CHEMBL1190761 13046 1 None 23 2 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 333 1 3 3 3.1 Oc1cc2c(c(Br)c1O)CCNCC2c1ccccc1 10.1021/jm00116a004
CHEMBL541559 13046 1 None 23 2 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 333 1 3 3 3.1 Oc1cc2c(c(Br)c1O)CCNCC2c1ccccc1 10.1021/jm00116a004
1241 99716 19 None -2 7 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL288090 99716 19 None -2 7 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL552611 99716 19 None -2 7 Human 7.9 pKi = 7.9 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00116a004
117773867 131932 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 1 4 4.9 Cc1cc(Oc2nccc(C)c2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697594 131932 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 1 4 4.9 Cc1cc(Oc2nccc(C)c2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
6917970 3635 54 None -1 34 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
8370 3635 54 None -1 34 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
CHEMBL487387 3635 54 None -1 34 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2014.09.024
127031422 138189 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 4 1 5 3.5 CCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3779928 138189 0 None 3 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 355 4 1 5 3.5 CCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
14198584 196592 0 None 12 2 Rat 7.9 pKi = 7.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00118a012
CHEMBL57579 196592 0 None 12 2 Rat 7.9 pKi = 7.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00118a012
117773559 131962 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 416 3 2 5 3.7 Cc1c(-c2ccc(Oc3ncccc3C(F)(F)F)c3[nH]ccc23)n(C)c(=O)[nH]c1=O nan
CHEMBL3697624 131962 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 416 3 2 5 3.7 Cc1c(-c2ccc(Oc3ncccc3C(F)(F)F)c3[nH]ccc23)n(C)c(=O)[nH]c1=O nan
10005244 110863 0 None 7 2 Rat 6.9 pKi = 6.9 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 476 5 1 3 5.9 CN(C)c1ccc(/C=C/CN2CCc3cc(Br)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL326927 110863 0 None 7 2 Rat 6.9 pKi = 6.9 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 476 5 1 3 5.9 CN(C)c1ccc(/C=C/CN2CCc3cc(Br)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
44323876 204856 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL88870 204856 0 None 2 4 Rat 6.9 pKi = 6.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 330 1 0 2 4.6 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
1353 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
3559 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
86 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
CHEMBL54 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
DB00502 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2008.06.030
117773696 131904 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 6 2.7 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1F nan
CHEMBL3697567 131904 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 6 2.7 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1F nan
86764101 131956 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
CHEMBL3697618 131956 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
276 3457 45 None -81 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
5312149 3457 45 None -81 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
CHEMBL431298 3457 45 None -81 13 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/j.bmcl.2007.11.045
11575479 94305 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL253096 94305 0 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 425 4 1 3 5.7 CC1(c2cccc(OCc3ccccc3)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
1353 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
3559 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
86 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
CHEMBL54 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
DB00502 1880 85 None -38 85 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.07.018
118709178 112849 0 None -69 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3317465 112849 0 None -69 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1154 32 0 17 9.5 O=C(CCc1cn(CCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189392 122731 0 None -54 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
CHEMBL3613878 122731 0 None -54 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 441 5 0 7 3.6 Clc1cccc(N2CCN(CCc3cn(-c4ccn5nccc5c4)nn3)CC2)c1Cl 10.1016/j.bmc.2015.07.050
71458071 79090 0 None -102 6 Bovine 5.9 pKi = 5.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
CHEMBL2113718 79090 0 None -102 6 Bovine 5.9 pKi = 5.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(02)00316-5
6603820 95330 13 None -4 13 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9800292
CHEMBL25856 95330 13 None -4 13 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm9800292
6603954 200918 2 None -81 3 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm9800292
CHEMBL612083 200918 2 None -81 3 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm9800292
11068912 30648 0 None -39 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL139722 30648 0 None -39 4 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
11057969 33052 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL141845 33052 0 None -1778 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 379 6 1 6 1.9 COc1ccccc1N1CCN(CCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44360992 118899 0 None -134 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
CHEMBL344677 118899 0 None -134 6 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc3ccnn23)CC1 10.1021/jm025558r
11036640 120634 0 None -29 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL357684 120634 0 None -29 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44264642 203095 0 None -398 4 Bovine 5.9 pKi = 5.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7506 203095 0 None -398 4 Bovine 5.9 pKi = 5.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
56833463 67994 0 None -602 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916552 67994 0 None -602 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 578 17 1 9 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
137643951 157714 0 None -831 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4088639 157714 0 None -831 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 8 1 7 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
56837635 68966 0 None -3981 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928132 68966 0 None -3981 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1129 44 2 17 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
118709164 112911 0 None -199 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318836 112911 0 None -199 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 902 22 0 8 11.7 O=C(CCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44371932 119143 0 None -467 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL346805 119143 0 None -467 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 354 4 0 5 3.1 O=Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
10404144 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL7927 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(02)00316-5
10404144 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
CHEMBL7927 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm015522j
44380785 120290 0 None -363 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL355566 120290 0 None -363 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
10404144 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7927 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
10404144 203591 19 None -2187 10 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
CHEMBL7927 203591 19 None -2187 10 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm060166w
44340097 9349 0 None -4365 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 9349 0 None -4365 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
45270861 193410 0 None -33 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL549638 193410 0 None -33 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 353 3 0 5 3.1 Cc1cc2nc(C)c(CN3CCN(c4ccc(F)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
681 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
940 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
947 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
CHEMBL59 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
DB00988 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.ejmech.2012.07.025
137651322 156933 0 None -13489 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
CHEMBL4079375 156933 0 None -13489 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 465 8 2 9 2.2 O=Cc1cnn2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc12 10.1016/j.bmc.2017.08.037
137640189 156411 0 None -15848 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4072780 156411 0 None -15848 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 466 7 3 7 2.6 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
681 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
940 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
947 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
CHEMBL59 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
DB00988 1437 65 None -154 38 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.05.014
107995 96678 17 None -28840 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
29982233 96678 17 None -28840 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
CHEMBL267723 96678 17 None -28840 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O 10.1016/j.bmc.2007.07.017
44329282 168549 0 None -19 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL440143 168549 0 None -19 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
10404144 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL7927 203591 19 None -4466 10 Bovine 4.9 pKi = 4.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
10247720 12943 0 None -794 5 Bovine 4.9 pKi = 4.9 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL1190042 12943 0 None -794 5 Bovine 4.9 pKi = 4.9 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL540039 12943 0 None -794 5 Bovine 4.9 pKi = 4.9 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 320 4 1 4 2.2 c1ccc(C2=NC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(01)00484-x
10474964 129949 0 None -8511 7 Bovine 4.9 pKi = 4.9 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 129949 0 None -8511 7 Bovine 4.9 pKi = 4.9 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 129949 0 None -8511 7 Bovine 4.9 pKi = 4.9 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
10404144 203591 19 None -4466 10 Human 4.9 pKi = 4.9 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL7927 203591 19 None -4466 10 Human 4.9 pKi = 4.9 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/acs.jmedchem.7b00151
45481841 196383 0 None -14 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(Cl)c(O)cc21 10.1016/j.bmc.2009.05.079
CHEMBL574111 196383 0 None -14 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(Cl)c(O)cc21 10.1016/j.bmc.2009.05.079
90142280 166743 1 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4293757 166743 1 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
15711855 13301 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192799 13301 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL544099 13301 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
13838742 98942 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
CHEMBL282710 98942 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
117773223 131929 0 None - 1 Human 5.9 pKi = 5.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 350 4 2 5 2.6 Cc1cc(Oc2ncccc2C(N)=O)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697591 131929 0 None - 1 Human 5.9 pKi = 5.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 350 4 2 5 2.6 Cc1cc(Oc2ncccc2C(N)=O)ccc1-c1c(C)n[nH]c(=O)c1C nan
25129807 102819 0 None -63 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084502 102819 0 None -63 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 366 3 2 2 4.8 O[C@@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
91899762 128930 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cn[nH]c(=O)c1C nan
CHEMBL3671307 128930 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cn[nH]c(=O)c1C nan
491 191 4 None -151356 12 Rat 4.9 pKi = 4.9 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
9891167 191 4 None -151356 12 Rat 4.9 pKi = 4.9 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
CHEMBL13856 191 4 None -151356 12 Rat 4.9 pKi = 4.9 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 476 6 1 7 3.6 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1cccc(c1)C 10.1016/s0960-894x(01)00159-7
2284 3133 27 None -36 28 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
4926 3133 27 None -36 28 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
7281 3133 27 None -36 28 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
CHEMBL564 3133 27 None -36 28 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
DB00420 3133 27 None -36 28 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C nan
44415582 138461 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 444 1 0 4 5.3 Cc1ccccc1C(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL378543 138461 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 444 1 0 4 5.3 Cc1ccccc1C(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
681 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
940 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
947 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
CHEMBL59 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
DB00988 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2009.04.047
44241581 13907 0 None -81 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 373 2 3 4 4.6 CCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197218 13907 0 None -81 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 373 2 3 4 4.6 CCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL562935 13907 0 None -81 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 373 2 3 4 4.6 CCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
3032727 13365 1 None -562 2 Rat 6.9 pKi = 6.9 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 281 1 2 3 3.2 CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL1193245 13365 1 None -562 2 Rat 6.9 pKi = 6.9 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 281 1 2 3 3.2 CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL544618 13365 1 None -562 2 Rat 6.9 pKi = 6.9 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 281 1 2 3 3.2 CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
74223828 128921 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 4 1 6 3.8 COc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
CHEMBL3671299 128921 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 4 1 6 3.8 COc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncnc1C nan
10519436 11122 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1178784 11122 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL41238 11122 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
10664137 162205 0 None 10 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL417164 162205 0 None 10 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
15711851 13429 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL1193797 13429 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL545264 13429 0 None 2 3 Goldfish 6.9 pKi = 6.9 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
9838572 63123 0 None -23 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 279 1 0 3 2.6 CN1CCN(C2=Cc3ccccc3Cn3cccc32)CC1 10.1021/jm049629t
CHEMBL179775 63123 0 None -23 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 279 1 0 3 2.6 CN1CCN(C2=Cc3ccccc3Cn3cccc32)CC1 10.1021/jm049629t
10072800 96214 3 None -6 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 384 4 0 5 4.7 O=C1c2ccsc2CC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL263790 96214 3 None -6 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 384 4 0 5 4.7 O=C1c2ccsc2CC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL554199 96214 3 None -6 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 384 4 0 5 4.7 O=C1c2ccsc2CC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
12050193 201506 0 None -2 4 Bovine 5.9 pKi = 5.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64325 201506 0 None -2 4 Bovine 5.9 pKi = 5.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 443 5 0 5 4.9 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
12050199 100345 0 None -32 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL293225 100345 0 None -32 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 7 1 5 4.9 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
10068602 99740 1 None -4677 3 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 384 6 0 4 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL28831 99740 1 None -4677 3 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 384 6 0 4 3.1 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
71528209 86544 0 None -1949 7 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
CHEMBL2323582 86544 0 None -1949 7 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 465 6 0 3 5.8 CC1=CC(C)=[N+]2C1=C(c1ccc(OCCCN3CCCCC3)cc1)c1c(C)cc(C)n1[B-]2(F)F 10.1021/ml300383n
57398351 69815 0 None -13 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940406 69815 0 None -13 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 347 6 0 2 5.1 Fc1ccc(OCCCN2CCC(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
10801923 177190 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 269 2 2 3 2.7 COc1cc2c(cc1O)C(c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4642805 177190 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 269 2 2 3 2.7 COc1cc2c(cc1O)C(c1ccccc1)CNCC2 10.1016/j.bmcl.2020.127305
44555445 198247 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)Cc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL594789 198247 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)Cc1ccccc1C2 10.1016/j.bmc.2009.08.028
127027739 137457 0 None -11220 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 382 7 1 6 1.7 O=C(NCCCN1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3764390 137457 0 None -11220 3 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 382 7 1 6 1.7 O=C(NCCCN1CCN(Cc2ccc3c(c2)OCO3)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
60167166 74945 0 None -41 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037430 74945 0 None -41 8 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 371 5 0 4 4.7 Clc1ccc(N2CCN(CCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
441383 20133 54 None -12 17 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20133 54 None -12 17 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
154705038 176072 1 None -38 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4584481 176072 1 None -38 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4598001 176072 1 None -38 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.2 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
145967904 164545 0 None -11 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4227192 164545 0 None -11 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 247 6 1 2 3.8 CCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
145988180 164679 0 None -10 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4229178 164679 0 None -10 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 10 1 2 5.3 CCCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
72699716 114691 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344459 114691 0 None -16 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
44326751 108128 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL320572 108128 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL539544 108128 0 None -2 4 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 384 3 0 5 4.7 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2sccc21 10.1021/jm981094e
24949690 181024 0 None -1819 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
CHEMBL477200 181024 0 None -1819 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
154705015 175940 1 None -295 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 175940 1 None -295 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 175940 1 None -295 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
9930475 204567 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL87026 204567 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm981094e
9930475 204567 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87026 204567 0 None -32 4 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 393 5 0 3 4.9 O=C(c1ccc(F)cc1)C1CCN(CCC2CCCc3ccccc3C2=O)CC1 10.1021/jm00042a009
91899761 128927 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 317 3 1 5 3.8 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
CHEMBL3671304 128927 0 None - 1 Human 6.9 pKi = 6.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 317 3 1 5 3.8 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
15937725 116603 0 None 158 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 279 1 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C(C2CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL339342 116603 0 None 158 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 279 1 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C(C2CCCC2)C1 10.1016/S0960-894X(00)80155-9
44415615 139005 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL379560 139005 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
44415507 79877 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
CHEMBL214016 79877 0 None 87 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
10710466 155874 0 None 11 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL40667 155874 0 None 11 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
74223725 128896 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C nan
CHEMBL3671275 128896 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C nan
117774412 131933 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.5 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)F nan
CHEMBL3697595 131933 0 None - 1 Human 7.9 pKi = 7.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.5 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)F nan
44281202 99939 2 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 379 1 1 2 3.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
CHEMBL290118 99939 2 None - 1 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 379 1 1 2 3.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00127a005
44320061 105552 0 None 75 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313304 105552 0 None 75 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
17755866 142352 1 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
CHEMBL389356 142352 1 None 1 5 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm070388+
681 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
940 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
947 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
CHEMBL59 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
DB00988 1437 65 None -154 38 Human 6.9 pKi = 6.9 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00018a002
15115517 9621 0 None -426 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL113196 9621 0 None -426 2 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
6852376 91167 11 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
CHEMBL1467585 91167 11 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
CHEMBL24077 91167 11 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
CHEMBL503958 91167 11 None -3 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00115a012
2865 4079 67 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
59 4079 67 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
60854 4079 67 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL708 4079 67 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00246 4079 67 None -114 53 Human 6.9 pKi = 6.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1016/j.bmc.2008.06.030
146025727 171119 0 None -4 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171119 0 None -4 27 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44415686 79569 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 7 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212700 79569 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 7 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
24800527 155179 0 None -4 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 1 3 3.5 CCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL405369 155179 0 None -4 2 Rat 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 1 3 3.5 CCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
57403525 69811 0 None -85 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940402 69811 0 None -85 10 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 361 6 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(CCCCc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
118709159 112906 0 None -21 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318831 112906 0 None -21 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 832 17 0 8 9.7 O=C(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
2337 3205 72 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
50 3205 72 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
5002 3205 72 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL716 3205 72 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
DB01224 3205 72 None -53 62 Human 5.9 pKi = 5.9 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1016/j.bmc.2008.06.030
44403219 71560 0 None -1174 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
CHEMBL197162 71560 0 None -1174 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)nc1 10.1016/j.bmcl.2005.07.037
10448562 114622 1 None 12 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL334350 114622 1 None 12 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
16105549 67443 0 None -2884 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL1908879 67443 0 None -2884 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
CHEMBL221640 67443 0 None -2884 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(F)nc3)cc2)CC1 10.1021/jm0611152
71459759 83657 0 None -81 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207633 83657 0 None -81 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 432 4 0 3 5.5 COc1ccccc1N1CCN(Cc2cc(C#Cc3ccccc3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44567686 191469 0 None -1 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 265 1 0 2 3.4 COc1cc2c3c(c1)-c1ccccc1C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.06.016
CHEMBL520262 191469 0 None -1 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 265 1 0 2 3.4 COc1cc2c3c(c1)-c1ccccc1C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.06.016
53327663 66146 0 None -134 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852239 66146 0 None -134 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3215641 66146 0 None -134 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 342 3 3 5 2.9 CN1CCc2cc(SCCN)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
137643309 157869 0 None -1174 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4090208 157869 0 None -1174 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccn2ncc(C=O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
122181326 121353 0 None -426 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
CHEMBL3590077 121353 0 None -426 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 413 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)/N=N/c2ccc(F)cc2)CC1 10.1016/j.bmc.2014.12.012
122181329 121356 0 None -4168 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590080 121356 0 None -4168 6 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 394 10 1 2 4.6 CCCN(CCCCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
57402787 68853 0 None -371 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1926700 68853 0 None -371 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 977 28 2 17 4.4 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
9995904 31004 2 None -14454 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL140099 31004 2 None -14454 5 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm060166w
11626748 139629 0 None -14 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
CHEMBL380287 139629 0 None -14 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 459 4 0 7 3.1 CN1CCN(c2ccc3nc(CN4CCN(c5ccc(Cl)c(Cl)c5)CC4)cn3n2)CC1 10.1021/jm060166w
44340186 9569 0 None -45 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 9569 0 None -45 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
9995904 31004 2 None -14454 5 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140099 31004 2 None -14454 5 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4)CC3)cc2c1 10.1021/jm0009989
25139180 183759 0 None -42 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL484357 183759 0 None -42 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 490 10 1 2 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
25099152 186703 0 None -20417 3 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 466 9 2 5 5.1 CCCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c2ccccc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL492883 186703 0 None -20417 3 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 466 9 2 5 5.1 CCCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c2ccccc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
25130817 186929 0 None -5888 3 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 518 9 2 5 6.5 CC(C)CCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL494309 186929 0 None -5888 3 Rat 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 518 9 2 5 6.5 CC(C)CCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
73347474 90628 0 None -12882 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397478 90628 0 None -12882 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
137655556 157993 0 None -3801 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4091507 157993 0 None -3801 5 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 2 7 3.3 O=c1ccc2c(N3CCCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
71733935 90552 0 None -30902 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2396663 90552 0 None -30902 6 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
14665503 90803 0 None -21379 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL240106 90803 0 None -21379 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 382 7 1 4 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
44437896 151936 0 None -1174 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397103 151936 0 None -1174 4 Pig 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 400 6 1 3 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)ccc1OC 10.1016/j.bmc.2007.07.017
44329283 205907 0 None -30 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@H]1CCn2c(CO)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL95230 205907 0 None -30 3 Bovine 4.9 pKi = 4.9 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 250 6 1 3 2.4 CCCN(CCC)[C@H]1CCn2c(CO)ccc2C1 10.1016/s0960-894x(01)00564-9
53321194 58294 0 None -56 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684135 58294 0 None -56 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
154724650 175763 1 None -74 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4543870 175763 1 None -74 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595492 175763 1 None -74 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
154706711 175941 1 None -48 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4439535 175941 1 None -48 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596930 175941 1 None -48 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
10024430 205879 0 None -41 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL95098 205879 0 None -41 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 8 0 4 3.9 O=C(CCCN1CCN(CCC2Cc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
135398737 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
38 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
722 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
CHEMBL42 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
DB00363 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.034
135398737 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
38 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
722 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
CHEMBL42 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
DB00363 944 89 None -44 91 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2006.06.022
156011597 176805 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4637938 176805 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
72699717 114692 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 5 1 4 4.9 CCCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344460 114692 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 5 1 4 4.9 CCCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
2600 3720 73 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
2608 3720 73 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
5405 3720 73 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
CHEMBL17157 3720 73 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
DB00342 3720 73 None -7 13 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O nan
57393083 69824 0 None -21 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940415 69824 0 None -21 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 314 6 0 4 2.8 Fc1ccc(CCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
45483261 196209 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 380 3 0 6 3.4 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2ncncc21 10.1016/j.bmcl.2009.09.041
CHEMBL572708 196209 0 None -5 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 380 3 0 6 3.4 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2ncncc21 10.1016/j.bmcl.2009.09.041
11795165 9279 1 None -3 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2sccc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL111352 9279 1 None -3 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2sccc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL541842 9279 1 None -3 3 Rat 6.9 pKi = 6.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2sccc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
45267373 13904 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197201 13904 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL562460 13904 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 295 1 2 3 3.5 CCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
44278589 97998 0 None -11 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@@H]1Cc1ccccc1-3 10.1021/jm00402a024
CHEMBL27574 97998 0 None -11 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@@H]1Cc1ccccc1-3 10.1021/jm00402a024
5311191 112134 5 None -35 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL330274 112134 5 None -35 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
15021875 103890 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm00111a046
CHEMBL310153 103890 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm00111a046
15021875 103890 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm981094e
CHEMBL310153 103890 0 None -208 5 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 350 4 0 4 3.3 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc3C2)CC1 10.1021/jm981094e
10645469 110068 0 None -5 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL325253 110068 0 None -5 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL542428 110068 0 None -5 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 414 7 0 5 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccsc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
9979654 206182 0 None -14 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL96781 206182 0 None -14 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 422 8 0 4 4.2 O=C(CCCN1CCN(CCC2CCc3ccccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
155516042 175719 0 None -891 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 175719 0 None -891 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 175719 0 None -891 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
12442999 87082 6 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2334890 87082 6 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
57391307 69820 0 None -19 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940411 69820 0 None -19 7 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 348 6 0 3 4.1 Fc1ccc(OCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
71722301 102000 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3040157 102000 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
CHEMBL3216146 102000 0 None -2 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1 10.1016/j.bmc.2013.05.014
53324045 56776 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644980 56776 0 None -3 16 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 487 7 1 2 7.3 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2018.10.036
44358192 200457 3 None -676 2 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 345 1 2 2 2.3 CN1C[C@H](C(N)=O)C=C2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1021/jm9800292
CHEMBL609151 200457 3 None -676 2 Human 5.9 pKi = 5.9 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 345 1 2 2 2.3 CN1C[C@H](C(N)=O)C=C2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1021/jm9800292
10862670 18316 0 None -281 5 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1 10.1021/jm0211220
CHEMBL126439 18316 0 None -281 5 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1 10.1021/jm0211220
CHEMBL127317 18316 0 None -281 5 Rat 5.9 pKi = 5.9 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccccc3n2)CC1 10.1021/jm0211220
15467373 101384 0 None -107 4 Bovine 4.9 pKi = 4.9 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL300553 101384 0 None -107 4 Bovine 4.9 pKi = 4.9 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(99)00302-9
53946795 67391 1 None -1122 2 Rat 4.9 pKi = 4.9 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
CHEMBL1907814 67391 1 None -1122 2 Rat 4.9 pKi = 4.9 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
136074292 201876 0 None -3 2 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cnccc3Nc3ccccc32)CC1 10.1021/jm00067a009
CHEMBL66730 201876 0 None -3 2 Rat 4.9 pKi = 4.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cnccc3Nc3ccccc32)CC1 10.1021/jm00067a009
44304652 198638 0 None -28 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 198638 0 None -28 4 Bovine 4.9 pKi = 4.9 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
71062646 149011 0 None -2238 13 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
CHEMBL3946661 149011 0 None -2238 13 Mouse 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 338 6 0 4 2.8 c1ccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)cc1 nan
13373172 198101 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL593897 198101 0 None -3 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 251 0 1 2 3.0 Oc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
17756212 85941 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL231374 85941 1 None -1 5 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
2286 3134 48 None -30 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
4927 3134 48 None -30 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
7282 3134 48 None -30 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
CHEMBL643 3134 48 None -30 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
DB01069 3134 48 None -30 29 Human 5.9 pKi = 5.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C nan
11080 28872 74 None -5 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
CHEMBL1381098 28872 74 None -5 6 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 185 1 0 2 3.6 S=C=Nc1cccc2ccccc12 nan
44210226 116031 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
CHEMBL336218 116031 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
117773821 131939 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 1 4 4.0 Cc1cc(Oc2ncc(F)cc2C)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697601 131939 0 None - 1 Human 6.9 pKi = 6.9 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 1 4 4.0 Cc1cc(Oc2ncc(F)cc2C)ccc1-c1c(C)n[nH]c(=O)c1C nan
10851717 78068 1 None -15 5 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 78068 1 None -15 5 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
154725484 175891 1 None -630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4439544 175891 1 None -630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596514 175891 1 None -630 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
9970201 170076 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
CHEMBL445129 170076 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
168295528 192429 0 None -338 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192429 0 None -338 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192429 0 None -338 20 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
10249506 8717 0 None -6 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL109673 8717 0 None -6 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL544091 8717 0 None -6 4 Rat 5.9 pKi = 5.9 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
10851717 78068 1 None -15 5 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 78068 1 None -15 5 Rat 6.9 pKi = 6.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
155770281 177173 0 None -1 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4642592 177173 0 None -1 9 Human 5.9 pKi = 5.9 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
23656544 169544 0 None -575 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 2 3 2.6 CN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
CHEMBL444368 169544 0 None -575 3 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 2 3 2.6 CN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
5352624 66903 40 None -3 5 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
CHEMBL18797 66903 40 None -3 5 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 340 4 1 2 5.4 CSc1ccc(/C=C2/C(C)=C(CC(=O)O)c3cc(F)ccc32)cc1 nan
2662 11279 124 None -3 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
CHEMBL118 11279 124 None -3 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 nan
16104 161368 15 None -1 5 Rat 7.9 pKi = 7.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
CHEMBL415300 161368 15 None -1 5 Rat 7.9 pKi = 7.9 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00043a008
44415544 79827 0 None 169 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Br)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213775 79827 0 None 169 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Br)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415628 139262 0 None 104 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL379874 139262 0 None 104 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccs3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
156017431 177203 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643069 177203 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 317 2 1 3 3.7 COc1cc2c(cc1O)C(c1ccccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
10981731 15100 0 None -3 3 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL121274 15100 0 None -3 3 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
11014679 114290 0 None -3 3 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL333955 114290 0 None -3 3 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
16351 102257 41 None -4 5 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL304902 102257 41 None -4 5 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
9841398 99058 3 None 3 4 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL28338 99058 3 None 3 4 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
44320024 106584 0 None 51 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315750 106584 0 None 51 2 Rat 7.9 pKi = 7.9 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86767093 128901 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
CHEMBL3671280 128901 0 None - 1 Human 7.9 pKi = 7.9 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
16351 102257 41 None -4 5 Rat 7.9 pKi = 7.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL304902 102257 41 None -4 5 Rat 7.9 pKi = 7.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
11014679 114290 0 None -3 3 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL333955 114290 0 None -3 3 Rat 7.9 pKi = 7.9 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 391 2 0 4 4.1 CCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
10981731 15100 0 None -3 3 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL121274 15100 0 None -3 3 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 377 1 0 4 3.7 CN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
44276412 97216 0 None 10 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL27117 97216 0 None 10 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44276556 99241 0 None 30 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL284644 99241 0 None 30 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
45482180 196227 0 None -17 4 Pig 6.9 pKi = 6.9 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL572867 196227 0 None -17 4 Pig 6.9 pKi = 6.9 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 544 12 1 7 4.6 COc1ccc(-n2cc(CCCC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
130442480 174698 0 None -1 24 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 174698 0 None -1 24 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
53328903 66125 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
CHEMBL1802237 66125 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
CHEMBL1852107 66125 0 None 2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 353 0 2 5 3.5 CN1CCc2c3c(cc4c2[C@H]1Cc1ccc(O)c(O)c1-4)SCCC3=O 10.1016/j.ejmech.2011.04.028
52919 14317 43 None -15 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL1200986 14317 43 None -15 4 Pig 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
14198590 201695 1 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00118a012
CHEMBL65397 201695 1 None -1 4 Rat 6.9 pKi = 6.9 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00118a012
10895106 32011 0 None -27 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL140968 32011 0 None -27 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 421 9 1 6 3.1 COc1ccccc1N1CCN(CCCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
10053476 116246 0 None -2570 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
CHEMBL337531 116246 0 None -2570 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 559 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[te]1 10.1021/jm025558r
44454707 97382 0 None -28 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
CHEMBL272073 97382 0 None -28 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmcl.2007.12.026
44393411 65762 0 None -316 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL183871 65762 0 None -316 5 Pig 5.9 pKi = 5.9 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 587 7 1 4 6.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2s1 10.1016/j.bmcl.2004.05.052
71459760 83658 0 None -74 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207634 83658 0 None -74 5 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 398 5 0 3 5.3 CCCC#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
25072941 155933 0 None -331 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 155933 0 None -331 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137640371 156273 0 None -933 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071185 156273 0 None -933 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 421 10 1 6 4.3 CCCN(CCCCOc1ccc2c(C=O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
118709165 112912 0 None -66 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318837 112912 0 None -66 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 916 23 0 8 12.1 O=C(CCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709167 112914 0 None -16 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318839 112914 0 None -16 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 972 27 0 8 13.6 O=C(CCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709170 112918 0 None -53 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318842 112918 0 None -53 4 Pig 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1057 33 0 8 16.0 O=C(CCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44372296 118982 0 None -72 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL345357 118982 0 None -72 4 Bovine 5.9 pKi = 5.9 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1ccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn2c1 10.1016/s0960-894x(01)00814-9
CHEMBL5074765 212561 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5079653 212859 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3NC4=O)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5085145 213178 0 None -4 2 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None N[C@H]1C[C@@H](CO)[C@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
CHEMBL5087121 213297 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of dopamine D1 receptor (unknown origin) assessed as binding constantInhibition of dopamine D1 receptor (unknown origin) assessed as binding constant
ChEMBL None None None CN(C)C(=O)COC(=O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
44380774 119969 0 None -851 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL354180 119969 0 None -851 4 Bovine 4.9 pKi = 4.9 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
44336571 4762 0 None -61 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL104201 4762 0 None -61 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
15508239 6179 0 None -5 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL108160 6179 0 None -5 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 336 3 0 2 4.6 C[Si](C)(C)C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
15508240 110038 0 None -15 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL325104 110038 0 None -15 4 Bovine 4.9 pKi = 4.9 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 264 3 0 2 3.3 C#Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
10496727 13151 0 None -24 3 Rat 4.9 pKi = 4.9 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 331 2 0 3 4.7 COc1c(-c2ccco2)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL119150 13151 0 None -24 3 Rat 4.9 pKi = 4.9 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 331 2 0 3 4.7 COc1c(-c2ccco2)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
90644066 111548 0 None -17 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289653 111548 0 None -17 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 5 0 3 4.8 Clc1ccc(N2CCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
53328721 66102 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1851968 66102 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3216523 66102 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
279 1631 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00067a009
49381 1631 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00067a009
CHEMBL63756 1631 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00067a009
279 1631 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00030a011
49381 1631 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00030a011
CHEMBL63756 1631 26 None -29 17 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 10.1021/jm00030a011
44210226 116031 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
CHEMBL336218 116031 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 1 2 4.0 CN1Cc2ccccc2C2c3cc(O)c(Br)cc3CCC21 10.1021/jm00051a008
14198588 170941 2 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
CHEMBL446396 170941 2 None 2 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
14198590 201695 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00129a006
CHEMBL65397 201695 1 None 1 4 Human 6.9 pKi = 6.9 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@H]2c1ccccc1 10.1021/jm00129a006
44582676 189187 0 None -10 17 Human 5.9 pKi = 5.9 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189187 0 None -10 17 Human 5.9 pKi = 5.9 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
13922235 99079 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
CHEMBL283489 99079 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
13922235 99079 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL283489 99079 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
13922235 99079 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
CHEMBL283489 99079 1 None -23 2 Rat 5.9 pKi = 5.9 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
10433336 78109 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 439 8 1 4 4.3 BC#N.CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL2111925 78109 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 439 8 1 4 4.3 BC#N.CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
135 2496 38 None -46 57 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
1796 2496 38 None -46 57 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
4184 2496 38 None -46 57 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
CHEMBL6437 2496 38 None -46 57 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
DB06148 2496 38 None -46 57 Rat 5.9 pKi = 5.9 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm049632c
5320227 95393 54 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 354 6 1 5 4.6 CC(C)=CC(O)C/C(C)=C/COc1c2ccoc2cc2oc(=O)ccc12 10.1016/j.bmc.2007.12.021
CHEMBL258939 95393 54 None - 1 Rat 5.9 pKi = 5.9 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 354 6 1 5 4.6 CC(C)=CC(O)C/C(C)=C/COc1c2ccoc2cc2oc(=O)ccc12 10.1016/j.bmc.2007.12.021
154706461 175774 1 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4470439 175774 1 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595600 175774 1 None -60 5 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 6.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
44537925 197067 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL582945 197067 0 None -1 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 624 12 2 9 5.2 COc1ccccc1N1CCN(CCCn2cc(CCCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
156010755 176567 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 351 2 1 3 4.3 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4633950 176567 0 None -2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 351 2 1 3 4.3 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CN(C)CC2 10.1016/j.bmcl.2020.127305
11112574 18321 0 None -131 3 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 419 8 1 6 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3n2)CC1 10.1021/jm0211220
CHEMBL127344 18321 0 None -131 3 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 419 8 1 6 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3n2)CC1 10.1021/jm0211220
10732337 112492 0 None -13 3 Rat 5.8 pKi = 5.8 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 291 2 0 2 4.1 C=Cc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL331100 112492 0 None -13 3 Rat 5.8 pKi = 5.8 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 291 2 0 2 4.1 C=Cc1ccc2c(c1OC)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
70684207 75717 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057452 75717 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70684207 75717 0 None - 1 Human 5.8 pKi = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057452 75717 0 None - 1 Human 5.8 pKi = 5.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)C1Cc3cc(C)cc(C)c3CN1CC2 nan
31101 720 39 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 720 39 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 720 39 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 720 39 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 720 39 None -436 35 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
44582490 189544 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 4.2 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL517349 189544 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 4.2 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
1353 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
3559 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
86 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
CHEMBL54 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
DB00502 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9810396
196129 67456 12 None -1819 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67456 12 None -1819 15 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
154704368 175897 1 None -31 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4569006 175897 1 None -31 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596571 175897 1 None -31 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 421 11 2 2 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
11408148 128198 0 None -371 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL366904 128198 0 None -371 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 443 6 1 4 4.8 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
154725234 175718 1 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4585289 175718 1 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4595149 175718 1 None -2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 472 12 0 6 5.2 CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
73453 29403 22 None -208 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29403 22 None -208 17 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
33630 178379 94 None -5 27 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL47050 178379 94 None -5 27 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
2389 3279 114 None -331 67 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
5073 3279 114 None -331 67 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
96 3279 114 None -331 67 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
CHEMBL85 3279 114 None -331 67 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
DB00734 3279 114 None -331 67 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm049632c
156014482 176638 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 303 2 2 3 3.3 COc1cc2c(cc1O)C(c1ccccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4635423 176638 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 303 2 2 3 3.3 COc1cc2c(cc1O)C(c1ccccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
2389 3279 114 None -467 67 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
5073 3279 114 None -467 67 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
96 3279 114 None -467 67 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
CHEMBL85 3279 114 None -467 67 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
DB00734 3279 114 None -467 67 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2009.09.041
21589014 143540 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3903297 143540 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
10044334 205392 13 None -64 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL92145 205392 13 None -64 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 364 5 0 4 3.7 COc1ccccc1N1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
44415568 139613 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL380236 139613 0 None 9 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C(F)(F)F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
155529453 170872 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranesDisplacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranes
ChEMBL 385 4 2 3 4.3 COc1ccc2[nH]cc(C3=CCN(Cc4cc(=O)[nH]c5ccccc45)CC3)c2c1 10.1016/j.ejmech.2019.07.050
CHEMBL4463034 170872 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranesDisplacement of [3H]SCH23390 from human D1 receptor expressed in commercial cell membranes
ChEMBL 385 4 2 3 4.3 COc1ccc2[nH]cc(C3=CCN(Cc4cc(=O)[nH]c5ccccc45)CC3)c2c1 10.1016/j.ejmech.2019.07.050
11406143 65801 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 372 7 0 3 4.5 c1ccc(Cc2ccccc2OCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm049720x
CHEMBL184073 65801 0 None -2 4 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 372 7 0 3 4.5 c1ccc(Cc2ccccc2OCCN2CCN(c3ccccc3)CC2)cc1 10.1021/jm049720x
10895039 18334 0 None -3019 8 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL127400 18334 0 None -3019 8 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
CHEMBL129022 18334 0 None -3019 8 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 418 8 1 5 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3cn2)CC1 10.1021/jm0211220
44593524 183474 0 None -12 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.11.025
CHEMBL482276 183474 0 None -12 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 365 5 0 4 4.5 CCCCC(=O)Oc1cccc2c1-c1cc(OC)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.11.025
10740666 25918 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 416 6 1 3 4.5 CN(C)CCCCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL135616 25918 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 416 6 1 3 4.5 CN(C)CCCCN1CCc2cc(Br)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL4576555 212264 3 None -1 14 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a DRD1
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 nan
117773324 131909 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2cc(C3CC3)ccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697572 131909 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2cc(C3CC3)ccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
1218 3559 24 None -11 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
938 3559 24 None -11 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
CHEMBL353335 3559 24 None -11 7 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/acsmedchemlett.9b00050
44415611 165706 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 435 2 1 6 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccco3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL426868 165706 0 None 54 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 435 2 1 6 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccco3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11567963 154516 0 None 40 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 419 3 1 5 3.9 COc1cc2c(cc1OC)-c1c(OC)c(O)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL401689 154516 0 None 40 2 Rat 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 419 3 1 5 3.9 COc1cc2c(cc1OC)-c1c(OC)c(O)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
10220 138231 12 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)C1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780481 138231 12 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)C1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
86763997 131951 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697613 131951 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
9884087 14468 0 None -5 3 Rat 7.8 pKi = 7.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 14468 0 None -5 3 Rat 7.8 pKi = 7.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
86767098 128908 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
CHEMBL3671287 128908 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
130442572 171342 0 None -3 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171342 0 None -3 24 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
44415395 137633 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 423 2 1 5 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL376928 137633 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 423 2 1 5 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
53328901 66148 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1802236 66148 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852245 66148 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 371 4 3 5 3.4 CN1CCc2cc(SCCC(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
90644226 111287 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287395 111287 0 None -72 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 490 9 0 7 4.8 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709179 112927 0 None -61 4 Pig 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318851 112927 0 None -61 4 Pig 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1198 35 0 18 9.5 O=C(CCc1cn(CCOCCOCCOCCOCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
681 1437 65 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
940 1437 65 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
947 1437 65 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
CHEMBL59 1437 65 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
DB00988 1437 65 None -97 38 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a018
10546131 99943 0 None 20 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290149 99943 0 None 20 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2 10.1021/jm970038v
10476504 33268 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 33268 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
44361021 118281 0 None -537 6 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
CHEMBL342060 118281 0 None -537 6 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccn3nccc3c2)CC1 10.1021/jm025558r
10884046 164817 0 None -107 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL423735 164817 0 None -107 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
44436602 144680 0 None -245 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL391256 144680 0 None -245 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2007.08.038
44436598 148763 0 None -3388 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL394473 148763 0 None -3388 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1cccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
53361302 63519 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1803049 63519 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2009919
11696910 77394 0 None -1174 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
CHEMBL209034 77394 0 None -1174 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 395 3 0 5 4.0 Clc1ccc2nc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)cn2n1 10.1021/jm060166w
53361302 63519 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803049 63519 0 None -208 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 493 13 0 8 4.4 CCCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
45268292 195012 0 None -446 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL564688 195012 0 None -446 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 460 4 1 6 3.5 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
71583848 87303 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 87303 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
137636498 155655 0 None -660 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064186 155655 0 None -660 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 446 7 2 6 3.8 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5ncccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
118709171 112919 0 None -5 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318843 112919 0 None -5 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1085 35 0 8 16.8 O=C(CCCCCCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
122189389 122728 0 None -346 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613875 122728 0 None -346 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 497 8 0 8 4.2 O=Cc1cnn2ccc(-n3cc(CCCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
13678304 101243 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 229 3 3 3 2.3 NCCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
CHEMBL299511 101243 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 229 3 3 3 2.3 NCCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
44371996 53341 0 None -8 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL160266 53341 0 None -8 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 500 6 0 6 4.6 Clc1ccc(N2CCN(Cc3cnn4c(N5CCN(Cc6ccccc6)CC5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
44371980 53652 0 None -57 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL160536 53652 0 None -57 4 Bovine 5.8 pKi = 5.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 514 6 0 6 4.9 Cc1nn2c(N3CCN(Cc4ccccc4)CC3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
44400674 124669 0 None -3019 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 124669 0 None -3019 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
44264623 203304 0 None -1174 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7686 203304 0 None -1174 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnc4ccccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
11659604 138045 0 None -30 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL377542 138045 0 None -30 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4ccncc4n3)CC2)cc1 10.1021/jm060166w
44336552 110852 0 None -53 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL326864 110852 0 None -53 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 316 4 0 4 3.8 N#CC(C#N)=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
9977478 203235 2 None -234422 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL76402 203235 2 None -234422 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 386 6 2 5 2.4 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Br)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
56926586 68667 0 None -2089 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923415 68667 0 None -2089 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 344 3 1 5 2.6 Oc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44381217 58834 0 None -9 4 Bovine 4.8 pKi = 4.8 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL169889 58834 0 None -9 4 Bovine 4.8 pKi = 4.8 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
44371997 49660 0 None -10000 4 Bovine 4.8 pKi = 4.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
CHEMBL156851 49660 0 None -10000 4 Bovine 4.8 pKi = 4.8 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 364 3 0 4 3.6 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)c(C)nn12 10.1016/s0960-894x(01)00814-9
154704941 176053 1 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4578364 176053 1 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597877 176053 1 None -47 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 470 11 0 6 5.8 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
167715 2832 12 None -194 5 Human 5.8 pKi = 5.8 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm9800292
969 2832 12 None -194 5 Human 5.8 pKi = 5.8 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm9800292
CHEMBL225230 2832 12 None -194 5 Human 5.8 pKi = 5.8 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm9800292
46231834 199228 0 None -117 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 488 3 1 5 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCN(c5ccccn5)CC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL601635 199228 0 None -117 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 488 3 1 5 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCN(c5ccccn5)CC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
10684714 99846 0 None 13 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115372 99846 0 None 13 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL289283 99846 0 None 13 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
72301 185536 72 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL487182 185536 72 None 1 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
44415367 79538 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 411 3 1 5 3.9 CCCC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL212597 79538 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 411 3 1 5 3.9 CCCC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
44401105 69233 0 None -17 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193435 69233 0 None -17 9 Human 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1021/jm049632c
44320327 162872 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL419680 162872 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
10623632 48030 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 453 4 1 3 5.1 CCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
CHEMBL155351 48030 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 453 4 1 3 5.1 CCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
44326982 8571 0 None -7 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981094e
CHEMBL109548 8571 0 None -7 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981094e
CHEMBL545727 8571 0 None -7 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 351 4 0 3 4.1 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)c2ccccc21 10.1021/jm981094e
9886130 204704 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL87943 204704 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm981094e
9886130 204704 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87943 204704 0 None -32 4 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 379 5 0 3 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccccc3C2=O)CC1 10.1021/jm00042a009
131990 43695 10 None -6 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cnccc3Sc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL151263 43695 10 None -6 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cnccc3Sc3ccccc32)CC1 10.1021/jm00030a011
156018868 177353 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 378 5 1 4 4.0 C=CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4645375 177353 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 378 5 1 4 4.0 C=CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
12050195 201593 0 None -21 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64696 201593 0 None -21 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 6 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(Cc3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
11057 175575 19 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
3468 175575 19 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL459265 175575 19 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
CHEMBL64894 175575 19 None -2 20 Human 5.8 pKi = 5.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 nan
117772791 131900 0 None - 1 Human 6.8 pKi = 6.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 323 3 1 5 2.5 Cc1cc(Oc2ccccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697563 131900 0 None - 1 Human 6.8 pKi = 6.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 323 3 1 5 2.5 Cc1cc(Oc2ccccn2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44415625 79685 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213145 79685 0 None 4 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
11732785 163168 0 None -1819 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
CHEMBL420510 163168 0 None -1819 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 432 7 0 5 3.7 COc1ccccc1N1CCN(CCCCN2CCn3c(cc4ccccc43)C2=O)CC1 10.1021/jm0211220
44278409 99870 0 None -616 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 418 6 0 4 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL28946 99870 0 None -616 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 418 6 0 4 3.8 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
44415543 79540 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212608 79540 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415543 79540 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212608 79540 0 None 7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 445 2 1 5 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
10052433 164805 0 None -501 4 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 521 10 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL423671 164805 0 None -501 4 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 521 10 1 6 4.1 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(S(C)(=O)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
16090821 81421 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL216439 81421 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
10851717 78068 1 None -15 5 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 78068 1 None -15 5 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
1353 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
3559 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
86 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
CHEMBL54 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
DB00502 1880 85 None -74 85 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm981094e
9817779 113934 0 None -2 3 Rat 6.8 pKi = 6.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
CHEMBL333246 113934 0 None -2 3 Rat 6.8 pKi = 6.8 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
1830 2552 39 None -16 27 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
207 2552 39 None -16 27 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
23897 2552 39 None -16 27 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
CHEMBL460 2552 39 None -16 27 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
DB01618 2552 39 None -16 27 Rat 5.8 pKi = 5.8 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1016/0960-894X(95)00076-6
10851717 78068 1 None -15 5 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL2111782 78068 1 None -15 5 Rat 6.8 pKi = 6.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN([C@@H]2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
44323894 167537 0 None -1 4 Rat 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL432762 167537 0 None -1 4 Rat 7.8 pKi = 7.8 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 304 1 0 2 3.9 CC1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
15115524 108523 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 735 3 5 8 7.8 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N/C(S)=N/c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)cc2)C1 10.1021/jm00115a012
CHEMBL321223 108523 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 735 3 5 8 7.8 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N/C(S)=N/c3ccc4c(c3)C(=O)OC43c4ccc(O)cc4Oc4cc(O)ccc43)cc2)C1 10.1021/jm00115a012
6761 67457 17 None -5 18 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67457 17 None -5 18 Human 7.8 pKi = 7.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
44415701 79676 0 None 16 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 569 5 1 8 5.1 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
CHEMBL213110 79676 0 None 16 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 569 5 1 8 5.1 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
44415584 138165 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Br)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL377877 138165 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 523 2 1 5 5.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Br)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415601 140929 0 None 33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 481 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL384269 140929 0 None 33 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 481 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
156018764 177221 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 2 1 3 3.8 COc1cc2c(cc1O)C(c1ccccc1Br)CN(C)CC2 10.1016/j.bmcl.2020.127305
CHEMBL4643426 177221 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 2 1 3 3.8 COc1cc2c(cc1O)C(c1ccccc1Br)CN(C)CC2 10.1016/j.bmcl.2020.127305
9844271 130160 1 None 1 5 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL368324 130160 1 None 1 5 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9884087 14468 0 None -5 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 14468 0 None -5 3 Rat 7.8 pKi = 7.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
9844271 130160 1 None 1 5 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL368324 130160 1 None 1 5 Rat 7.8 pKi = 7.8 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9844271 130160 1 None 1 5 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL368324 130160 1 None 1 5 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 333 1 0 4 3.6 CN1CCN([C@@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
11716449 140684 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
CHEMBL382850 140684 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 304 1 1 1 4.2 CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm050846j
72699815 114698 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 349 3 1 4 3.9 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344467 114698 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 349 3 1 4 3.9 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
117773776 131937 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 3 1 5 3.9 Cc1cc(Sc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697599 131937 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 3 1 5 3.9 Cc1cc(Sc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
9817779 113934 0 None -2 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
CHEMBL333246 113934 0 None -2 3 Rat 6.8 pKi = 6.8 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm9706832
45269168 194256 0 None -10 4 Bovine 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL559399 194256 0 None -10 4 Bovine 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 410 4 1 6 2.3 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccc(F)cc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
122189390 122729 0 None -16 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613876 122729 0 None -16 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 469 6 0 8 3.4 O=Cc1cnn2ccc(-n3cc(CCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
10973768 107074 0 None -4073 10 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 107074 0 None -4073 10 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
681 1437 65 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -23 38 Bovine 5.8 pKi = 5.8 Binding
Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
10403608 77798 6 None -1584 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210405 77798 6 None -1584 6 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44412468 165377 0 None -616 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL425057 165377 0 None -616 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cnn(-c4ccccn4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
53317282 58290 0 None -173 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684131 58290 0 None -173 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
24949534 188927 0 None -2041 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
CHEMBL514074 188927 0 None -2041 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
10403608 77798 6 None -1584 6 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL210405 77798 6 None -1584 6 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
145979897 166053 0 None -158 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4280542 166053 0 None -158 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 480 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(I)cc1)CC2 10.1021/acsmedchemlett.8b00229
57400556 68968 0 None -2398 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928134 68968 0 None -2398 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 3.1 CCOCCOc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
10476504 33268 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
CHEMBL142020 33268 1 None -64 7 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1016/j.bmc.2017.04.036
10824155 56944 1 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL165022 56944 1 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 243 5 0 1 3.6 C#CC(C#C)=C1CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44436601 91511 0 None -1584 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL241424 91511 0 None -1584 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(C#Cc3ccccc3)cc2)CC1 10.1016/j.bmc.2007.08.038
15508238 4727 0 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
CHEMBL104092 4727 0 None -4 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 340 3 0 2 4.7 C(#Cc1cccn1C1CCN(Cc2ccccc2)CC1)c1ccccc1 10.1016/s0960-894x(99)00540-5
72544787 92698 0 None -501 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443008 92698 0 None -501 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 587 12 3 12 1.2 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOC4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4F)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
57400562 68976 0 None -16 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928247 68976 0 None -16 5 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(N2CCN(CCCCNC(=O)c3ccccc3)CC2)c(OC)c1 10.1016/j.bmc.2011.10.063
71449034 78014 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111526 78014 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
44319361 204007 0 None -7 4 Bovine 4.8 pKi = 4.8 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 204007 0 None -7 4 Bovine 4.8 pKi = 4.8 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
10200496 83180 0 None -295 5 Human 6.8 pKi = 6.8 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
CHEMBL2204343 83180 0 None -295 5 Human 6.8 pKi = 6.8 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 391 6 1 3 3.6 O=C(CCCN1CC[Si](O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm1013693
11653679 180609 1 None -24 11 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
CHEMBL476108 180609 1 None -24 11 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmc.2008.06.030
9872676 77826 0 None -4073 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77826 0 None -4073 17 Human 5.8 pKi = 5.8 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
11419055 128782 0 None -24 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 431 4 1 5 3.0 O=C1NCCN1CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL367087 128782 0 None -24 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 431 4 1 5 3.0 O=C1NCCN1CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
10335576 120418 5 None 2 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3ccccc3Sc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL356076 120418 5 None 2 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3ccccc3Sc3ncccc32)CC1 10.1021/jm00030a011
44278267 99800 0 None -53 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 368 6 0 2 4.6 O=C1c2ccccc2CN1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL28884 99800 0 None -53 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 368 6 0 2 4.6 O=C1c2ccccc2CN1CCCCN1CCC(c2ccc(Cl)cc2)C1 10.1016/s0960-894x(99)00201-2
16090821 81421 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
CHEMBL216439 81421 0 None -52 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 10.1021/jm060213k
46889212 7388 0 None -263 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccncc1 10.1016/j.bmcl.2010.02.106
CHEMBL1086958 7388 0 None -263 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccncc1 10.1016/j.bmcl.2010.02.106
13678338 100255 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.8 Oc1ccc(-c2c(O)c(O)c(Cl)c3c2CCNCC3)cc1 10.1021/jm00160a018
CHEMBL292611 100255 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.8 Oc1ccc(-c2c(O)c(O)c(Cl)c3c2CCNCC3)cc1 10.1021/jm00160a018
14198580 196285 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 301 3 0 2 4.1 COc1cc2c(cc1Cl)CCN(C)C2Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL573412 196285 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 301 3 0 2 4.1 COc1cc2c(cc1Cl)CCN(C)C2Cc1ccccc1 10.1016/j.bmc.2009.05.079
154725766 176071 1 None -1380 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4527244 176071 1 None -1380 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4598000 176071 1 None -1380 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
10546132 160708 0 None 9 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL41196 160708 0 None 9 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
44299852 196458 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 245 3 4 4 2.0 NCCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
CHEMBL57470 196458 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 245 3 4 4 2.0 NCCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
11346967 124907 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 3 3.4 O=C(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
CHEMBL364586 124907 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 3 3.4 O=C(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
11812345 16732 0 None -213 3 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1cc2ccccc2o1 10.1021/jm0211220
CHEMBL125193 16732 0 None -213 3 Rat 5.8 pKi = 5.8 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1cc2ccccc2o1 10.1021/jm0211220
15711860 13746 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1195937 13746 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL555619 13746 0 None 1 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
15069443 100502 0 None 3 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@H]21 10.1021/jm00128a038
CHEMBL294215 100502 0 None 3 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@H]21 10.1021/jm00128a038
154726922 175967 1 None -19 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442936 175967 1 None -19 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597157 175967 1 None -19 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 468 12 0 6 5.6 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
15696481 79256 0 None 21 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2115213 79256 0 None 21 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
11404156 65950 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 311 6 0 3 3.4 CC1CN(CCOc2ccccc2Cc2ccccc2)CCO1 10.1021/jm049720x
CHEMBL184724 65950 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 311 6 0 3 3.4 CC1CN(CCOc2ccccc2Cc2ccccc2)CCO1 10.1021/jm049720x
71722295 101994 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397381 101994 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040115 101994 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
145990190 166300 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4285528 166300 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
127035062 135928 0 None -58 19 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
CHEMBL3735756 135928 0 None -58 19 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membrane after 90 mins by scintillation counting method
ChEMBL 447 12 0 5 5.2 COc1ccc(CCN(CCCc2ccccc2)CCc2ccc3c(c2)OCO3)cc1OC 10.1039/C4MD00418C
135398737 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
38 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
722 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
CHEMBL42 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
DB00363 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm981094e
135398737 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
38 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
722 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
CHEMBL42 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
DB00363 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009890
24800688 155177 0 None -15 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 309 3 1 3 3.9 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL405345 155177 0 None -15 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 309 3 1 3 3.9 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
10498848 119547 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)cc2c1C(Cc1ccccc1O)N(C)CC2 10.1021/jm991034o
CHEMBL350471 119547 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 361 3 1 3 3.9 COc1cc(Br)cc2c1C(Cc1ccccc1O)N(C)CC2 10.1021/jm991034o
72708061 91767 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425372 91767 0 None -1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
44582461 181335 0 None 4 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 350 5 0 4 2.3 O=C1c2ccccc2CCN1CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477961 181335 0 None 4 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 350 5 0 4 2.3 O=C1c2ccccc2CCN1CCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
70692655 75721 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057456 75721 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
71109804 87078 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 nan
CHEMBL2334882 87078 0 None 12 3 Human 7.8 pKi = 7.8 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 nan
70692655 75721 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2057456 75721 0 None 8 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 371 4 2 6 2.6 COc1cc2c(cc1O)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
117772871 131959 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697621 131959 0 None - 1 Human 7.8 pKi = 7.8 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
74223831 128931 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 2 6 2.1 Cc1c(-c2ccc(Oc3nccc4n[nH]cc34)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3671308 128931 0 None - 1 Human 7.8 pKi = 7.8 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 349 3 2 6 2.1 Cc1c(-c2ccc(Oc3nccc4n[nH]cc34)cc2)n(C)c(=O)[nH]c1=O nan
15115518 8849 0 None -380 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL109787 8849 0 None -380 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
135398737 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
38 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
722 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
CHEMBL42 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
DB00363 944 89 None -83 91 Rat 6.8 pKi = 6.8 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm960084f
44447996 154965 0 None -44 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL404137 154965 0 None -44 2 Rat 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
145967572 164381 0 None -33 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4224763 164381 0 None -33 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 275 8 1 2 4.5 CCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
122167 12135 12 None -56 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Dopamine receptor D1In vitro binding affinity towards Dopamine receptor D1
ChEMBL 263 5 2 3 3.1 CCCN(CCC)C1CCc2c(ccc(O)c2O)C1 10.1021/jm0307786
CHEMBL11845 12135 12 None -56 2 Rat 6.8 pKi = 6.8 Binding
In vitro binding affinity towards Dopamine receptor D1In vitro binding affinity towards Dopamine receptor D1
ChEMBL 263 5 2 3 3.1 CCCN(CCC)C1CCc2c(ccc(O)c2O)C1 10.1021/jm0307786
44340302 9660 0 None -3 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 9660 0 None -3 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25139329 186520 0 None -11 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
CHEMBL491466 186520 0 None -11 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 514 10 0 4 7.6 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#Cc2ccccc2)CC1 10.1021/jm800895v
71583848 87303 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336892 87303 0 None -478 4 Bovine 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(N2CCN(Cc3cnn(-c4cc5ccc4CCc4ccc(cc4)CC5)c3)CC2)cc1 10.1016/j.bmc.2013.01.065
137636460 155579 0 None -120 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063282 155579 0 None -120 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 7 1 6 2.9 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
122189387 122726 0 None -45 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613873 122726 0 None -45 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 417 7 0 8 2.7 COc1ccccc1N1CCN(CCCc2cn(-c3ccn4nccc4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
44400594 133052 0 None -85 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL371165 133052 0 None -85 5 Pig 5.8 pKi = 5.8 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
240 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
2769 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
44279790 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
660 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL1729 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
CHEMBL560739 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
DB00604 931 39 None -19 25 Rat 5.8 pKi = 5.8 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
ChEMBL 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N 10.1021/jm00086a019
4420454 55966 6 None -41 5 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 55966 6 None -41 5 Bovine 4.8 pKi = 4.8 Binding
Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Binding Affinity was determined for decoupling of the ternary complex of Compound to Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
10454684 203097 0 None -5623 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7508 203097 0 None -5623 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 418 3 0 4 3.3 Ic1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44340186 9569 0 None -45 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
CHEMBL112831 9569 0 None -45 4 Bovine 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCCN(Cc2ccccc2)C1 10.1016/s0960-894x(03)00678-4
137640152 156212 0 None -10715 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4070604 156212 0 None -10715 5 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 631 15 3 10 4.0 CCCCn1cc(CCCOc2ccc(C(=O)NCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
44437897 152519 0 None -776 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL397592 152519 0 None -776 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 352 6 1 3 2.8 C=CCN1CCC[C@H]1CNC(=O)c1cc(Br)ccc1OC 10.1016/j.bmc.2007.07.017
90644059 111538 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 111538 0 None -22 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
25132869 102820 0 None -269 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
CHEMBL3084503 102820 0 None -269 6 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 400 3 2 2 5.5 O[C@]1(c2ccc(Cl)c(Cl)c2)C[C@@H]2CC[C@H](C1)N2Cc1c[nH]c2ccccc12 10.1021/jm800532x
154705296 175820 1 None -39 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4444691 175820 1 None -39 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595970 175820 1 None -39 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 6.9 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01835
154726793 175659 1 None -57 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4590966 175659 1 None -57 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594692 175659 1 None -57 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 454 11 0 6 5.2 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
45481839 196417 0 None -22 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 4 1 2 3.7 CCCCC1NCCc2cc(Cl)c(OC)cc21 10.1016/j.bmc.2009.05.079
CHEMBL574418 196417 0 None -22 2 Rat 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 253 4 1 2 3.7 CCCCC1NCCc2cc(Cl)c(OC)cc21 10.1016/j.bmc.2009.05.079
46227284 198033 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
CHEMBL593394 198033 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.5 COc1ccc2c(c1)CCN(C)Cc1ccccc1CC2 10.1016/j.bmc.2009.08.028
11351639 60200 0 None -93 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
CHEMBL175734 60200 0 None -93 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 459 6 1 4 5.3 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm900095y
44299993 101452 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL301003 101452 0 None - 1 Rat 5.8 pKi = 5.8 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
72708058 91763 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425368 91763 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
25256817 180844 0 None -169 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 445 6 0 3 5.0 O=C1c2ccccc2CCCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476394 180844 0 None -169 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 445 6 0 3 5.0 O=C1c2ccccc2CCCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
44582489 189208 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 3.9 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL516270 189208 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 417 5 0 3 3.9 O=C1c2ccccc2CCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
14198596 101173 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 101173 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
145969667 164413 0 None -30 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164413 0 None -30 6 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
14198596 101173 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00118a012
CHEMBL299056 101173 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00118a012
13678327 200369 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 329 8 3 4 4.1 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
CHEMBL60861 200369 0 None 1 2 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 329 8 3 4 4.1 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccc(O)cc1 10.1021/jm00160a018
11151583 128941 0 None -15 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 327 2 1 5 2.6 CN1CCN(C2=Cn3c(CO)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL367180 128941 0 None -15 3 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 327 2 1 5 2.6 CN1CCN(C2=Cn3c(CO)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
44415738 79484 0 None 22 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 1 1 4 6.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C(=O)Nc3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212384 79484 0 None 22 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 513 1 1 4 6.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(C(=O)Nc3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
135995891 201271 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62996 201271 0 None -30 4 Bovine 4.8 pKi = 4.8 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 413 4 1 5 4.1 Oc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
154726046 175737 1 None -446 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4442408 175737 1 None -446 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595266 175737 1 None -446 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
44582678 180992 0 None -12 10 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 180992 0 None -12 10 Human 5.8 pKi = 5.8 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
15696482 79149 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL2114209 79149 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
14198596 101173 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 101173 0 None 2 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
14198600 101421 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL300778 101421 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
14198601 100434 1 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
CHEMBL293828 100434 1 None 1 4 Human 6.8 pKi = 6.8 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
44582115 181093 0 None -154 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 6 0 3 4.6 O=C1c2ccccc2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477646 181093 0 None -154 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 6 0 3 4.6 O=C1c2ccccc2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
180 397 50 None -109 38 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 397 50 None -109 38 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 397 50 None -109 38 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 397 50 None -109 38 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 397 50 None -109 38 Human 6.8 pKi = 6.8 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
130907 193017 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL53294 193017 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
1704 3466 76 None -57 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
4331799 3466 76 None -57 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
CHEMBL1334465 3466 76 None -57 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 3 2 3 4.5 O=C(Nc1cc(C)nc2c1cc(F)cc2F)Nc1ccc(cc1)N(C)C 10.1016/j.bmcl.2013.06.057
23656545 146237 0 None -83 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 3 3.5 COc1cc2c3c(c1)-c1c(ccc(C)c1O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2007.05.057
CHEMBL392447 146237 0 None -83 3 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 1 3 3.5 COc1cc2c3c(c1)-c1c(ccc(C)c1O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2007.05.057
14198600 101421 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL300778 101421 2 None 3 2 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
1212 1632 45 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
204 1632 45 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
3372 1632 45 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
CHEMBL726 1632 45 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
DB00623 1632 45 None -51 65 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1016/j.bmcl.2008.09.012
14198601 100434 1 None -1 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
CHEMBL293828 100434 1 None -1 4 Rat 6.8 pKi = 6.8 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
13678309 193257 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 255 1 3 3 2.5 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2 10.1021/jm00160a018
CHEMBL54168 193257 1 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 255 1 3 3 2.5 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2 10.1021/jm00160a018
3036864 201066 16 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 201066 16 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 201066 16 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 201066 16 None -26 27 Bovine 7.8 pKi = 7.8 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid glandAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of calf parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
10084583 104299 3 None -33 6 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104299 3 None -33 6 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
5281878 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
5281881 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
948 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
968 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
CHEMBL42055 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
CHEMBL54661 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
DB00875 1630 33 None -34 16 Bovine 7.8 pKi = 7.8 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm950759z
44578927 189070 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 335 4 0 3 4.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CC)c1-3 10.1016/j.bmc.2008.08.056
CHEMBL515187 189070 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 335 4 0 3 4.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)CC)c1-3 10.1016/j.bmc.2008.08.056
11976 907 54 None -12 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
667467 907 54 None -12 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
CHEMBL908 907 54 None -12 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
DB01239 907 54 None -12 23 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1016/j.bmcl.2008.09.012
10684714 99846 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115372 99846 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL289283 99846 0 None 13 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
9796958 146045 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 146045 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 146045 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 146045 0 None 25 4 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10684715 160093 0 None 11 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL41132 160093 0 None 11 2 Rat 7.8 pKi = 7.8 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
11089340 12779 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 2 0 4 4.0 CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL118889 12779 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 2 0 4 4.0 CCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
17756101 98132 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL276778 98132 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1021/jm070388+
86764103 131915 7 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697578 131915 7 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
10457445 102718 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 470 14 4 6 5.0 CCCN(CCCCCCN1CCC[C@@H]1Cc1ccc(O)c(O)c1)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL308295 102718 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 470 14 4 6 5.0 CCCN(CCCCCCN1CCC[C@@H]1Cc1ccc(O)c(O)c1)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
10656804 116059 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL336366 116059 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2cc(O)ccc2[C@H]1c1ccccc1 10.1021/jm960318v
1621 2396 16 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
17 2396 16 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
5761 2396 16 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
CHEMBL263881 2396 16 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
DB04829 2396 16 None -112 44 Mouse 6.8 pKi = 6.8 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
ChEMBL 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm020153s
44276414 97179 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL27101 97179 0 None 12 2 Human 6.8 pKi = 6.8 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
45482169 196161 0 None -6 4 Pig 6.8 pKi = 6.8 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
CHEMBL572379 196161 0 None -6 4 Pig 6.8 pKi = 6.8 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 559 12 1 8 4.5 O=C(CCCc1cn(-c2ccc([N+](=O)[O-])cc2)nn1)NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmc.2009.06.041
135398737 944 89 None -44 91 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
38 944 89 None -44 91 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
722 944 89 None -44 91 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
CHEMBL42 944 89 None -44 91 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
DB00363 944 89 None -44 91 Human 6.8 pKi = 6.8 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9601720
44209472 69829 2 None -97 11 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940420 69829 2 None -97 11 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 315 6 0 4 2.8 Fc1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
90644228 111294 0 None -29 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287402 111294 0 None -29 5 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
11092112 205894 0 None -3162 9 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 205894 0 None -3162 9 Rat 5.8 pKi = 5.8 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
44403232 70732 0 None -112 5 Pig 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL195247 70732 0 None -112 5 Pig 5.8 pKi = 5.8 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 459 8 1 4 4.0 O=S(=O)(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
44436610 91517 0 None -234 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241436 91517 0 None -234 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
130907 193017 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL53294 193017 5 None -3311 4 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
52937680 60845 0 None -3235 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
CHEMBL1765632 60845 0 None -3235 4 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 466 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1Cc2cccn3ncc(c23)C1 10.1021/jm101639t
137659990 158684 0 None -3019 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4098859 158684 0 None -3019 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccn2ncc(/C=N\O)c2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
57393627 68965 0 None -199 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928131 68965 0 None -199 5 Pig 5.8 pKi = 5.8 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1101 42 2 17 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
11077918 204868 0 None -13 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
CHEMBL88937 204868 0 None -13 4 Bovine 4.8 pKi = 4.8 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccc4ccnn34)CC2)cc1 10.1021/jm015522j
46869265 16081 0 None -4 7 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
CHEMBL1224527 16081 0 None -4 7 Human 4.8 pKi = 4.8 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2010.07.052
73353534 90627 0 None -4168 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
CHEMBL2397477 90627 0 None -4168 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 549 18 1 7 5.4 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cnn(CCCC)n3)c(OC)c2)CC1 10.1021/jm400520c
71733932 90621 0 None -24547 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
CHEMBL2397389 90621 0 None -24547 6 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm501889t
23642427 91367 0 None -38904 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL241169 91367 0 None -38904 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 430 7 1 4 2.7 C=CCN1CCC[C@H]1CNC(=O)c1cc(I)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
24824061 97448 0 None -25 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
CHEMBL272396 97448 0 None -25 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
10021692 145849 12 None -23442 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
CHEMBL392158 145849 12 None -23442 4 Pig 4.8 pKi = 4.8 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 364 10 1 4 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)cc(OC)c1OC 10.1016/j.bmc.2007.07.017
132060743 161686 0 None -7 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 161686 0 None -7 13 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
145969667 164413 0 None -30 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225278 164413 0 None -30 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 289 9 1 2 4.9 CCCCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
228 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
33 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
6005 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
CHEMBL53 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
DB00714 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm991034o
11559090 155021 0 None -60 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
CHEMBL404352 155021 0 None -60 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH-23390 from human cloned dopamine D1 receptor
ChEMBL 335 1 2 3 3.8 CC1(c2cccc(O)c2)C(=O)Nc2cc(Cl)cc(Cl)c2C1=O 10.1016/j.bmcl.2007.11.045
44567689 183227 0 None -7 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 309 3 1 3 3.9 CCCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
CHEMBL480525 183227 0 None -7 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 309 3 1 3 3.9 CCCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
145979855 165975 0 None -83 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4279136 165975 0 None -83 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 405 7 2 5 3.5 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccnc3ccccc13)CC2 10.1021/acsmedchemlett.8b00229
72708058 91763 0 None 1 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425368 91763 0 None 1 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 329 2 0 3 4.0 COc1ccc2c(c1)CC1c3cc(OC)c(Cl)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
70690497 75710 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057438 75710 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.bmc.2012.05.057
70690497 75710 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL2057438 75710 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 1 6 2.6 COc1cc(OC)c2c(c1CO)C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
681 1437 65 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
940 1437 65 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
947 1437 65 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
CHEMBL59 1437 65 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
DB00988 1437 65 None -154 38 Human 4.7 pKi = 4.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9800292
13903144 99624 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 285 1 0 1 4.2 Fc1ccc([C@@H]2CN3CCC[C@@H]3c3cc(F)ccc32)cc1 10.1021/jm00391a028
CHEMBL1743798 99624 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 285 1 0 1 4.2 Fc1ccc([C@@H]2CN3CCC[C@@H]3c3cc(F)ccc32)cc1 10.1021/jm00391a028
CHEMBL287332 99624 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 285 1 0 1 4.2 Fc1ccc([C@@H]2CN3CCC[C@@H]3c3cc(F)ccc32)cc1 10.1021/jm00391a028
46227317 198479 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
CHEMBL596448 198479 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.4 COc1ccc2c(c1)CCN1Cc3ccccc3CC21 10.1016/j.bmc.2009.08.028
45379377 7376 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
CHEMBL1086790 7376 0 None -1 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3cccc4[nH]cc(c34)C21 10.1021/jm901291r
10107367 101961 1 None -7 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL303993 101961 1 None -7 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
11777127 25606 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL135318 25606 0 None 1 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
117773975 131912 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 367 4 1 6 2.9 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1C nan
CHEMBL3697575 131912 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 367 4 1 6 2.9 COc1cc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)ncc1C nan
4011 81996 43 None -64 23 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
CHEMBL21731 81996 43 None -64 23 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 nan
71722293 102002 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL2397380 102002 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
CHEMBL3040164 102002 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2013.05.014
135398737 944 89 None -44 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
38 944 89 None -44 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
722 944 89 None -44 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
CHEMBL42 944 89 None -44 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
DB00363 944 89 None -44 91 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C5MD00258C
60165416 74946 0 None -478 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL2037431 74946 0 None -478 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 0 4 5.1 Clc1ccc(N2CCN(CCCCc3nc4ccccc4s3)CC2)cc1 10.1016/j.bmc.2014.04.026
44439944 151337 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2c(c1)CCN(C)CCc1c([nH]c3ccccc13)C2 10.1016/j.bmcl.2006.11.093
CHEMBL396561 151337 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 320 1 1 2 3.8 COc1ccc2c(c1)CCN(C)CCc1c([nH]c3ccccc13)C2 10.1016/j.bmcl.2006.11.093
49782600 17271 0 None -4 5 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257689 17271 0 None -4 5 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 1 3 4.4 Cc1ccc(C)c(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
127031397 138201 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 397 7 1 5 4.6 CCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3780140 138201 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 397 7 1 5 4.6 CCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
44401106 123808 0 None -29 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL363581 123808 0 None -29 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
9796255 128526 0 None -17 8 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL367045 128526 0 None -17 8 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm0309811
9796255 128526 0 None -17 8 Rat 7.7 pKi = 7.7 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm049629t
CHEMBL367045 128526 0 None -17 8 Rat 7.7 pKi = 7.7 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 297 1 0 4 3.2 CN1CCN(C2=Cn3cccc3Sc3ccccc32)CC1 10.1021/jm049629t
10894826 10386 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL116542 10386 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
9884087 14468 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 14468 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
71733935 90552 0 None -457 6 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2396663 90552 0 None -457 6 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
1242 3556 23 None -5 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2008.09.049
935 3556 23 None -5 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL286080 3556 23 None -5 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2008.09.049
25110707 12499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 2 3 3 4.7 Oc1cc2c(c(-c3ccc(Cl)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186974 12499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 2 3 3 4.7 Oc1cc2c(c(-c3ccc(Cl)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL485036 12499 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 365 2 3 3 4.7 Oc1cc2c(c(-c3ccc(Cl)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
10594054 31198 1 None -562 4 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL140258 31198 1 None -562 4 Bovine 5.7 pKi = 5.7 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2cc(CN3CCN(c4ccccc4Cl)CC3)[nH]c2c1 10.1021/jm0009989
14198600 101421 2 None 3 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL300778 101421 2 None 3 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 301 3 1 2 4.4 CCCN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
54583898 61282 0 None -3801 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771114 61282 0 None -3801 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 417 7 0 4 3.3 C#Cc1ccc2c(c1)CCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44412482 77797 0 None -4365 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210404 77797 0 None -4365 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cnn(-c3ccccn3)c2)CC1 10.1016/j.bmcl.2006.02.075
17475863 168219 3 None -660 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL437490 168219 3 None -660 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
53317208 58247 0 None -234 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 634 14 0 8 6.4 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCn2cc(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684029 58247 0 None -234 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 634 14 0 8 6.4 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCn2cc(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
24854106 160514 1 None -95 8 Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
CHEMBL411663 160514 1 None -95 8 Human 5.7 pKi = 5.7 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 367 6 1 3 3.9 O=C1Nc2ccc(F)cc2C1CCCCN1CCN(c2ccccc2)CC1 10.1021/jm070279v
10960333 205256 0 None -2 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL91362 205256 0 None -2 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 398 5 0 6 3.5 CCOC(=O)c1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
44339953 109212 0 None -707 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 109212 0 None -707 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
21559988 112928 2 None -30 4 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318852 112928 2 None -30 4 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 389 5 1 3 4.0 O=C(CCC(=O)N1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2014.06.079
9797495 68662 0 None -17378 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
CHEMBL1923292 68662 0 None -17378 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 328 3 0 4 2.9 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cc1 10.1021/jm200762g
44381279 58431 0 None -41 4 Bovine 4.7 pKi = 4.7 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168571 58431 0 None -41 4 Bovine 4.7 pKi = 4.7 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44415837 139009 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 3 1 5 5.9 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL379593 139009 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 3 1 5 5.9 CC(C)N1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
154724369 176115 1 None -51 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4584372 176115 1 None -51 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4598389 176115 1 None -51 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 484 12 0 6 6.1 CCCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
681 1437 65 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
940 1437 65 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
947 1437 65 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
CHEMBL59 1437 65 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
DB00988 1437 65 None -154 38 Human 6.7 pKi = 6.7 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00170a025
6603800 3492 9 None 1 2 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2c([C@@H](C1)c1ccccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
956 3492 9 None 1 2 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2c([C@@H](C1)c1ccccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
CHEMBL63321 3492 9 None 1 2 Human 6.7 pKi = 6.7 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 287 1 1 2 3.7 CN1CCc2c([C@@H](C1)c1ccccc1)cc(c(c2)Cl)O 10.1021/jm00081a010
5281148 202211 44 None 5 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 260 8 2 2 2.8 C=C[C@@H](O)C#CC#C[C@@H](O)/C=C\CCCCCCC 10.1016/j.bmc.2007.12.021
CHEMBL69018 202211 44 None 5 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from rat HA-tagged D1 dopamine receptor expressed in CHO cells
ChEMBL 260 8 2 2 2.8 C=C[C@@H](O)C#CC#C[C@@H](O)/C=C\CCCCCCC 10.1016/j.bmc.2007.12.021
14198585 100334 1 None 1 4 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 100334 1 None 1 4 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
44582705 186413 0 None -12 13 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186413 0 None -12 13 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
2351 3234 60 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3234 60 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3234 60 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3234 60 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3234 60 None -16 21 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
12488 1627 51 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
941361 1627 51 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
CHEMBL30008 1627 51 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
DB04841 1627 51 None -19 23 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F nan
10338282 34464 1 None -2 6 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143022 34464 1 None -2 6 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 355 4 0 4 3.8 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2occc21 10.1021/jm0009890
13678325 101450 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 313 8 2 3 4.4 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
CHEMBL300995 101450 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 313 8 2 3 4.4 CCCN(CCC)CCc1ccc(O)c(O)c1-c1ccccc1 10.1021/jm00160a018
6937303 201517 6 None -43 4 Bovine 4.7 pKi = 4.7 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64376 201517 6 None -43 4 Bovine 4.7 pKi = 4.7 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 335 4 0 4 4.1 c1ccc(-c2nc(CN3CCN(c4ccccc4)CC3)cs2)cc1 10.1016/s0960-894x(00)00405-4
44278364 98961 0 None -169 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 334 6 0 2 3.9 O=C1c2ccccc2CN1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL282822 98961 0 None -169 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 334 6 0 2 3.9 O=C1c2ccccc2CN1CCCCN1CCC(c2ccccc2)C1 10.1016/s0960-894x(99)00201-2
68950 127017 10 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 8 0 2 4.0 CCN(CC)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL366265 127017 10 None 1 3 Human 5.7 pKi = 5.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 8 0 2 4.0 CCN(CC)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
191 399 92 None -26 28 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
201 399 92 None -26 28 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
2170 399 92 None -26 28 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
CHEMBL1113 399 92 None -26 28 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
DB00543 399 92 None -26 28 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 nan
242 467 117 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
34 467 117 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
60795 467 117 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
CHEMBL1112 467 117 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
DB01238 467 117 None -74 51 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm800689g
46931072 200360 0 None -8 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL608530 200360 0 None -8 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
15711870 12847 0 None 1 3 Goldfish 6.7 pKi = 6.7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1189332 12847 0 None 1 3 Goldfish 6.7 pKi = 6.7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL538520 12847 0 None 1 3 Goldfish 6.7 pKi = 6.7 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
164610779 184500 0 None -81 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 558 7 2 5 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(I)c(OC)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4855891 184500 0 None -81 3 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 558 7 2 5 4.5 COc1cc2c(cc1O)CN(Cc1ccccc1CNC(=O)c1ccc(I)c(OC)c1)CC2 10.1016/j.bmcl.2021.128047
10046389 61087 0 None -1122 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 61087 0 None -1122 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
15136 107624 2 None -154 2 Rat 5.7 pKi = 5.7 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL319557 107624 2 None -154 2 Rat 5.7 pKi = 5.7 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
44432812 87140 0 None -5 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 3 2 3 3.4 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
CHEMBL233567 87140 0 None -5 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 3 2 3 3.4 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(CO)c(O)c1-3 10.1016/j.bmcl.2007.05.057
154703541 175725 1 None -85 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4541924 175725 1 None -85 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595195 175725 1 None -85 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 464 11 1 3 6.1 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
11186895 87079 21 None -5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmcl.2017.01.090
CHEMBL2334885 87079 21 None -5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmcl.2017.01.090
1353 1880 85 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
3559 1880 85 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
86 1880 85 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
CHEMBL54 1880 85 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
DB00502 1880 85 None -74 85 Rat 6.7 pKi = 6.7 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0009890
46231589 199616 0 None 999 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNc3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
CHEMBL604108 199616 0 None 999 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccc(CNc3ccccc3)cc2)C1 10.1016/j.bmcl.2009.12.100
37459 735 10 None -10 24 Human 8.7 pKi = 8.7 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127053
62 735 10 None -10 24 Human 8.7 pKi = 8.7 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127053
CHEMBL8514 735 10 None -10 24 Human 8.7 pKi = 8.7 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127053
142405827 179285 0 None -14 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 421 2 1 4 6.1 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(OC(F)(F)F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4745489 179285 0 None -14 3 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 421 2 1 4 6.1 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccc(OC(F)(F)F)cc32)CCN1C 10.1016/j.bmcl.2020.127563
142405818 180277 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 367 2 1 4 5.2 COc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4757297 180277 0 None 34 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 367 2 1 4 5.2 COc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
15937728 19795 0 None 288 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C(C2C=CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL130328 19795 0 None 288 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C(C2C=CCCC2)C1 10.1016/S0960-894X(00)80155-9
11623343 140311 1 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
CHEMBL381936 140311 1 None -2 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 283 0 2 3 2.7 CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 10.1021/jm051237e
44415702 139369 0 None 87 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 2 1 5 5.4 Cc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL379942 139369 0 None 87 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 2 1 5 5.4 Cc1ccccc1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
16665071 92969 0 None -8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245764 92969 0 None -8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 334 1 0 3 3.8 COc1ccc2c(c1)c1c(n2C)Cc2ccccc2CCN(C)CC1 10.1016/j.bmcl.2006.11.093
10004036 94785 0 None 33 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL256075 94785 0 None 33 2 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 453 2 2 5 3.5 COc1cc2c(cc1O)C[C@H]1c3c(c(I)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
71563084 87143 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335736 87143 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
46231847 198890 0 None 3 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL599116 198890 0 None 3 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 343 1 2 3 3.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(CO)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
6603950 201633 9 None -6 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64875 201633 9 None -6 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
6603950 201633 9 None -6 9 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL64875 201633 9 None -6 9 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
16090814 81169 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL216258 81169 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2008.04.081
6603950 201633 9 None -6 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64875 201633 9 None -6 9 Rat 8.7 pKi = 8.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
10935201 20684 0 None 758 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.1 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL131054 20684 0 None 758 2 Rat 8.7 pKi = 8.7 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 291 1 1 2 4.1 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCCC2)C1 10.1016/S0960-894X(00)80155-9
16090814 81169 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
CHEMBL216258 81169 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cellsDisplacement of [3H]SCH 23390 from human D1 dopamine receptor expressed in HEK293 cells
ChEMBL 304 0 1 1 4.2 CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/jm060213k
134151764 152610 0 None 31 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 433 4 2 5 4.3 CCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3976659 152610 0 None 31 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 433 4 2 5 4.3 CCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
1238 201484 21 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64249 201484 21 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
15115523 108382 1 None 691 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 346 1 2 3 3.4 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N)cc2)C1 10.1021/jm00115a012
CHEMBL321042 108382 1 None 691 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 346 1 2 3 3.4 CN1CCc2cc(Br)c(O)cc2C(c2ccc(N)cc2)C1 10.1021/jm00115a012
11315462 198782 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)C4CC4)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL598516 198782 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(NC(=O)C4CC4)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
46231833 199227 0 None 218 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 384 2 2 3 4.3 CCC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL601634 199227 0 None 218 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 384 2 2 3 4.3 CCC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
142405825 179259 0 None -24 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4745124 179259 0 None -24 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.5 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
134135947 143856 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 5 2 5 4.7 CCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3905947 143856 0 None 46 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 5 2 5 4.7 CCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
37459 735 10 None -10 24 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2016.03.037
62 735 10 None -10 24 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2016.03.037
CHEMBL8514 735 10 None -10 24 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2016.03.037
46231782 198819 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL598730 198819 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 371 1 1 4 3.8 COC(=O)c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
46232064 199663 0 None 707 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 473 2 1 3 6.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(OC(F)(F)F)c4)c3CC[C@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604383 199663 0 None 707 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 473 2 1 3 6.5 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(-c4cccc(OC(F)(F)F)c4)c3CC[C@H]21 10.1016/j.bmcl.2009.12.094
1238 201484 21 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL64249 201484 21 None -5 16 Rat 8.6 pKi = 8.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
10662054 83991 0 None 151 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114444 83991 0 None 151 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219803 83991 0 None 151 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
146266 100231 7 None 2 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00118a012
CHEMBL292418 100231 7 None 2 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00118a012
CHEMBL540857 100231 7 None 2 4 Rat 8.6 pKi = 8.6 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00118a012
46231772 199624 0 None 371 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL604132 199624 0 None 371 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 399 2 3 3 4.1 CCNC(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
162676091 182742 0 None 512 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 401 2 1 4 5.7 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(OC(F)(F)F)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4797375 182742 0 None 512 2 Human 8.6 pKi = 8.6 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 401 2 1 4 5.7 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(OC(F)(F)F)ccc1N2 10.1016/j.bmcl.2020.127563
75202022 170243 2 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL4453318 170243 2 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 363 3 1 6 3.3 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
10537185 25481 0 None -12 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135224 25481 0 None -12 2 Rat 8.6 pKi = 8.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
44415672 79764 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213492 79764 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(F)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
70690500 75720 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.12.016
CHEMBL2057455 75720 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.12.016
70690500 75720 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057455 75720 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.bmc.2012.05.057
70690500 75720 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 75720 0 None - 1 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
44415689 138579 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378669 138579 0 None -2 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 494 2 2 6 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
46231846 199654 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604316 199654 0 None 1 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 341 1 1 3 3.8 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
17755867 85682 1 None -1 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL231070 85682 1 None -1 6 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
9993922 59651 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 282 1 0 2 3.5 CN1CCc2cccc3c2C(C1)CN3c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
CHEMBL173315 59651 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 282 1 0 2 3.5 CN1CCc2cccc3c2C(C1)CN3c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
46231768 197799 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL591685 197799 0 None 2 3 Human 8.6 pKi = 8.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
11439190 199620 0 None 31 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL604127 199620 0 None 31 4 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 338 0 1 3 3.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C#N)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
37461 16953 10 None -3 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/j.bmcl.2021.128047
CHEMBL1255588 16953 10 None -3 8 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1016/j.bmcl.2021.128047
44268688 166022 0 None 37 2 Rat 8.5 pKi = 8.5 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
CHEMBL427996 166022 0 None 37 2 Rat 8.5 pKi = 8.5 Binding
Compound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brainCompound was evaluated for affinity towards dopamine D1-like receptor in homogenate of caudate putamen tissue from rat brain
ChEMBL None None None None 10.1016/s0960-894x(00)00185-2
4350931 168747 39 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
CHEMBL441618 168747 39 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
4350931 168747 39 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
CHEMBL441618 168747 39 None -63 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 10.1021/acs.jmedchem.1c01327
1353 1880 85 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
3559 1880 85 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
86 1880 85 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
CHEMBL54 1880 85 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
DB00502 1880 85 None -74 85 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/s0960-894x(98)00138-3
44331310 106882 1 None 25 3 Human 7.7 pKi = 7.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9800292
CHEMBL317741 106882 1 None 25 3 Human 7.7 pKi = 7.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1 10.1021/jm9800292
44415649 137896 0 None 162 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
CHEMBL377420 137896 0 None 162 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
135398745 2869 108 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
47 2869 108 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
CHEMBL715 2869 108 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
DB00334 2869 108 None -23 65 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm100294b
10894826 10386 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
CHEMBL116542 10386 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 407 3 1 5 3.1 OCCN1CCN(C2Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm010982y
10519435 170903 0 None 87 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL446350 170903 0 None 87 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10015045 13541 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00004a011
CHEMBL119455 13541 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00004a011
10015045 13541 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960188q
CHEMBL119455 13541 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960188q
10015045 13541 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
CHEMBL119455 13541 1 None -2 6 Rat 7.7 pKi = 7.7 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm960189i
16103 202932 37 None -2 4 Rat 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
CHEMBL73538 202932 37 None -2 4 Rat 6.7 pKi = 6.7 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 292 0 1 4 3.1 CN1CCN(C2=Nc3ccccc3Nc3ccccc32)CC1 10.1021/jm00043a008
155515982 169443 0 None -794 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4442460 169443 0 None -794 17 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 473 10 2 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccccc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
56833464 68054 0 None -99 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916720 68054 0 None -99 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1138 38 2 16 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
14378574 108100 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
CHEMBL320397 108100 0 None -7 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(O)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
57390116 68956 0 None -323 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928122 68956 0 None -323 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
118709175 112924 0 None -107 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318848 112924 0 None -107 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 474 10 0 5 4.9 CN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10378194 196088 0 None -338 6 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL57176 196088 0 None -338 6 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 265 3 1 2 2.3 C#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
10862425 116133 0 None -467 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
CHEMBL336930 116133 0 None -467 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc3ccnn3c2)CC1 10.1021/jm025558r
10613676 13744 0 None -165 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1021/jm060959i
CHEMBL119593 13744 0 None -165 4 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1021/jm060959i
10092819 16594 0 None -1412 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL124444 16594 0 None -1412 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
52947756 16988 0 None -478 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256170 16988 0 None -478 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 567 6 0 2 8.3 O=C(CCCN1CCC(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
44319368 105584 0 None -7 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 105584 0 None -7 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
44319369 204105 0 None -11 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 204105 0 None -11 4 Bovine 5.7 pKi = 5.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
44380802 161142 0 None -131 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL413343 161142 0 None -131 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 401 7 2 4 3.9 CNc1cc(OC)c(C(=O)NC[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(99)00086-4
6469693 79545 17 None -7079 6 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
CHEMBL212631 79545 17 None -7079 6 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 322 4 0 5 2.7 COc1ccccc1N1CCN(Cc2cn3ccccc3n2)CC1 10.1021/jm060166w
44319369 204105 0 None -11 4 Bovine 4.7 pKi = 4.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
CHEMBL83306 204105 0 None -11 4 Bovine 4.7 pKi = 4.7 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 335 4 0 4 3.0 C[C@@H]1OC(c2ccccc2)=N[C@H]1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(01)00484-x
2247 502 77 None -61 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 502 77 None -61 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 502 77 None -61 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 502 77 None -61 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 502 77 None -61 41 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
24949857 181185 0 None -7413 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
CHEMBL477765 181185 0 None -7413 3 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 10.1021/jm800176x
53318500 58242 0 None -57 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 630 10 0 7 6.9 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684024 58242 0 None -57 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 630 10 0 7 6.9 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
2993172 126646 3 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
CHEMBL365697 126646 3 None 1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 0 3 3.0 c1ccc(Cc2ccccc2OCCN2CCOCC2)cc1 10.1021/jm049720x
134551 355 25 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 355 25 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 355 25 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 355 25 None -28 21 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
2105 3005 34 None -537 33 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
47811 3005 34 None -537 33 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
48 3005 34 None -537 33 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
CHEMBL531 3005 34 None -537 33 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
DB01186 3005 34 None -537 33 Human 5.7 pKi = 5.7 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1021/jm9800292
25212275 173849 0 None -4897 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL455288 173849 0 None -4897 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
25212276 189473 0 None -575 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517244 189473 0 None -575 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
135446209 9494 53 None -22 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 298 0 2 5 3.1 Cc1cc2c(s1)Nc1ccccc1N=C2N1CCNCC1 10.1016/S0960-894X(96)00567-7
CHEMBL1125 9494 53 None -22 3 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 298 0 2 5 3.1 Cc1cc2c(s1)Nc1ccccc1N=C2N1CCNCC1 10.1016/S0960-894X(96)00567-7
71061709 148995 0 None -14 12 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3946540 148995 0 None -14 12 Mouse 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 372 6 0 4 3.5 Clc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
44582113 181053 0 None -169 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 364 6 0 4 2.7 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477434 181053 0 None -169 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 364 6 0 4 2.7 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
10474964 129949 0 None -8511 7 Bovine 5.7 pKi = 5.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 129949 0 None -8511 7 Bovine 5.7 pKi = 5.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 129949 0 None -8511 7 Bovine 5.7 pKi = 5.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
5353853 17803 41 None -19 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9556529 17803 41 None -19 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1262 17803 41 None -19 15 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
127262 13369 8 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL1193274 13369 8 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
46227325 198443 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
CHEMBL596179 198443 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 1 2 3.4 CN1CCCc2cc(O)ccc2Cc2ccccc2C1 10.1016/j.bmc.2009.08.028
71474079 142732 0 None - 1 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3896731 142732 0 None - 1 Human 6.7 pKi = 6.7 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 307 0 0 3 3.7 Cc1ccc(C)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
10550785 162880 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 433 4 1 2 5.9 Oc1cc2c(cc1Br)CCN(C/C=C/c1ccccc1)CC2c1ccccc1 10.1021/jm960143p
CHEMBL419759 162880 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 433 4 1 2 5.9 Oc1cc2c(cc1Br)CCN(C/C=C/c1ccccc1)CC2c1ccccc1 10.1021/jm960143p
53359025 62024 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
CHEMBL1779058 62024 0 None -2 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 339 5 1 3 2.5 O=C(CCCN1C2C3C4CC5C6C4C2C6C1(O)C53)c1ccc(F)cc1 10.1016/j.bmcl.2011.04.098
6603703 206 7 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
9637 206 7 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
CHEMBL291143 206 7 None -1 5 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm00018a002
2389 3279 114 None -467 67 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
5073 3279 114 None -467 67 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
96 3279 114 None -467 67 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
CHEMBL85 3279 114 None -467 67 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
DB00734 3279 114 None -467 67 Human 7.7 pKi = 7.7 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm0002432
86764100 131955 22 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697617 131955 22 None - 1 Human 7.7 pKi = 7.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
6603820 95330 13 None -2 13 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
CHEMBL25856 95330 13 None -2 13 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm0604979
135398737 944 89 None -44 91 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
38 944 89 None -44 91 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
722 944 89 None -44 91 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
CHEMBL42 944 89 None -44 91 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
DB00363 944 89 None -44 91 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2009.09.041
75201901 165872 14 None -1 24 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165872 14 None -1 24 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
17756101 98132 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL276778 98132 1 None -5 6 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCN(C)CCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
10903748 78067 0 None -11 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL2111781 78067 0 None -11 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
2435 3533 78 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
60149 3533 78 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
98 3533 78 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
CHEMBL12713 3533 78 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
DB06144 3533 78 None -72 48 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm030480f
228 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
33 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
6005 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
CHEMBL53 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
DB00714 441 26 None -30 24 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
53364153 63510 0 None -38 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803023 63510 0 None -38 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 929 25 0 16 7.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCCCCCCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
135398737 944 89 None -83 91 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
38 944 89 None -83 91 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
722 944 89 None -83 91 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
CHEMBL42 944 89 None -83 91 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
DB00363 944 89 None -83 91 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm100294b
52945819 17371 0 None -14 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258037 17371 0 None -14 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 354 6 0 3 4.2 Cc1ccc(C)c(N2CCN(CCCC(=O)c3ccc(F)cc3)CC2)c1 10.1021/jm100899z
127047996 139116 0 None -46 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797758 139116 0 None -46 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 303 8 3 5 2.3 COc1ccccc1OCCNCCc1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
137636351 155332 0 None -602 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4060403 155332 0 None -602 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 459 7 1 6 4.0 O=Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
25072002 155573 0 None -1047 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 155573 0 None -1047 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
122189388 122727 0 None -40 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
CHEMBL3613874 122727 0 None -40 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 483 7 0 8 3.8 O=Cc1cnn2ccc(-n3cc(CCCN4CCN(c5cccc(Cl)c5Cl)CC4)nn3)cc12 10.1016/j.bmc.2015.07.050
44300865 200310 0 None -173 7 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL60815 200310 0 None -173 7 Bovine 5.7 pKi = 5.7 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/s0960-894x(02)00316-5
44340302 9660 0 None -3 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL113471 9660 0 None -3 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 466 7 1 3 5.3 COc1c(C(=O)NCC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340376 110157 0 None -24 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 110157 0 None -24 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
54581963 61272 0 None -7762 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
CHEMBL1771105 61272 0 None -7762 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 437 8 0 5 3.7 COc1ccc2c(c1)CCCN(CCCCN1CCN(c3ccccc3OC)CC1)C2=O 10.1016/j.bmcl.2010.12.083
44300865 200310 0 None -173 7 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL60815 200310 0 None -173 7 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 317 4 1 2 4.0 c1ccc(-c2c[nH]c(CN3CCN(c4ccccc4)CC3)c2)cc1 10.1016/j.bmcl.2006.02.075
9980998 30819 0 None -3981 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL139926 30819 0 None -3981 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL2112911 30819 0 None -3981 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
45273442 194777 0 None -100 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL563078 194777 0 None -100 4 Bovine 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 403 3 0 5 4.3 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44567594 172064 0 None -34 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 339 4 2 4 4.0 CCCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL449461 172064 0 None -34 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 339 4 2 4 4.0 CCCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
49783040 17508 0 None -446 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
CHEMBL1258494 17508 0 None -446 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 395 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cc(C)ccc2C)CC1 10.1021/jm100899z
137660837 158534 0 None -3019 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158534 0 None -3019 5 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
11154555 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
5037 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
7671 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL2028019 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL3085826 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB06016 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
11154555 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
5037 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
7671 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL2028019 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
CHEMBL3085826 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
DB06016 788 57 None -1445 12 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.04.036
15723715 13303 0 None - 1 Human 5.7 pKi = 5.7 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 337 1 2 3 4.0 CN1CCc2c(Cl)c(O)c(O)c(Cl)c2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL1192815 13303 0 None - 1 Human 5.7 pKi = 5.7 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 337 1 2 3 4.0 CN1CCc2c(Cl)c(O)c(O)c(Cl)c2C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL544118 13303 0 None - 1 Human 5.7 pKi = 5.7 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 337 1 2 3 4.0 CN1CCc2c(Cl)c(O)c(O)c(Cl)c2C(c2ccccc2)C1 10.1021/jm00116a004
44316315 203808 0 None -1318 5 Bovine 4.7 pKi = 4.7 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL80845 203808 0 None -1318 5 Bovine 4.7 pKi = 4.7 Binding
Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390Binding affinity of compound measured against Dopamine receptor D1 from bovine striatal membranes using radioligand [3H]-SCH- 23390
ChEMBL 215 2 0 3 2.1 CCCN1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
44264622 96695 5 None -72 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL267853 96695 5 None -72 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 327 3 0 5 2.7 Clc1ccc(N2CCN(Cc3cnc4ncccn34)CC2)cc1 10.1016/s0960-894x(98)00692-1
44412268 77964 8 None -2089 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL211026 77964 8 None -2089 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 319 4 0 5 2.6 c1ccc(N2CCN(Cc3cn(-c4ccccc4)nn3)CC2)cc1 10.1016/j.bmcl.2006.02.075
72544789 92700 0 None -912 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443010 92700 0 None -912 5 Pig 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 363 9 0 7 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
45379515 7375 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3[nH]c4ccccc4c3C21 10.1021/jm901291r
CHEMBL1086789 7375 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 274 0 1 1 3.7 c1ccc2c(c1)CCN1CCc3[nH]c4ccccc4c3C21 10.1021/jm901291r
44448027 154491 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 481 4 0 5 4.1 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL401567 154491 0 None 2 2 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 481 4 0 5 4.1 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
12301195 198034 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.2 COc1ccc2c(c1)CCN1CCc3ccccc3C21 10.1016/j.bmc.2009.08.028
CHEMBL593395 198034 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 265 1 0 2 3.2 COc1ccc2c(c1)CCN1CCc3ccccc3C21 10.1016/j.bmc.2009.08.028
9817779 113934 0 None -2 3 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL333246 113934 0 None -2 3 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
10085633 119491 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 290 4 1 3 2.4 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCOCC1)CC2 10.1016/0960-894X(95)00076-6
CHEMBL349997 119491 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 290 4 1 3 2.4 CCc1c(C)[nH]c2c1C(=O)C(CCN1CCOCC1)CC2 10.1016/0960-894X(95)00076-6
15654855 102190 0 None 4 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3cc(Cl)ccc32)CC1 10.1021/jm00067a009
CHEMBL304493 102190 0 None 4 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3cc(Cl)ccc32)CC1 10.1021/jm00067a009
2337 3205 72 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
50 3205 72 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
5002 3205 72 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
CHEMBL716 3205 72 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
DB01224 3205 72 None -53 62 Human 6.7 pKi = 6.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 nan
9927411 201364 0 None -89 4 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL63576 201364 0 None -89 4 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 327 0 1 5 3.1 CN1CCN(C2=Nc3cccnc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL4566600 212261 0 None -1 6 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 nan
CHEMBL4745071 212261 0 None -1 6 Human 5.7 pKi = 5.7 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000337aCl DRD1
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 nan
112500026 131940 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697602 131940 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 0 5 4.1 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)ncc(=O)n1C nan
118711262 113458 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1cccc(-c2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
CHEMBL3325913 113458 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1cccc(-c2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
9817779 113934 0 None -2 3 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
CHEMBL333246 113934 0 None -2 3 Rat 6.7 pKi = 6.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 299 1 0 4 2.9 CN1CCN(C2Cn3cccc3Sc3ccccc32)CC1 10.1021/jm010982y
168290235 192366 0 None -1513 20 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5201074 192366 0 None -1513 20 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222491 192366 0 None -1513 20 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 315 6 4 3 1.1 C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 10.1021/acs.jmedchem.1c00692
9998826 119971 0 None -33113 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
CHEMBL354210 119971 0 None -33113 5 Bovine 4.7 pKi = 4.7 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 363 5 1 3 3.1 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccccc1 10.1021/jm950759z
2389 3279 114 None -331 67 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
5073 3279 114 None -331 67 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
96 3279 114 None -331 67 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
CHEMBL85 3279 114 None -331 67 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
DB00734 3279 114 None -331 67 Rat 7.7 pKi = 7.7 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/s0960-894x(98)00138-3
9884087 14468 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 14468 0 None -5 3 Rat 7.7 pKi = 7.7 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
44415624 79695 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213193 79695 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415577 79735 0 None 20 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 436 2 1 7 3.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccon3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213372 79735 0 None 20 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 436 2 1 7 3.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccon3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
25142456 81994 2 None -10 9 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 81994 2 None -10 9 Pig 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
439654 16321 34 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL1235966 16321 34 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
21527771 69813 0 None -8 10 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940404 69813 0 None -8 10 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 363 6 1 3 4.2 OC1(c2ccc(Cl)cc2)CCN(CCCOc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
10903748 78067 0 None -11 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL2111781 78067 0 None -11 3 Rat 7.7 pKi = 7.7 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN([C@H]2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
10830234 99912 0 None 20 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289867 99912 0 None 20 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
11186523 126989 0 None -15 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL366164 126989 0 None -15 9 Human 7.7 pKi = 7.7 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1C[C@@H]2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
44408818 139635 1 None -12 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL380330 139635 1 None -12 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
53361301 63511 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1803024 63511 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
54585810 61275 0 None -22 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771108 61275 0 None -22 5 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3c(cccc3-c3ccccc3)C2=O)CC1 10.1016/j.bmcl.2010.12.083
53361301 63511 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803024 63511 0 None -14 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 985 29 0 16 8.6 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
53364226 63515 0 None -67 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803028 63515 0 None -67 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 989 29 0 18 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
118709160 112907 0 None -18 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318832 112907 0 None -18 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 846 18 0 8 10.1 O=C(CCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
118709161 112908 0 None -83 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318833 112908 0 None -83 4 Pig 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 860 19 0 8 10.5 O=C(CCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10524751 57056 0 None -1 4 Bovine 5.7 pKi = 5.7 Binding
Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
CHEMBL165171 57056 0 None -1 4 Bovine 5.7 pKi = 5.7 Binding
Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 395 5 0 1 6.5 CCCN(CCC)C1CCC(=C(C#Cc2ccccc2)C#Cc2ccccc2)CC1 10.1021/jm991098z
11036641 31562 0 None -147 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
CHEMBL140612 31562 0 None -147 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 393 7 1 6 2.3 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm025558r
11517928 76750 0 None -18 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL207543 76750 0 None -18 4 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 444 4 0 6 4.3 Clc1ccc(N2CCN(Cc3cn4nc(N5CCCCC5)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
15548770 66117 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 375 2 2 4 5.0 CN1CCc2cc(Sc3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1802234 66117 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 375 2 2 4 5.0 CN1CCc2cc(Sc3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852041 66117 0 None -3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 375 2 2 4 5.0 CN1CCc2cc(Sc3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
122181333 121360 0 None -1548 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590084 121360 0 None -1548 6 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 366 8 1 2 3.8 CCCN(CCNC(=O)/C=C/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
57402365 68953 0 None -169 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928119 68953 0 None -169 5 Pig 5.7 pKi = 5.7 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 441 12 1 6 3.1 CCOCCOc1cccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
44270558 164736 0 None -812 4 Bovine 5.7 pKi = 5.7 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL423247 164736 0 None -812 4 Bovine 5.7 pKi = 5.7 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44400553 70435 0 None -2398 5 Pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL195083 70435 0 None -2398 5 Pig 5.7 pKi = 5.7 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
15467372 168544 0 None -138 4 Bovine 4.7 pKi = 4.7 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
CHEMBL440120 168544 0 None -138 4 Bovine 4.7 pKi = 4.7 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1[nH]ccc1CN1CCN(c2ccccc2)CC1 10.1016/s0960-894x(99)00302-9
44264644 203035 0 None -1737 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL7442 203035 0 None -1737 4 Bovine 4.7 pKi = 4.7 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 330 3 0 4 3.2 Clc1ccc(N2CCN(Cc3cnn4c3CCCC4)CC2)cc1 10.1016/s0960-894x(98)00692-1
45269161 194661 0 None -181 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL562384 194661 0 None -181 4 Bovine 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 336 3 0 6 2.4 Cc1cc2nc(C)c(CN3CCN(c4ccccn4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
46850462 76209 0 None -16 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccccc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
CHEMBL2062849 76209 0 None -16 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccccc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
46850464 76211 0 None -87 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062851 76211 0 None -87 3 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
5353432 97046 84 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
CHEMBL270299 97046 84 None -1 3 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 249 2 0 3 2.8 CC(C)(C)c1ccc(S(=O)(=O)/C=C/C#N)cc1 nan
45481889 197337 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 637 10 2 10 5.4 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5nsc6ccccc56)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
CHEMBL585741 197337 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 637 10 2 10 5.4 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5nsc6ccccc56)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
90644062 111542 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 111542 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
90644062 111542 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289647 111542 0 None -11 5 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 345 6 0 4 3.8 Cc1ccc(N2CCN(CCCSc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
44448065 154942 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL404037 154942 0 None -2 2 Rat 4.7 pKi = 4.7 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
117773891 131903 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 379 5 1 6 3.1 Cc1cc(Oc2ncccc2OC2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697566 131903 0 None - 1 Human 6.7 pKi = 6.7 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 379 5 1 6 3.1 Cc1cc(Oc2ncccc2OC2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
145979741 166132 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4282096 166132 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
46231835 199148 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 410 2 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCCCC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL600998 199148 0 None -8 2 Human 6.7 pKi = 6.7 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 410 2 1 3 5.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cc(CN4CCCCC4)ccc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL1200633 206858 3 None -7 8 Human 5.7 pKi = 5.7 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(CC[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(CC[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
112500027 131941 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697603 131941 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
44320257 204455 0 None -5 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86325 204455 0 None -5 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
49783209 17427 0 None -3981 27 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat dopamine D1 receptorBinding affinity to rat dopamine D1 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17427 0 None -3981 27 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat dopamine D1 receptorBinding affinity to rat dopamine D1 receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
19795148 116090 0 None 97 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 265 0 1 2 3.3 CN1CCc2cc(Cl)c(O)cc2C2(CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL336610 116090 0 None 97 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 265 0 1 2 3.3 CN1CCc2cc(Cl)c(O)cc2C2(CCCC2)C1 10.1016/S0960-894X(00)80155-9
44447998 154854 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 363 6 0 3 5.3 CCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL403550 154854 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 363 6 0 3 5.3 CCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415844 79716 0 None 20 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3nccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213278 79716 0 None 20 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3nccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
17756102 85717 0 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
CHEMBL231171 85717 0 None 2 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 309 1 0 2 4.1 COc1ccc2c(c1)CCCN(C)CCCc1ccccc1C2 10.1021/jm070388+
15069442 100234 0 None 104 2 Rat 7.6 pKi = 7.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
CHEMBL292451 100234 0 None 104 2 Rat 7.6 pKi = 7.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
71110293 142847 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 142847 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
71110293 142847 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 142847 0 None 6 3 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
70682088 75715 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057446 75715 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
117773010 131931 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.9 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C nan
CHEMBL3697593 131931 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.9 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C nan
10947658 28490 0 None -208 16 Mouse 6.6 pKi = 6.6 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL137781 28490 0 None -208 16 Mouse 6.6 pKi = 6.6 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
6603954 200918 2 None -81 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL612083 200918 2 None -81 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
11392229 62650 0 None -15 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 293 1 0 3 2.9 Cc1ccc2n1Cc1ccccc1C=C2N1CCN(C)CC1 10.1021/jm049629t
CHEMBL178564 62650 0 None -15 4 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 293 1 0 3 2.9 Cc1ccc2n1Cc1ccccc1C=C2N1CCN(C)CC1 10.1021/jm049629t
44360984 34855 0 None -208 6 Human 5.6 pKi = 5.6 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
CHEMBL143352 34855 0 None -208 6 Human 5.6 pKi = 5.6 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cccn3nccc23)CC1 10.1021/jm025558r
11516033 138588 5 None -1949 6 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL378680 138588 5 None -1949 6 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 360 3 0 4 4.0 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1Cl 10.1021/jm060166w
54583897 61273 0 None -1445 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771106 61273 0 None -1445 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 411 7 0 4 3.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(F)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363109 63517 0 None -691 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803030 63517 0 None -691 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 465 11 0 8 4.0 CCCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
137660046 158796 0 None -3235 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4100183 158796 0 None -3235 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 437 7 2 8 2.4 O=C1COc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2N1 10.1021/acs.jmedchem.7b00363
52937871 60844 0 None -588 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
CHEMBL1765631 60844 0 None -588 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 458 11 1 5 4.6 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(C=O)c2C1 10.1021/jm101639t
122177644 120699 0 None -19054 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577345 120699 0 None -19054 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
56926585 68663 0 None -5495 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
CHEMBL1923293 68663 0 None -5495 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 358 4 0 5 2.9 COc1cc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)ccc1F 10.1021/jm200762g
44381424 58762 0 None -190 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169562 58762 0 None -190 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
44381432 120206 0 None -6 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL354748 120206 0 None -6 4 Bovine 4.6 pKi = 4.6 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 3 1 4 2.6 c1ccc(C2=NC[C@@H](N3CCN(c4ccccc4)CC3)CCN2)cc1 10.1016/s0960-894x(03)00004-0
72301 185536 72 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL487182 185536 72 None 1 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
44591134 175626 0 None -194 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459373 175626 0 None -194 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
154726381 175953 1 None -446 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 175953 1 None -446 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 175953 1 None -446 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
90644057 111540 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 111540 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
90644057 111540 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289645 111540 0 None -190 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 365 6 0 4 3.7 FC(F)(F)c1ccc(OCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
145992269 166400 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
CHEMBL4287192 166400 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12 10.1021/acs.jmedchem.8b01622
46227273 198129 0 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
CHEMBL594127 198129 0 None 2 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 3 0 2 3.8 COc1ccc2c(c1)CCN(C)C2Cc1ccccc1C 10.1016/j.bmc.2009.08.028
135398737 944 89 None -83 91 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
38 944 89 None -83 91 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
722 944 89 None -83 91 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
CHEMBL42 944 89 None -83 91 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
DB00363 944 89 None -83 91 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9810396
14198576 196211 0 None -2 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 3 1 2 3.8 COc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL572720 196211 0 None -2 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 3 1 2 3.8 COc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
228 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
33 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
6005 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
CHEMBL53 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
DB00714 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00004a011
228 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
33 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
6005 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
CHEMBL53 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
DB00714 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
228 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
33 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
6005 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
CHEMBL53 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
DB00714 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960188q
228 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
33 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
6005 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
CHEMBL53 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
DB00714 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm960189i
44415613 77713 0 None 15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 543 3 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCN(C)CC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL210016 77713 0 None 15 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 543 3 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCN(C)CC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
72708061 91767 0 None -1 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425372 91767 0 None -1 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 309 1 0 4 3.1 COc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
44415645 138814 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 613 4 1 7 6.5 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc4c(c3)OCCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL379286 138814 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 613 4 1 7 6.5 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc4c(c3)OCCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
44209480 69827 0 None -218 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940418 69827 0 None -218 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 313 6 0 3 3.4 Fc1ccc(CCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
10264172 10334 0 None -7413 2 Rat 4.6 pKi = 4.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 2 2 3.1 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960188q
CHEMBL116367 10334 0 None -7413 2 Rat 4.6 pKi = 4.6 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 251 0 2 2 3.1 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm960188q
3037308 43829 19 None -99 6 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
CHEMBL151475 43829 19 None -99 6 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 452 7 1 7 4.2 O=c1c(CO)coc2cc(OCCCN3CCC(c4noc5cc(F)ccc45)CC3)ccc12 10.1021/jm9810396
9928073 201954 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL67284 201954 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00030a011
10108504 38670 0 None 6 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3ccccc3Oc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL146741 38670 0 None 6 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3ccccc3Oc3ncccc32)CC1 10.1021/jm00030a011
44582518 181011 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.6 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477055 181011 0 None -10 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.6 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1016/j.bmcl.2009.01.067
3036864 201066 16 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 201066 16 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 201066 16 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 201066 16 None -2 27 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
44385451 59280 0 None -7 2 Rat 7.6 pKi = 7.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 284 3 0 2 3.9 Cc1cccc2c1C(CN(C)C)CN2c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
CHEMBL171903 59280 0 None -7 2 Rat 7.6 pKi = 7.6 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 284 3 0 2 3.9 Cc1cccc2c1C(CN(C)C)CN2c1ccc(F)cc1 10.1016/s0960-894x(98)00138-3
13838745 94294 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
CHEMBL25305 94294 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 281 1 3 3 2.9 Oc1cc2c3c(c1O)CC[C@@H]3CNC[C@@H]2c1ccccc1 10.1021/jm00170a025
1353 1880 85 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
3559 1880 85 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
86 1880 85 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
CHEMBL54 1880 85 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
DB00502 1880 85 None -74 85 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00391a028
15937721 18913 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 255 2 1 3 2.6 CCOC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL128917 18913 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 255 2 1 3 2.6 CCOC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
44415670 138387 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 565 2 1 5 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL378341 138387 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 565 2 1 5 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)ccc3C(F)(F)F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415745 165769 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL427230 165769 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(Cl)cc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
86764211 131924 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697587 131924 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
90140334 128891 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc2n[nH]cc2c(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)n1 nan
CHEMBL3671270 128891 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc2n[nH]cc2c(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)n1 nan
44276535 97937 0 None 50 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL275379 97937 0 None 50 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
10432808 58441 0 None -6 4 Bovine 6.6 pKi = 6.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168611 58441 0 None -6 4 Bovine 6.6 pKi = 6.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
2389 3279 114 None -467 67 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
5073 3279 114 None -467 67 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
96 3279 114 None -467 67 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
CHEMBL85 3279 114 None -467 67 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
DB00734 3279 114 None -467 67 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 nan
10042942 154964 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1OC)-c1c(OC)c(O)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL404136 154964 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1OC)-c1c(OC)c(O)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
137642380 157961 0 None -48 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4091155 157961 0 None -48 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 431 6 1 5 4.2 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2nccc2c1 10.1021/acs.jmedchem.6b01857
90644227 111288 0 None -186 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287396 111288 0 None -186 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 448 8 1 6 4.1 OCc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
228 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
33 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
6005 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
CHEMBL53 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
DB00714 441 26 None -30 24 Rat 6.6 pKi = 6.6 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
9928073 201954 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00067a009
CHEMBL67284 201954 0 None -7 3 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3cc(Cl)ccc3Sc3ccccc32)CC1 10.1021/jm00067a009
53362716 63631 0 None -26 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
CHEMBL1806871 63631 0 None -26 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
49783039 17471 0 None -954 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
CHEMBL1258383 17471 0 None -954 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 421 7 1 4 4.9 Cc1ccc(C)c(N2CCN(CCCCNC(=O)c3cc4ccccc4s3)CC2)c1 10.1021/jm100899z
57400557 68970 0 None -1995 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928136 68970 0 None -1995 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 509 14 1 8 3.2 CCOCCOCc1ccn2ncc(C(=O)NCCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
15654854 101785 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cccnc3Nc3ccccc32)CC1 10.1021/jm00067a009
CHEMBL303173 101785 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3cccnc3Nc3ccccc32)CC1 10.1021/jm00067a009
11589069 95800 0 None -1479 8 Human 5.6 pKi = 5.6 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
CHEMBL260994 95800 0 None -1479 8 Human 5.6 pKi = 5.6 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 383 6 1 3 4.4 O=C1Nc2ccccc2C1CCCCN1CCN(c2ccc(Cl)cc2)CC1 10.1021/jm070279v
15115513 108193 0 None -218 2 Human 4.6 pKi = 4.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL320779 108193 0 None -218 2 Human 4.6 pKi = 4.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
681 1437 65 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
940 1437 65 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
947 1437 65 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
CHEMBL59 1437 65 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
DB00988 1437 65 None -154 38 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01622
44299917 168882 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@@H]21 10.1021/jm00128a038
CHEMBL442740 168882 0 None - 1 Rat 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)CCN(C)[C@H]1CCc3ccccc3[C@@H]21 10.1021/jm00128a038
90134304 165961 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
CHEMBL4278861 165961 1 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21 10.1021/acs.jmedchem.8b01622
71562963 87148 0 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335741 87148 0 None -2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
10691657 119409 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 387 3 0 3 5.1 CCCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
CHEMBL349311 119409 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 387 3 0 3 5.1 CCCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
168294767 192417 0 None -457 20 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192417 0 None -457 20 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192417 0 None -457 20 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
117773347 131905 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 378 4 1 6 2.8 Cc1cc(Oc2ncccc2N2CCC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697568 131905 0 None - 1 Human 6.6 pKi = 6.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 378 4 1 6 2.8 Cc1cc(Oc2ncccc2N2CCC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
71110290 146627 0 None - 1 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3927835 146627 0 None - 1 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)C1Cc3c(OC)ccc(OC)c3CN1CC2 nan
15711860 13746 0 None -1 2 Goldfish 6.6 pKi = 6.6 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1195937 13746 0 None -1 2 Goldfish 6.6 pKi = 6.6 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL555619 13746 0 None -1 2 Goldfish 6.6 pKi = 6.6 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 285 3 2 4 2.7 COc1ccc2c(c1O)C[C@@H](c1ccccc1)O[C@H]2CN 10.1021/jm00114a002
14198588 170941 2 None 2 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL446396 170941 2 None 2 2 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
44320001 204297 0 None 2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84983 204297 0 None 2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44591135 189584 0 None -158 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL517407 189584 0 None -158 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 532 10 0 4 8.0 CN(CC/C=C1\c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
71110293 142847 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
CHEMBL3897805 142847 0 None 6 3 Human 6.6 pKi = 6.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCO4 nan
135398745 2869 108 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
47 2869 108 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
CHEMBL715 2869 108 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
DB00334 2869 108 None -23 65 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm800689g
1353 1880 85 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
3559 1880 85 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
86 1880 85 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
CHEMBL54 1880 85 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
DB00502 1880 85 None -38 85 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH233930 from human D1 receptor expressed in HEK cellsDisplacement of [3H]SCH233930 from human D1 receptor expressed in HEK cells
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2011.04.098
1242 3556 23 None -5 17 Human 7.6 pKi = 7.6 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
935 3556 23 None -5 17 Human 7.6 pKi = 7.6 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
CHEMBL286080 3556 23 None -5 17 Human 7.6 pKi = 7.6 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00116a004
75306277 108767 0 None -12 23 Human 7.6 pKi = 7.6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 108767 0 None -12 23 Human 7.6 pKi = 7.6 Binding
Binding affinity to dopamine D1 receptor (unknown origin) by PDSP assayBinding affinity to dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
9884087 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
71474026 153765 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
CHEMBL3986624 153765 0 None 1 2 Human 7.6 pKi = 7.6 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 353 2 0 5 3.1 COc1ccc(OC)c2c1C[C@H]1c3cc4c(cc3CCN1C2)OCCO4 nan
11718008 74941 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL203734 74941 0 None -1 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 349 1 0 2 4.6 COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
44415954 80689 0 None 72 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 467 6 1 5 5.4 CCCC(CCC)C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL215581 80689 0 None 72 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 467 6 1 5 5.4 CCCC(CCC)C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
135398745 2869 108 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
47 2869 108 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
CHEMBL715 2869 108 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
DB00334 2869 108 None -26 65 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm030480f
53364154 63512 0 None -13 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803025 63512 0 None -13 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1013 31 0 16 9.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
45273443 193958 0 None -66 4 Bovine 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL556288 193958 0 None -66 4 Bovine 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 392 4 1 6 2.2 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
137644966 157948 0 None -363 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
CHEMBL4091064 157948 0 None -363 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 456 6 1 6 4.1 N#Cc1cnn2ccc(NC(=O)CCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/acs.jmedchem.6b01857
122191607 123205 0 None -346 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622099 123205 0 None -346 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 468 9 1 3 5.0 CCCN(CCN1CCN(CCc2c[nH]c3ccccc23)CC1)c1ccc(Br)cc1 10.1021/acsmedchemlett.5b00131
56837636 68955 0 None -177 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928121 68955 0 None -177 5 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 897 28 2 13 5.1 COc1ccccc1N1CCN(CCCNC(=O)c2cccc(OCCOCCOCCOCCOc3cccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)c3)c2)CC1 10.1016/j.bmc.2011.10.063
44401042 124309 0 None -67 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL364270 124309 0 None -67 9 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
11575799 77775 0 None -2511 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
CHEMBL210341 77775 0 None -2511 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 438 3 0 4 4.7 Clc1ccc(N2CCN(Cc3cn4cc(Br)ccc4n3)CC2)cc1Cl 10.1021/jm060166w
25256814 181030 0 None -1318 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 181030 0 None -1318 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363110 63520 0 None -194 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803050 63520 0 None -194 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 507 14 0 8 4.8 CCCCn1cc(CCCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
24823922 160246 0 None -15 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
CHEMBL411437 160246 0 None -15 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
11725531 53769 1 None -1659 5 Bovine 5.6 pKi = 5.6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160626 53769 1 None -1659 5 Bovine 5.6 pKi = 5.6 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 351 3 0 5 3.2 N#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
15522515 97709 0 None -1479 4 Bovine 4.6 pKi = 4.6 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL273860 97709 0 None -1479 4 Bovine 4.6 pKi = 4.6 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 292 3 0 4 2.7 c1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
71734028 90622 0 None -7762 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397390 90622 0 None -7762 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
2389 3279 114 None -331 67 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
5073 3279 114 None -331 67 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
96 3279 114 None -331 67 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
CHEMBL85 3279 114 None -331 67 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
DB00734 3279 114 None -331 67 Rat 6.6 pKi = 6.6 Binding
Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.Binding affinity measured at the Dopamine receptor D1 by the inhibition of [3H]SCH-23390 binding to rat striatum using unlabeled apomorphine for nonspecific binding.
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm9810396
44320002 106558 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315535 106558 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44582491 180973 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 6 0 4 3.3 COc1ccccc1N1CCN(CCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476641 180973 0 None -12 3 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 6 0 4 3.3 COc1ccccc1N1CCN(CCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
10022123 53035 0 None -28 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL159969 53035 0 None -28 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL92673 53035 0 None -28 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 371 5 0 4 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3sccc3C2=O)CC1 10.1021/jm981094e
71562966 87145 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
CHEMBL2335738 87145 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
44478261 191699 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 0 3 6 3.0 CN1CCc2c3c(cc4nc(N)sc24)-c2c(ccc(O)c2O)C[C@H]31 10.1016/j.bmc.2008.05.077
CHEMBL520610 191699 0 None -7 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 0 3 6 3.0 CN1CCc2c3c(cc4nc(N)sc24)-c2c(ccc(O)c2O)C[C@H]31 10.1016/j.bmc.2008.05.077
175 3598 38 None -831 7 Mouse 5.6 pKi = 5.6 Binding
Tested for binding affinity against dopamine receptor D1Tested for binding affinity against dopamine receptor D1
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00069a010
68186 3598 38 None -831 7 Mouse 5.6 pKi = 5.6 Binding
Tested for binding affinity against dopamine receptor D1Tested for binding affinity against dopamine receptor D1
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00069a010
CHEMBL79834 3598 38 None -831 7 Mouse 5.6 pKi = 5.6 Binding
Tested for binding affinity against dopamine receptor D1Tested for binding affinity against dopamine receptor D1
ChEMBL 383 6 1 4 3.0 Fc1ccc(cc1)OCCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00069a010
145988779 166726 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
CHEMBL4293356 166726 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C 10.1021/acs.jmedchem.8b01622
72164182 91718 0 None -41 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
CHEMBL2420777 91718 0 None -41 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 326 3 0 3 4.4 Clc1ccc(N2CCN(Cc3cccs3)CC2)cc1Cl 10.1016/j.bmcl.2013.07.033
10092819 16594 0 None -2454 12 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
CHEMBL124444 16594 0 None -2454 12 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm0211220
44415647 138710 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 639 5 1 6 7.6 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL378893 138710 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 639 5 1 6 7.6 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
164612037 184795 0 None -144 20 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
CHEMBL4860528 184795 0 None -144 20 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D1 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1021/acs.jmedchem.1c00692
57396484 69826 2 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940417 69826 2 None -61 6 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 316 6 0 5 2.2 Fc1ccc(OCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
13015797 204181 0 None -1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
CHEMBL83915 204181 0 None -1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 400 6 0 5 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3ccc(F)cc3)CC1)OCC2 10.1021/jm960084f
44415836 79726 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 4 1 5 5.9 CCCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213335 79726 0 None 15 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 507 4 1 5 5.9 CCCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
70607606 176630 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 333 1 3 3 3.1 Oc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4635277 176630 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 333 1 3 3 3.1 Oc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
6852376 91167 11 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
CHEMBL1467585 91167 11 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
CHEMBL24077 91167 11 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
CHEMBL503958 91167 11 None -3 5 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1016/j.bmc.2008.09.049
72699812 114688 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 315 2 1 4 3.7 CCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344456 114688 0 None 1 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 315 2 1 4 3.7 CCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
10566865 115479 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL335515 115479 0 None -4 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
10015045 13541 1 None -2 6 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL119455 13541 1 None -2 6 Rat 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
86764215 131935 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697597 131935 0 None - 1 Human 7.6 pKi = 7.6 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
14198587 201441 1 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm00129a006
CHEMBL64117 201441 1 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2[C@@H]1Cc1ccccc1 10.1021/jm00129a006
11728201 13866 0 None -7 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL119687 13866 0 None -7 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9884087 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL120512 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
15115514 8983 0 None -54 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL109897 8983 0 None -54 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
90644061 111541 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 111541 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
136056636 111296 0 None -309 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111296 0 None -309 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
118709174 112923 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318847 112923 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 946 23 0 10 9.6 CN(CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)CCN(C)CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10917953 206249 0 None -7585 10 Rat 5.6 pKi = 5.6 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 206249 0 None -7585 10 Rat 5.6 pKi = 5.6 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
71583849 87304 0 None -147 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
CHEMBL2336893 87304 0 None -147 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 448 4 0 4 5.1 c1ccc(-n2cc(CN3CCN(c4cc5ccc4CCc4ccc(cc4)CC5)CC3)cn2)cc1 10.1016/j.bmc.2013.01.065
14659268 79228 2 None -35 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL2115032 79228 2 None -35 3 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 10.1016/j.bmc.2008.02.038
122180956 121257 0 None -263 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3589577 121257 0 None -263 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 404 7 1 3 4.8 CCCN(CCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
122177641 120696 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577342 120696 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
72544566 92699 0 None -1318 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443009 92699 0 None -1318 5 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 375 10 0 6 3.1 COc1ccccc1N1CCN(Cc2cn(CCCCCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
9865384 172923 27 None -30902 7 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
CHEMBL45305 172923 27 None -30902 7 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 393 5 1 3 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3ccc(F)c(Cl)c3)CC2)nc1 10.1021/jm100835q
10014924 106787 0 None -1548 5 Bovine 4.6 pKi = 4.6 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL316983 106787 0 None -1548 5 Bovine 4.6 pKi = 4.6 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
11472028 66434 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 1 3 3.2 OC(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
CHEMBL185875 66434 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 6 1 3 3.2 OC(c1ccccc1)c1ccccc1OCCN1CCCC1 10.1021/jm049720x
15711855 13301 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192799 13301 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL544099 13301 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 289 3 2 3 3.5 CNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
11696813 187335 12 None -316 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm100294b
CHEMBL496739 187335 12 None -316 9 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm100294b
90644061 111541 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289646 111541 0 None -239 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 6 0 4 3.1 Cc1ccc(N2CCN(CCCOc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
72708126 91770 0 None -7 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425375 91770 0 None -7 2 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
14198588 170941 2 None 2 2 Rat 4.6 pKi = 4.6 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
CHEMBL446396 170941 2 None 2 2 Rat 4.6 pKi = 4.6 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
57401706 69828 0 None -45 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940419 69828 0 None -45 11 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 331 6 0 4 3.5 Fc1ccc(SCCCN2CCN(c3ccccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44320218 204698 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
CHEMBL87897 204698 0 None 1 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1 10.1021/jm00112a034
10993765 78357 0 None -36 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 433 5 0 5 4.1 COc1ccccc1N1CCN(CC2CCN(C(=O)c3cc4ccccc4o3)CC2)CC1 10.1021/jm0211220
CHEMBL2112643 78357 0 None -36 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 433 5 0 5 4.1 COc1ccccc1N1CCN(CC2CCN(C(=O)c3cc4ccccc4o3)CC2)CC1 10.1021/jm0211220
91899757 128918 0 None - 1 Human 6.6 pKi = 6.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-n1c(C)nc2cnccc21 nan
CHEMBL3671296 128918 0 None - 1 Human 6.6 pKi = 6.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 356 3 1 6 4.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-n1c(C)nc2cnccc21 nan
4543 169982 36 None -5 29 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL1201156 169982 36 None -5 29 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
CHEMBL445 169982 36 None -5 29 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 nan
25256816 181026 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477206 181026 0 None -4168 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
9884087 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
CHEMBL120512 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm9706832
21533446 69812 0 None -7 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
CHEMBL1940403 69812 0 None -7 10 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 379 6 1 3 4.9 OC1(c2ccc(Cl)cc2)CCN(CCCSc2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.07.018
11728201 13866 0 None -7 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL119687 13866 0 None -7 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 363 3 1 5 3.0 OCCN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
9884087 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL120512 14468 0 None -5 3 Rat 7.6 pKi = 7.6 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 333 1 0 4 3.6 CN1CCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
70684965 77481 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL2092940 77481 0 None -39 2 Human 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
1353 1880 85 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
3559 1880 85 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
86 1880 85 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
CHEMBL54 1880 85 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
DB00502 1880 85 None -38 85 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm030480f
44249745 193772 0 None -363 6 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL552373 193772 0 None -363 6 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
CHEMBL567286 193772 0 None -363 6 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranesDisplacement of [3H]SCH 23990 from dopamine D1 receptor in porcine cerebral cortex membranes
ChEMBL 366 4 0 3 3.1 N#Cc1cccc(N2CCN(CCN3CCC(C(F)(F)F)CC3)C2=O)c1 10.1016/j.bmcl.2010.09.142
24878061 140879 0 None 25 2 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
CHEMBL384046 140879 0 None 25 2 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2 10.1021/jm0604979
10061323 11801 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL118254 11801 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
53364227 63516 0 None -50 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803029 63516 0 None -50 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1033 32 0 19 6.3 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCOCCOCCOCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
10061323 11801 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL118254 11801 0 None -60 4 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 263 1 0 1 4.0 CCc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
11405107 197385 0 None -32 4 Bovine 5.6 pKi = 5.6 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
CHEMBL58662 197385 0 None -32 4 Bovine 5.6 pKi = 5.6 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 341 3 1 2 3.7 C(#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1)c1ccccc1 10.1016/s0960-894x(02)00316-5
44403210 70199 0 None -630 5 Pig 5.6 pKi = 5.6 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194727 70199 0 None -630 5 Pig 5.6 pKi = 5.6 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 385 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
9970201 170076 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
CHEMBL445129 170076 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 267 0 2 3 2.6 Oc1cc2c(cc1O)C1c3ccccc3CCN1CC2 10.1021/jm00051a008
52938728 58246 0 None -1000 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684028 58246 0 None -1000 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 606 12 0 8 6.0 CCCN1CCc2cccc3c2C1Cc1cccc(OCc2cn(CCCCN4CCN(c5ccccc5OC)CC4)nn2)c1-3 10.1016/j.bmc.2011.01.053
137636066 155692 0 None -1698 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4064742 155692 0 None -1698 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 480 7 3 7 3.0 O=C1CCc2ccc(OCCCCN3CCCN(c4ccc(O)c5c4OCC(=O)N5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
4150 776 36 None -407 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
5288 776 36 None -407 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
644019 776 36 None -407 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
CHEMBL190461 776 36 None -407 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
DB09061 776 36 None -407 12 Human 5.6 pKi = 5.6 Binding
Inhibition of D1 dopamine receptor (unknown origin)Inhibition of D1 dopamine receptor (unknown origin)
ChEMBL 314 6 2 2 5.8 CCCCCc1cc(O)c(c(c1)O)[C@@H]1C=C(C)CC[C@H]1C(=C)C 10.1021/acs.jmedchem.0c00724
11689612 79429 0 None -28840 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
CHEMBL212160 79429 0 None -28840 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 388 5 0 7 2.9 COc1ccccc1N1CCN(Cc2cn3c(-n4cccn4)cccc3n2)CC1 10.1021/jm060166w
44412269 77746 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210232 77746 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2006.02.075
44412269 77746 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL210232 77746 0 None -10000 4 Pig 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 349 5 0 6 2.6 COc1ccccc1N1CCN(Cc2cn(-c3ccccc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
45271653 193565 0 None -2238 4 Bovine 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL550920 193565 0 None -2238 4 Bovine 4.6 pKi = 4.6 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)ncn34)CC2)cc1 10.1016/j.bmc.2009.05.015
10046389 61087 0 None -1122 5 Bovine 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
CHEMBL177031 61087 0 None -1122 5 Bovine 4.6 pKi = 4.6 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 397 5 1 3 3.8 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(Cl)cc1 10.1021/jm950759z
135 2496 38 None -91 57 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
1796 2496 38 None -91 57 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
4184 2496 38 None -91 57 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
CHEMBL6437 2496 38 None -91 57 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
DB06148 2496 38 None -91 57 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 nan
44406077 132297 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
CHEMBL370136 132297 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
90644071 111550 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289655 111550 0 None -1 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 368 5 0 3 5.2 Clc1ccc(N2CCCN(CCCc3cc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
131396 205008 6 None -549 5 Rat 5.6 pKi = 5.6 Binding
Compound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligandCompound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligand
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm00092a024
CHEMBL89934 205008 6 None -549 5 Rat 5.6 pKi = 5.6 Binding
Compound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligandCompound was evaluated for in vitro binding affinity towards Dopamine receptor D1 in striatum using [3H]- SCH 23390 as radioligand
ChEMBL 435 6 0 5 4.6 CC1SC(C)(C)C(=O)N1CCCCN1CCN(c2csc3cc(F)ccc23)CC1 10.1021/jm00092a024
118711255 113454 0 None -26 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(NCc3cccc(Cl)c3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325905 113454 0 None -26 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 392 4 2 3 5.3 CN1CCc2cc(NCc3cccc(Cl)c3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
45269964 13510 0 None -30 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1194295 13510 0 None -30 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL550180 13510 0 None -30 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 309 2 2 3 3.9 CCCN1CCc2cc(C)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
10825256 10083 0 None -6 3 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 260 0 0 2 3.3 CN1CCc2cccc3c2[C@H]1Cc1cccc(C#N)c1-3 10.1021/jm960189i
CHEMBL115969 10083 0 None -6 3 Rat 6.6 pKi = 6.6 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 260 0 0 2 3.3 CN1CCc2cccc3c2[C@H]1Cc1cccc(C#N)c1-3 10.1021/jm960189i
44432811 87139 0 None -5 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 323 3 1 3 4.2 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1016/j.bmcl.2007.05.057
CHEMBL233566 87139 0 None -5 3 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 323 3 1 3 4.2 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(C)c(O)c1-3 10.1016/j.bmcl.2007.05.057
44366021 120514 0 None - 1 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
CHEMBL356597 120514 0 None - 1 Human 7.6 pKi = 7.6 Binding
Ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranesAbility to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 of canine striatal membranes
ChEMBL 420 2 1 3 4.6 CN1CCc2cc(I)c(O)cc2[C@@H](c2ccc(N=[N+]=[N-])cc2)C1 10.1021/jm00164a009
44415559 79753 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213444 79753 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 496 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415673 138714 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 545 4 1 7 6.1 CCOc1c(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)sc2ccccc12 10.1016/j.bmcl.2006.06.022
CHEMBL378914 138714 0 None 6 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 545 4 1 7 6.1 CCOc1c(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)sc2ccccc12 10.1016/j.bmcl.2006.06.022
16104 161368 15 None -1 5 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
CHEMBL415300 161368 15 None -1 5 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00067a009
74223830 128928 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671305 128928 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
16104 161368 15 None -1 5 Rat 7.6 pKi = 7.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL415300 161368 15 None -1 5 Rat 7.6 pKi = 7.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
17755999 142353 1 None -5 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL389357 142353 1 None -5 6 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
86767095 128905 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 345 3 1 5 4.1 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671284 128905 0 None - 1 Human 7.6 pKi = 7.6 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 345 3 1 5 4.1 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
10566865 115479 0 None -4 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL335515 115479 0 None -4 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 309 6 1 2 4.6 CCCN(CCC)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
44408818 139635 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
CHEMBL380330 139635 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1021/jm051237e
44408818 139635 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2006.11.093
CHEMBL380330 139635 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmcl.2006.11.093
44408818 139635 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
CHEMBL380330 139635 1 None -12 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 10.1016/j.bmc.2009.08.028
45379370 7442 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
CHEMBL1087301 7442 0 None -2 5 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c([nH]c3ccccc23)CC1 10.1021/jm901291r
10090424 34474 1 None -3 6 Rat 7.5 pKi = 7.5 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
CHEMBL143027 34474 1 None -3 6 Rat 7.5 pKi = 7.5 Binding
In vitro affinity against Dopamine receptor D1In vitro affinity against Dopamine receptor D1
ChEMBL 368 3 0 5 4.2 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2occc21 10.1021/jm0009890
70692656 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2057457 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.12.016
70692656 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057457 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692656 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057457 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
70692656 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057457 75722 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 309 1 1 3 3.7 COc1cc2c(cc1O)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
44276651 99279 0 None 32 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL284959 99279 0 None 32 2 Human 6.6 pKi = 6.6 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
15225749 80273 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 341 0 1 5 3.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(N)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL215140 80273 0 None 2 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 341 0 1 5 3.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(N)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
137651073 156926 0 None -53 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4079301 156926 0 None -53 5 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C#N)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
118709162 112909 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318834 112909 0 None -97 4 Pig 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 874 20 0 8 10.9 O=C(CCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
10689581 99700 0 None 1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL287931 99700 0 None 1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2 10.1021/jm970038v
44380770 165159 0 None -91 4 Bovine 5.6 pKi = 5.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL424575 165159 0 None -91 4 Bovine 5.6 pKi = 5.6 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
11706497 77812 0 None -776 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 77812 0 None -776 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
56833379 67992 0 None -234 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
CHEMBL1916550 67992 0 None -234 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1155 37 2 18 8.6 COc1cc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2009919
44340415 8492 0 None -3 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 8492 0 None -3 4 Bovine 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
127045854 139034 0 None -218 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139034 0 None -218 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
127046949 139379 0 None -446 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799455 139379 0 None -446 6 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 472 12 3 5 4.6 COc1cc(CCNCCc2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
24936042 157047 0 None -218 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4080762 157047 0 None -218 5 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccn3nccc3c2)CC1 10.1021/acs.jmedchem.6b01857
57390115 68954 0 None -575 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
CHEMBL1928120 68954 0 None -575 5 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.4 CCOCCOc1cccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)c1 10.1016/j.bmc.2011.10.063
24824065 97502 0 None -1 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
CHEMBL272602 97502 0 None -1 4 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccccc1N1CCN(Cc2cnn3ccccc23)CC1 10.1021/jm701375u
10404144 203591 19 None -2187 10 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
CHEMBL7927 203591 19 None -2187 10 Pig 5.6 pKi = 5.6 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
14198593 196997 1 None 4 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
CHEMBL57988 196997 1 None 4 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
14198594 198419 1 None 6 2 Human 6.6 pKi = 6.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNC[C@H]2c1ccccc1 10.1021/jm00129a006
CHEMBL59603 198419 1 None 6 2 Human 6.6 pKi = 6.6 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNC[C@H]2c1ccccc1 10.1021/jm00129a006
44582178 180677 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 378 6 0 4 3.1 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476185 180677 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 378 6 0 4 3.1 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ccccn2)CC1 10.1016/j.bmcl.2009.01.067
9951008 204671 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm981094e
CHEMBL87717 204671 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm981094e
9951008 204671 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm00042a009
CHEMBL87717 204671 0 None -39 4 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 365 5 0 3 4.2 O=C(c1ccc(F)cc1)C1CCN(CCC2Cc3ccccc3C2=O)CC1 10.1021/jm00042a009
3561 18886 34 None -1 11 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
CHEMBL1289 18886 34 None -1 11 Human 6.6 pKi = 6.6 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl nan
15711852 13228 0 None -6 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192193 13228 0 None -6 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL543389 13228 0 None -6 3 Rat 5.6 pKi = 5.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
5041 3242 5 None -11220 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
981 3242 5 None -11220 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
CHEMBL4096543 3242 5 None -11220 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 465 6 0 4 4.6 CC(Oc1cccnc1N(C1CCN(CC1)Cc1ccc(cc1)I)C)C 10.1021/acs.jmedchem.7b00151
15711851 13429 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL1193797 13429 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
CHEMBL545264 13429 0 None -2 3 Rat 6.6 pKi = 6.6 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 303 3 1 3 3.8 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN(C)C 10.1021/jm00114a002
14198586 200148 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
CHEMBL60706 200148 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
91899758 128919 0 None - 1 Human 6.5 pKi = 6.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cc(=O)[nH]nc1C nan
CHEMBL3671297 128919 0 None - 1 Human 6.5 pKi = 6.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1cc(=O)[nH]nc1C nan
117773787 131919 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.7 Cc1cc(Oc2ncccc2C2COC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697582 131919 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.7 Cc1cc(Oc2ncccc2C2COC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
10333195 47922 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
CHEMBL155208 47922 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
1353 1880 85 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
3559 1880 85 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
86 1880 85 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
CHEMBL54 1880 85 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
DB00502 1880 85 None -74 85 Rat 7.5 pKi = 7.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm020938y
103 4089 56 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
2875 4089 56 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
5736 4089 56 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
CHEMBL285802 4089 56 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
DB09225 4089 56 None -28 53 Human 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm0002432
10379766 4837 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.2 CCc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
CHEMBL104571 4837 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 295 1 3 3 3.2 CCc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
17755999 142353 1 None -5 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
CHEMBL389357 142353 1 None -5 6 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 1 0 2 3.7 COc1ccc2c(c1)CCCN(C)CCc1ccccc1C2 10.1021/jm070388+
86767097 128907 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 359 3 1 5 4.5 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671286 128907 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 359 3 1 5 4.5 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
135398737 944 89 None -44 91 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
38 944 89 None -44 91 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
722 944 89 None -44 91 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
CHEMBL42 944 89 None -44 91 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
DB00363 944 89 None -44 91 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2008.06.030
10472143 118772 0 None -645 16 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL343755 118772 0 None -645 16 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@H]1C[C@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
11777127 25606 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL135318 25606 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
228 441 26 None -35 24 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
33 441 26 None -35 24 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
6005 441 26 None -35 24 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
CHEMBL53 441 26 None -35 24 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
DB00714 441 26 None -35 24 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2008.05.077
10154 141597 54 None -58 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL388342 141597 54 None -58 4 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 327 2 2 5 2.9 COc1cc2c(cc1O)C[C@H]1c3c(cc(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
9980998 30819 0 None -3981 8 Human 5.5 pKi = 5.5 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL139926 30819 0 None -3981 8 Human 5.5 pKi = 5.5 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
CHEMBL2112911 30819 0 None -3981 8 Human 5.5 pKi = 5.5 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm025558r
11697270 76957 0 None -3467 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
CHEMBL208274 76957 0 None -3467 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 412 5 0 5 4.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-c4ccccc4)c3n2)CC1 10.1021/jm060166w
44340376 110157 0 None -24 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325818 110157 0 None -24 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 6 1 3 4.9 COc1c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
25256816 181026 0 None -4466 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 181026 0 None -4466 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
16754 85148 43 None -67 7 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL228082 85148 43 None -67 7 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 355 4 0 5 3.5 COc1cc2c(cc1OC)-c1c(OC)c(OC)cc3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
25139181 183760 0 None -1513 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 183760 0 None -1513 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
44567587 177660 0 None -66 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 311 2 2 4 3.2 CCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL465055 177660 0 None -66 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 311 2 2 4 3.2 CCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
127046951 139372 0 None -61 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139372 0 None -61 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137633705 156077 0 None -5370 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
CHEMBL4069091 156077 0 None -5370 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 474 7 2 7 4.0 O=C(CCCN1CCN(c2cccc(Cl)c2Cl)CC1)Nc1ccn2ncc(/C=N\O)c2c1 10.1021/acs.jmedchem.6b01857
122177645 120700 0 None -13803 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577346 120700 0 None -13803 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 591 18 2 8 5.6 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)[C@H]3CCc4c(O)cccc4C3)cc2OC)nn1 10.1021/jm501889t
57391897 68967 0 None -301 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928133 68967 0 None -301 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 481 12 1 8 2.7 CCOCCOc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
57393634 68977 0 None -26 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928248 68977 0 None -26 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1cc(COCCOCCOCCOCCOCc2ccc(N3CCN(CCCCNC(=O)c4ccccc4)CC3)c(OC)c2)ccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1016/j.bmc.2011.10.063
24824063 97552 10 None -5 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cc4ccccn4n3)CC2)cc1 10.1021/jm701375u
CHEMBL272853 97552 10 None -5 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cc4ccccn4n3)CC2)cc1 10.1021/jm701375u
44381216 119826 0 None -19054 4 Bovine 4.5 pKi = 4.5 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL352925 119826 0 None -19054 4 Bovine 4.5 pKi = 4.5 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
44329314 206204 0 None -69 3 Bovine 4.5 pKi = 4.5 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL96958 206204 0 None -69 3 Bovine 4.5 pKi = 4.5 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2c(C)ccc2C1 10.1016/s0960-894x(01)00564-9
154706546 175872 1 None -63 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4452329 175872 1 None -63 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4596339 175872 1 None -63 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(F)c1 10.1021/acs.jmedchem.9b01835
17755991 151766 0 None 1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
CHEMBL396950 151766 0 None 1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 267 0 2 2 3.1 Oc1ccc2c(c1)CCCNCCc1ccccc1C2 10.1021/jm070388+
96918 12384 22 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
CHEMBL1186488 12384 22 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
118711257 113456 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccccc1CNc1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
CHEMBL3325907 113456 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccccc1CNc1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
44568534 173744 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 265 0 2 3 2.6 CN1CCc2cc(N)cc3c2[C@H]1Cc1cccc(N)c1-3 10.1016/j.bmc.2008.05.077
CHEMBL455051 173744 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 265 0 2 3 2.6 CN1CCc2cc(N)cc3c2[C@H]1Cc1cccc(N)c1-3 10.1016/j.bmc.2008.05.077
10438027 65857 0 None -954 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
CHEMBL184383 65857 0 None -954 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1021/jm900095y
44415805 81123 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 561 4 1 5 7.1 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(CC3CCCCC3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL216047 81123 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 561 4 1 5 7.1 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(CC3CCCCC3)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
96918 12384 22 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
CHEMBL1186488 12384 22 None -8 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 309 5 0 3 4.1 COc1cc(CCN(C)C)c2ccc3ccccc3c2c1OC 10.1016/j.bmcl.2013.06.078
154704705 175751 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4590356 175751 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595409 175751 1 None -1 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 11 1 6 4.9 CCOc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
10367486 9204 1 None -6 4 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL110948 9204 1 None -6 4 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
CHEMBL543613 9204 1 None -6 4 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 398 4 0 5 5.0 O=C1c2ccsc2CCC1CCN1CCC(c2noc3cc(F)ccc23)CC1 10.1021/jm981094e
1042 1551 20 None -204 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1551 20 None -204 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1551 20 None -204 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1551 20 None -204 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1551 20 None -204 16 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
72708126 91770 0 None -7 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425375 91770 0 None -7 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
71450550 83393 0 None -6 16 Human 5.5 pKi = 5.5 Binding
Binding affinity to D1 dopamine receptorBinding affinity to D1 dopamine receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
CHEMBL2205836 83393 0 None -6 16 Human 5.5 pKi = 5.5 Binding
Binding affinity to D1 dopamine receptorBinding affinity to D1 dopamine receptor
ChEMBL 309 4 1 3 2.0 COc1ccccc1CCN1C2C3C4CC5C6C4C2C6C1(O)C53 10.1016/j.bmcl.2012.08.046
736083 161665 15 None -50 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL416288 161665 15 None -50 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 267 0 2 3 2.9 CN1CCc2cccc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
10452020 117772 2 None 10 3 Human 8.5 pKi = 8.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm9800292
CHEMBL34095 117772 2 None 10 3 Human 8.5 pKi = 8.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)[C@@H](c2ccccc2)C1 10.1021/jm9800292
10516818 25447 0 None 2 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135197 25447 0 None 2 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 279 4 1 2 3.6 C=CCN(C)[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
122324 203 17 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00114a002
6077 203 17 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00114a002
CHEMBL86931 203 17 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00114a002
10467946 48205 3 None -1 4 Bovine 8.5 pKi = 8.5 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
CHEMBL155596 48205 3 None -1 4 Bovine 8.5 pKi = 8.5 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 263 5 2 3 3.1 CCCN(CCC)[C@H]1CCc2c(ccc(O)c2O)C1 10.1021/jm020990u
14809027 106546 0 None 257 4 Rat 8.5 pKi = 8.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL315468 106546 0 None 257 4 Rat 8.5 pKi = 8.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
122324 203 17 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
6077 203 17 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
CHEMBL86931 203 17 None 323 3 Rat 8.5 pKi = 8.5 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 10.1021/jm00173a005
44415690 79727 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL213336 79727 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
44415690 79727 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213336 79727 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 2 1 5 5.1 Cc1cccc(C)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
44415506 79829 0 None 169 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
CHEMBL213793 79829 0 None 169 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)c1 10.1016/j.bmcl.2006.06.022
46231845 199049 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL600083 199049 0 None 2 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 391 0 1 2 4.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(Br)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
1153 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
12668023 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
30026874 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
30026875 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
3341 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
6603851 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
933 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
939 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
985 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
CHEMBL1160786 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
CHEMBL1161520 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
CHEMBL588 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
DB00800 1598 53 None -1 10 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm00160a018
44401164 69473 0 None -19 9 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 69473 0 None -19 9 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
11573628 74350 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
CHEMBL203047 74350 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 301 0 1 2 3.7 CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 10.1021/jm051237e
46231848 198854 0 None 8 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598949 198854 0 None 8 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 396 1 1 3 4.1 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(N4CCCC4=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
3038603 101395 6 None 2 3 Human 8.5 pKi = 8.5 Binding
The compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligandThe compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL300647 101395 6 None 2 3 Human 8.5 pKi = 8.5 Binding
The compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligandThe compound was tested for binding affinity against Dopamine receptor D1 using SCH-23390 as radioligand
ChEMBL 335 1 0 1 5.4 CN(C)C1C=CC2(CC1)c1ccccc1C=Cc1ccc(Cl)cc12 10.1021/jm00109a026
86763997 131951 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697613 131951 0 None - 1 Human 8.5 pKi = 8.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
11778580 65796 1 None -5 5 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
CHEMBL184050 65796 1 None -5 5 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 283 0 1 3 2.9 CN1CCOc2cc(O)ccc2Cc2ccccc2CC1 10.1021/jm049720x
11493746 140792 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
CHEMBL383451 140792 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 335 0 1 2 4.3 CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 10.1021/jm051237e
17755867 85682 1 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
CHEMBL231070 85682 1 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2ccc(O)cc2CC1 10.1021/jm070388+
44415704 79749 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL213424 79749 0 None -1 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 474 2 2 6 4.4 Cc1cccc(N)c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
15937717 20447 0 None 346 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 253 2 1 2 3.4 CCCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL130851 20447 0 None 346 2 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 253 2 1 2 3.4 CCCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
56944383 111627 0 None -6 12 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
CHEMBL3290012 111627 0 None -6 12 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cellsDisplacement of [3H]SCH23390 from human recombinant D1 receptor expressed in CHO cells
ChEMBL 487 8 1 6 5.1 O=S(=O)(NCCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2ccccc2s1 10.1021/jm401895u
9861622 197763 3 None 1202 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 10.1021/jm00128a038
CHEMBL59139 197763 3 None 1202 2 Rat 8.5 pKi = 8.5 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 10.1021/jm00128a038
44415723 141248 0 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL386122 141248 0 None 70 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
6917970 3635 54 None -1 34 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.12.016
8370 3635 54 None -1 34 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.12.016
CHEMBL487387 3635 54 None -1 34 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.12.016
11079319 131278 1 None -13 3 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 1 0 4 3.9 CN1CCN(C2=Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm0309811
CHEMBL369367 131278 1 None -13 3 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 1 0 4 3.9 CN1CCN(C2=Cn3cccc3Sc3ccc(Br)cc32)CC1 10.1021/jm0309811
5249956 73048 1 None -4 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL201525 73048 1 None -4 6 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2008.04.081
44415536 138101 0 None 95 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(I)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL377584 138101 0 None 95 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(I)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
117774127 131901 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697564 131901 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
142405812 180421 0 None -40 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 381 3 1 4 5.6 CCOc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4758966 180421 0 None -40 3 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 381 3 1 4 5.6 CCOc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1cc(Cl)ccc1N2 10.1016/j.bmcl.2020.127563
15937730 18762 0 None 478 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 301 1 1 2 3.9 CN1CCc2cc(Cl)c(O)cc2C(C2C=CC=CC=C2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL128649 18762 0 None 478 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 301 1 1 2 3.9 CN1CCc2cc(Cl)c(O)cc2C(C2C=CC=CC=C2)C1 10.1016/S0960-894X(00)80155-9
44439945 92935 0 None 1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2cc(O)ccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL245571 92935 0 None 1 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 306 0 2 2 3.5 CN1CCc2cc(O)ccc2Cc2[nH]c3ccccc3c2CC1 10.1016/j.bmcl.2006.11.093
71474025 144794 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 144794 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
71474025 144794 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3913343 144794 0 None 131 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
44561317 188387 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 1 2 3.4 CCN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
CHEMBL508399 188387 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 281 1 1 2 3.4 CCN1CCc2ccccc2Cc2ccc(O)cc2CC1 10.1016/j.bmcl.2008.04.081
44415593 79837 0 None -3 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213834 79837 0 None -3 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc4ccccc34)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
6603703 206 7 None 1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysisDisplacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysis
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1016/j.ejmech.2020.113073
9637 206 7 None 1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysisDisplacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysis
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1016/j.ejmech.2020.113073
CHEMBL291143 206 7 None 1 5 Pig 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysisDisplacement of [3H]SCH-23390 from porcine striatum dopamine D1 receptor incubated for 30 mins by radioligand competition binding assay based scintillation counter analysis
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1016/j.ejmech.2020.113073
12668019 10143 6 None 204 3 Human 7.5 pKi = 7.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/jm9800292
CHEMBL1160787 10143 6 None 204 3 Human 7.5 pKi = 7.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1cc2c(c(Cl)c1O)CCNC[C@@H]2c1ccccc1 10.1021/jm9800292
44415338 155215 0 None 69 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 579 3 1 7 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnn(-c4ccccc4)c3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL405751 155215 0 None 69 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 579 3 1 7 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cnn(-c4ccccc4)c3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
6603703 206 7 None -7 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
9637 206 7 None -7 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
CHEMBL291143 206 7 None -7 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 10.1021/jm970038v
74223723 128893 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 334 3 1 4 4.6 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671272 128893 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 334 3 1 4 4.6 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
44320378 204343 0 None 25 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85409 204343 0 None 25 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86764212 131926 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 4 4.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697589 131926 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 4 4.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
9949441 113963 0 None -7 5 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL333455 113963 0 None -7 5 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
53364155 63513 0 None -27 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803026 63513 0 None -27 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 1041 33 0 16 10.2 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCCc1cn(CCCCCCCCCCn2cc(CCCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
71733932 90621 0 None -416 6 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
CHEMBL2397389 90621 0 None -416 6 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 414 10 1 2 5.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm400520c
145988693 166613 0 None -12 17 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL4291048 166613 0 None -12 17 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 524 7 1 3 7.1 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
10310103 106828 0 None -776 9 Rat 5.5 pKi = 5.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 106828 0 None -776 9 Rat 5.5 pKi = 5.5 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
3038495 700 30 None -2041 19 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
7625 700 30 None -2041 19 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
CHEMBL25236 700 30 None -2041 19 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm0211220
44436600 91370 0 None -3019 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 91370 0 None -3019 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
44340227 110152 0 None -2137 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 110152 0 None -2137 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10663221 33491 1 None -60 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
CHEMBL142217 33491 1 None -60 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4)CC3)c2c1 10.1021/jm0009989
11983282 138414 0 None -5128 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138414 0 None -5128 6 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
10333195 47922 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
CHEMBL155208 47922 0 None -10 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
25128757 102829 0 None -831 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
CHEMBL3084512 102829 0 None -831 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 383 3 1 3 5.6 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1csc2ccccc12 10.1021/jm800532x
44448058 154665 0 None 2 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL402517 154665 0 None 2 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
72545007 92690 0 None -199 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443000 92690 0 None -199 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 407 12 0 8 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
24824060 155174 0 None -12 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
CHEMBL405292 155174 0 None -12 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cc4ccccn4n3)CC2)n1 10.1021/jm701375u
10404663 166308 8 None -1000 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
CHEMBL428561 166308 8 None -1000 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 334 9 1 3 3.0 C=CCN1CCC[C@H]1CNC(=O)c1cc(CCCF)ccc1OC 10.1016/j.bmc.2007.07.017
12050198 198570 0 None -87 4 Bovine 4.5 pKi = 4.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59702 198570 0 None -87 4 Bovine 4.5 pKi = 4.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 347 6 1 4 4.1 c1ccc(CN2CCC(NCc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
156012196 176758 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4637246 176758 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 296 1 2 4 2.7 COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
46227242 198248 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 2 1 2 3.5 Cc1ccccc1CC1c2ccc(O)cc2CCN1C 10.1016/j.bmc.2009.08.028
CHEMBL594798 198248 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 2 1 2 3.5 Cc1ccccc1CC1c2ccc(O)cc2CCN1C 10.1016/j.bmc.2009.08.028
10809507 119179 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(OC)cc(Br)c2C1Cc1ccccc1O 10.1021/jm991034o
CHEMBL347243 119179 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(OC)cc(Br)c2C1Cc1ccccc1O 10.1021/jm991034o
76314268 105953 0 None -2630 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 105953 0 None -2630 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 105953 0 None -2630 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
188249 39415 4 None -2 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL147463 39415 4 None -2 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm00030a011
CHEMBL2022280 39415 4 None -2 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 328 0 0 5 3.2 CN1CCN(C2=Nc3cc(Cl)ccc3Oc3ncccc32)CC1 10.1021/jm00030a011
15654862 201956 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ccncc32)CC1 10.1021/jm00067a009
CHEMBL67298 201956 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ccncc32)CC1 10.1021/jm00067a009
15654863 201745 0 None 7 2 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ccncc32)CC1 10.1021/jm00067a009
CHEMBL65768 201745 0 None 7 2 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ccncc32)CC1 10.1021/jm00067a009
15654861 100274 0 None 3 2 Rat 4.5 pKi = 4.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ncccc32)CC1 10.1021/jm00067a009
CHEMBL292738 100274 0 None 3 2 Rat 4.5 pKi = 4.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3ccccc3N(C=O)c3ncccc32)CC1 10.1021/jm00067a009
44591099 175616 0 None -1122 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL459350 175616 0 None -1122 6 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
9796958 146045 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL2115374 146045 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL39230 146045 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL544814 146045 0 None -28 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm00018a002
CHEMBL3215298 209485 12 None -6 2 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL None None None CC[C@H](C)[C@H]1O[C@]2(C=C[C@@H]1C)C[C@@H]1C[C@@H](C/C=C(\C)[C@@H](O[C@H]3C[C@H](OC)[C@@H](O[C@H]4C[C@H](OC)[C@@H](O)[C@H](C)O4)[C@H](C)O3)[C@@H](C)/C=C/C=C3\CO[C@@H]4[C@H](O)C(C)=C[C@@H](C(=O)O1)[C@]34O)O2.CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@@H]3/C(C)=C/C[C@@H]4C[C@@H](C[C@]5(C=C[C@H](C)[C@@H](C(C)C)O5)O4)OC(=O)[C@@H]4C=C(C)[C@@H](O)[C@H]5OC/C(=C\C=C\[C@@H]3C)[C@@]45O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O nan
681 1437 65 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
940 1437 65 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
947 1437 65 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
CHEMBL59 1437 65 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
DB00988 1437 65 None -97 38 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
10474964 129949 0 None -8511 7 Bovine 5.5 pKi = 5.5 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL368061 129949 0 None -8511 7 Bovine 5.5 pKi = 5.5 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
CHEMBL5206021 129949 0 None -8511 7 Bovine 5.5 pKi = 5.5 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 381 5 1 3 3.3 O=C(NCCN1CCN(C2CCCc3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm950759z
10693836 9247 0 None -19 4 Rat 5.5 pKi = 5.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL111189 9247 0 None -19 4 Rat 5.5 pKi = 5.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL545488 9247 0 None -19 4 Rat 5.5 pKi = 5.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 428 8 0 5 4.3 O=C(CCCN1CCN(CCC2CCc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
44579031 189243 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 391 8 0 3 6.1 CCCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
CHEMBL516580 189243 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 391 8 0 3 6.1 CCCCCCC(=O)Oc1cccc2c1-c1cccc3c1[C@@H](C2)N(CCC)CC3 10.1016/j.bmc.2008.08.056
44415835 139264 0 None 181 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
CHEMBL379875 139264 0 None 181 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 5 1 8 4.5 COc1cc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc(OC)c1OC 10.1016/j.bmcl.2006.06.034
45271622 13917 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197278 13917 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL564909 13917 0 None -2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 357 2 2 3 4.9 CCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
134147903 148895 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 383 6 2 5 4.3 CCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3945856 148895 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 383 6 2 5 4.3 CCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
9949441 113963 0 None -7 5 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL333455 113963 0 None -7 5 Rat 7.5 pKi = 7.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 331 2 0 4 3.5 CCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
117774096 131908 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 5 3.7 Cc1cc(Oc2ncccc2C(C)C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697571 131908 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 5 3.7 Cc1cc(Oc2ncccc2C(C)C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
135398737 944 89 None -44 91 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
38 944 89 None -44 91 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
722 944 89 None -44 91 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
CHEMBL42 944 89 None -44 91 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
DB00363 944 89 None -44 91 Human 7.5 pKi = 7.5 Binding
Binding affinity against Dopamine D1 receptorBinding affinity against Dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2004.06.005
64638 105661 1 None 40 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL313530 105661 1 None 40 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 329 2 3 4 3.3 NC[C@@H]1OC(C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44320053 204059 0 None 257 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL82899 204059 0 None 257 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
44319976 106480 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
CHEMBL315005 106480 0 None 2 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1 10.1021/jm00112a034
11186895 87079 21 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
CHEMBL2334885 87079 21 None -5 4 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3OC)C[C@@H]21 10.1016/j.bmc.2012.12.016
242 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
34 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
60795 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
CHEMBL1112 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
DB01238 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmc.2017.08.037
242 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
34 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
60795 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL1112 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
DB01238 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
242 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 467 117 None -281 51 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
44436599 91369 0 None -257 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
CHEMBL241211 91369 0 None -257 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(C#Cc2ccccc2)c1 10.1016/j.bmc.2007.08.038
136043855 140996 0 None -389 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 482 2 1 6 5.6 FC1(F)Oc2cccc(CN3CCN(C4=Nc5cc(Cl)ccc5Nc5ccccc54)CC3)c2O1 10.1016/j.bmcl.2006.06.034
CHEMBL384634 140996 0 None -389 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 482 2 1 6 5.6 FC1(F)Oc2cccc(CN3CCN(C4=Nc5cc(Cl)ccc5Nc5ccccc54)CC3)c2O1 10.1016/j.bmcl.2006.06.034
127031949 138226 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 317 7 2 5 2.8 COc1cc(CCN(C)Cc2cccc(O)c2OC)ccc1O 10.1016/j.bmc.2016.03.037
CHEMBL3780438 138226 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 317 7 2 5 2.8 COc1cc(CCN(C)Cc2cccc(O)c2OC)ccc1O 10.1016/j.bmc.2016.03.037
4189 205195 91 None -25 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 205195 91 None -25 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 205195 91 None -25 34 Human 5.5 pKi = 5.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
117773625 131891 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.4 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2)c(C)c(=O)[nH]c1=O nan
CHEMBL3697554 131891 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.4 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2)c(C)c(=O)[nH]c1=O nan
44319988 204359 0 None 3 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85552 204359 0 None 3 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
156012433 176740 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 326 2 1 5 3.1 COc1cc2c3c(c1O)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4636948 176740 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 326 2 1 5 3.1 COc1cc2c3c(c1O)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
3246545 200787 1 None -7 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL1573438 200787 1 None -7 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL611207 200787 1 None -7 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting methodBinding affinity to dopamine D1 receptor in rat striatum by liquid scintillation counting method
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01584
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm800689g
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm010982y
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm0309811
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049629t
44319915 204249 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL84557 204249 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44415848 79499 0 None 40 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212438 79499 0 None 40 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 517 2 1 5 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
134150852 151163 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 461 6 2 5 5.1 CCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3964242 151163 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 461 6 2 5 5.1 CCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
86764320 131947 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697609 131947 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
15711869 13229 0 None -6 6 Goldfish 7.5 pKi = 7.5 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1192194 13229 0 None -6 6 Goldfish 7.5 pKi = 7.5 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL543390 13229 0 None -6 6 Goldfish 7.5 pKi = 7.5 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
6852376 91167 11 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
CHEMBL1467585 91167 11 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
CHEMBL24077 91167 11 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
CHEMBL503958 91167 11 None -3 5 Human 6.5 pKi = 6.5 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm9800292
71109986 150100 0 None - 1 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
CHEMBL3955446 150100 0 None - 1 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3cc(OC)c(OC)c(OC)c3CN1CC2 nan
54585811 61281 0 None -2454 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771113 61281 0 None -2454 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 418 7 0 5 3.2 COc1ccccc1N1CCN(CCCCN2CCc3cc(C#N)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
49783042 17509 0 None -112 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258495 17509 0 None -112 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 393 7 1 3 4.3 Cc1ccc(C)c(C(=O)NCCCCN2CCN(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
10871118 205080 0 None -489 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
CHEMBL90374 205080 0 None -489 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cccn4nccc34)CC2)cc1 10.1021/jm015522j
10667043 28337 0 None 7 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 7 2 3 4.6 NCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL137637 28337 0 None 7 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 7 2 3 4.6 NCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
44537929 196403 0 None -53 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(O)c(Cl)cc21 10.1016/j.bmc.2009.05.079
CHEMBL574296 196403 0 None -53 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 239 3 2 2 3.4 CCCCC1NCCc2cc(O)c(Cl)cc21 10.1016/j.bmc.2009.05.079
2470 3596 46 None -4168 59 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
3300 3596 46 None -4168 59 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
5265 3596 46 None -4168 59 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
99 3596 46 None -4168 59 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
CHEMBL267930 3596 46 None -4168 59 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00115a012
15021876 102935 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm00111a046
CHEMBL308480 102935 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm00111a046
15021876 102935 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm981094e
CHEMBL308480 102935 0 None -60 6 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 365 4 0 3 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2ccccc21 10.1021/jm981094e
10093238 205883 0 None -1 3 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 414 8 0 5 3.9 O=C(CCCN1CCN(CCC2Cc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL95112 205883 0 None -1 3 Rat 6.5 pKi = 6.5 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 414 8 0 5 3.9 O=C(CCCN1CCN(CCC2Cc3sccc3C2=O)CC1)c1ccc(F)cc1 10.1021/jm981094e
10738913 203255 0 None -5 5 Rat 4.5 pKi = 4.5 Binding
Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.
ChEMBL 386 8 2 5 1.5 CCOC(=O)c1[nH]c2ccc(CCN3C(=O)CNC3=O)cc2c1CCN(C)C 10.1021/jm9605849
CHEMBL76480 203255 0 None -5 5 Rat 4.5 pKi = 4.5 Binding
Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.Affinity pKi for Dopamine receptor D1 was measured in rat cortex homogenates.
ChEMBL 386 8 2 5 1.5 CCOC(=O)c1[nH]c2ccc(CCN3C(=O)CNC3=O)cc2c1CCN(C)C 10.1021/jm9605849
73356845 91772 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425377 91772 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
235224 127633 24 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
CHEMBL36654 127633 24 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
45481864 196457 0 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 2 2 3.5 Oc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL574695 196457 0 None -4 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 2 2 3.5 Oc1cc2c(cc1Cl)CCNC2Cc1ccccc1 10.1016/j.bmc.2009.05.079
2402 3318 58 None -74 25 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
5095 3318 58 None -74 25 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
7295 3318 58 None -74 25 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
CHEMBL589 3318 58 None -74 25 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
DB00268 3318 58 None -74 25 Human 4.5 pKi = 4.5 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1039/C4MD00066H
44320328 204506 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
CHEMBL86669 204506 0 None 1 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1 10.1021/jm00112a034
11696813 187335 12 None -316 9 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
CHEMBL496739 187335 12 None -316 9 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 10.1021/jm800689g
73356845 91772 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425377 91772 0 None -4 2 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1ccc2c(c1)CC1c3cc4c(cc3CCN1C2)OCO4 10.1016/j.ejmech.2013.07.036
6603820 95330 13 None -4 13 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
CHEMBL25856 95330 13 None -4 13 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1021/jm00018a002
6603820 95330 13 None -4 13 Human 7.5 pKi = 7.5 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL25856 95330 13 None -4 13 Human 7.5 pKi = 7.5 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
15937720 116374 0 None 81 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 271 2 1 3 3.3 CCSC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL338237 116374 0 None 81 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 271 2 1 3 3.3 CCSC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
86763999 131954 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.5 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2C)n(C)c(=O)[nH]c1=O nan
CHEMBL3697616 131954 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.5 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2C)n(C)c(=O)[nH]c1=O nan
45483269 195284 0 None -7 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 426 4 0 7 4.1 CSc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
CHEMBL566508 195284 0 None -7 4 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 426 4 0 7 4.1 CSc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
44396220 124903 1 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
CHEMBL364565 124903 1 None -1 6 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 295 6 0 2 4.1 c1ccc(Cc2ccccc2OCCN2CCCCC2)cc1 10.1021/jm049720x
90666899 108957 0 None -6 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
CHEMBL3220215 108957 0 None -6 7 Human 7.5 pKi = 7.5 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 381 3 1 4 4.2 Cc1nc2c(o1)CC(CN1CCC(c3c[nH]c4cc(F)ccc34)CC1)CC2=O 10.1039/C1MD00202C
2865 4079 67 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
59 4079 67 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
60854 4079 67 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
CHEMBL708 4079 67 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
DB00246 4079 67 None -114 53 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm030480f
511482 96803 5 None -251 5 Bovine 6.5 pKi = 6.5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268799 96803 5 None -251 5 Bovine 6.5 pKi = 6.5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 325 3 1 2 4.1 Clc1ccc(N2CCN(Cc3c[nH]c4ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
46917637 67990 0 None -275 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916548 67990 0 None -275 4 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1053 34 1 15 9.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(CN5CCN(c6ccccc6OC)CC5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
44417647 81749 0 None 1 2 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL1203924 81749 0 None 1 2 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
CHEMBL216945 81749 0 None 1 2 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21 10.1021/jm0604979
44400519 132608 0 None -549 5 Pig 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL370297 132608 0 None -549 5 Pig 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
10438027 65857 0 None -1096 6 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
CHEMBL184383 65857 0 None -1096 6 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 571 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2cc(I)ccc2o1 10.1016/j.bmcl.2004.05.052
44381147 58421 0 None -93 4 Bovine 5.5 pKi = 5.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168544 58421 0 None -93 4 Bovine 5.5 pKi = 5.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@@H]1CN(Cc2ccccc2)C[C@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
44340415 8492 0 None -3 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL109472 8492 0 None -3 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 460 5 1 3 5.3 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(C#Cc2ccccc2)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340333 9571 0 None -1071 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 9571 0 None -1071 4 Bovine 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
122181330 121357 0 None -3890 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 121357 0 None -3890 6 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
44372153 119659 0 None -89 4 Bovine 5.5 pKi = 5.5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
CHEMBL351550 119659 0 None -89 4 Bovine 5.5 pKi = 5.5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 416 4 0 4 5.3 Cc1nn2c(-c3ccccc3)cccc2c1CN1CCN(c2ccc(Cl)cc2)CC1 10.1016/s0960-894x(01)00814-9
71734127 90626 0 None -6760 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397476 90626 0 None -6760 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
10247561 97555 0 None -3 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
CHEMBL272873 97555 0 None -3 4 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
118711252 113451 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(N)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325901 113451 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(N)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
71562965 87146 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
CHEMBL2335739 87146 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 2 1 3 3.9 COc1ccc2c(c1)CCN1CC[C@@](O)(c3ccc(Cl)cc3)C[C@H]21 10.1016/j.bmcl.2012.12.046
24829343 158475 0 None -4265 9 Human 5.5 pKi = 5.5 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
CHEMBL409662 158475 0 None -4265 9 Human 5.5 pKi = 5.5 Binding
Inhibition of dopamine D1 receptorInhibition of dopamine D1 receptor
ChEMBL 429 7 1 3 5.1 CCC1(CCCCN2CCN(c3ccc(Cl)cc3)CC2)C(=O)Nc2cc(F)ccc21 10.1021/jm070279v
112500031 131946 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 0 5 4.3 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697608 131946 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 0 5 4.3 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)cnc(=O)n1C nan
70682090 75716 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057451 75716 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 10.1016/j.bmc.2012.05.057
70682090 75716 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
CHEMBL2057451 75716 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 323 2 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1Cc3cc(C)cc(C)c3CN1CC2 nan
72708128 91773 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425378 91773 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
11154555 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
2105 3005 34 None -537 33 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3005 34 None -537 33 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3005 34 None -537 33 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3005 34 None -537 33 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3005 34 None -537 33 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
86764215 131935 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697597 131935 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 4 4.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
10537185 25481 0 None -12 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
CHEMBL135224 25481 0 None -12 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 225 1 2 2 2.4 N[C@@H]1Cc2ccc(O)cc2[C@H]1c1ccccc1 10.1021/jm960318v
86767087 128894 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 318 3 1 4 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnn1C nan
CHEMBL3671273 128894 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 318 3 1 4 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnn1C nan
9948254 107783 0 None -141 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm00402a024
CHEMBL31973 107783 0 None -141 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 263 2 0 1 4.2 CCCN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm00402a024
15115515 108119 0 None -47 2 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL320526 108119 0 None -47 2 Human 6.5 pKi = 6.5 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 713 8 5 8 8.2 CCCN(CCc1ccc(N/C(S)=N/c2ccc3c(c2)C(=O)OC32c3ccc(O)cc3Oc3cc(O)ccc32)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
167715 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
969 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
CHEMBL225230 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00168a040
53317727 57637 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 313 3 1 3 3.5 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
CHEMBL1672313 57637 0 None -14 3 Human 6.5 pKi = 6.5 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 313 3 1 3 3.5 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
11121216 29925 0 None -169 14 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
CHEMBL138989 29925 0 None -169 14 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 335 1 1 2 3.0 C[C@@H]1C[C@@H](C)N1C(=O)[C@@H]1C=C2c3cccc4[nH]cc(c34)CC2N(C)C1 10.1021/jm020153s
167715 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00105a005
969 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00105a005
CHEMBL225230 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00105a005
44395741 180999 0 None -23 10 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL476935 180999 0 None -23 10 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL558392 180999 0 None -23 10 Pig 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 360 6 0 3 4.3 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 10.1021/jm100899z
56597938 3877 1 None -870 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
7651 3877 1 None -870 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
CHEMBL2165126 3877 1 None -870 9 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.7b00363
167715 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
969 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
CHEMBL225230 2832 12 None -954 5 Rat 6.5 pKi = 6.5 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00163a007
44454734 97278 0 None -912 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL271513 97278 0 None -912 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2ccc(OCCF)cc2)CC1 10.1016/j.bmcl.2007.12.026
25130816 187128 0 None -4786 3 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 490 8 2 5 5.8 CCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL495327 187128 0 None -4786 3 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 490 8 2 5 5.8 CCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
45483654 196441 0 None -14 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
CHEMBL574569 196441 0 None -14 5 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7cccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)c7)nn6)cc5)cc4)nn3)c2)CC1 10.1021/jm901120h
2779264 110854 36 None -30 4 Bovine 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL326877 110854 36 None -30 4 Bovine 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 240 3 0 2 3.3 c1ccc(CN2CCC(n3cccc3)CC2)cc1 10.1016/s0960-894x(99)00540-5
42605994 17692 0 None -16 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
CHEMBL1259071 17692 0 None -16 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 425 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3cc(Br)cs3)CC2)nc1 10.1021/jm100835q
11566745 74345 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL1202298 74345 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
CHEMBL203029 74345 0 None -1 4 Human 6.5 pKi = 6.5 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 283 0 2 3 2.7 CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 10.1021/jm050846j
167715 2832 12 None -954 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
969 2832 12 None -954 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
CHEMBL225230 2832 12 None -954 5 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm701045j
11154555 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
5037 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7671 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL2028019 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
CHEMBL3085826 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
DB06016 788 57 None -1445 12 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from D1 receptor (unknown origin) expressed in HEK293T cell membranes measured after 2 hrs by microbeta scintillation counting method
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.1c01327
7077 66625 24 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL186720 66625 24 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
CHEMBL3925724 66625 24 None -3 5 Human 6.5 pKi = 6.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 10.1021/jm049720x
3158 55974 21 None -2398 20 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
CHEMBL1628227 55974 21 None -2398 20 Human 6.5 pKi = 6.5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 nan
72708128 91773 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
CHEMBL2425378 91773 0 None -10 2 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 295 0 1 4 2.8 Oc1cccc2c1CN1CCc3cc4c(cc3C1C2)OCO4 10.1016/j.ejmech.2013.07.036
117774393 131936 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 307 3 1 4 3.5 Cc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c1 nan
CHEMBL3697598 131936 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 307 3 1 4 3.5 Cc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c1 nan
44588898 12495 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 331 2 3 3 4.0 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186959 12495 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 331 2 3 3 4.0 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL484352 12495 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 331 2 3 3 4.0 Oc1cc2c(c(-c3ccccc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
25256815 188963 0 None -51 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 397 6 0 3 3.9 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL514382 188963 0 None -51 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 397 6 0 3 3.9 O=C1c2ccccc2CCN1CCCCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2009.01.067
10833201 168046 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 373 2 0 3 4.7 CCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
CHEMBL436042 168046 0 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 373 2 0 3 4.7 CCN1CCc2c(Br)ccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
10707972 168490 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
CHEMBL439639 168490 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm991034o
72708127 91771 0 None -40 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425376 91771 0 None -40 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
13091359 113040 0 None -489 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
CHEMBL3321790 113040 0 None -489 10 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccc(F)cc1 10.1016/j.bmcl.2014.07.018
112500033 131949 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697611 131949 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)cnc(=O)n1C nan
118711265 113460 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 345 2 2 3 4.4 CN1CCc2cc(-c3ccc(O)cc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325916 113460 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 345 2 2 3 4.4 CN1CCc2cc(-c3ccc(O)cc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
44415551 79899 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL214142 79899 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(Cl)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
2726 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
621 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
83 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
CHEMBL71 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
DB00477 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00067a009
6852376 91167 11 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL1467585 91167 11 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL24077 91167 11 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
CHEMBL503958 91167 11 None -4 5 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm970038v
2726 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
621 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
83 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
CHEMBL71 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
DB00477 906 64 None -18 72 Rat 7.5 pKi = 7.5 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00030a011
10402378 65794 0 None -19 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
CHEMBL184049 65794 0 None -19 5 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 297 1 0 3 3.2 COc1ccc2c(c1)OCCN(C)CCc1ccccc1C2 10.1021/jm049720x
86764105 131961 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 3 1 5 3.6 Cc1cc(Sc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697623 131961 0 None - 1 Human 7.5 pKi = 7.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 3 1 5 3.6 Cc1cc(Sc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
6603820 95330 13 None -4 13 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
CHEMBL25856 95330 13 None -4 13 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.bmc.2009.08.028
90140110 128916 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cn[nH]c(=O)c1C nan
CHEMBL3671294 128916 0 None - 1 Human 7.5 pKi = 7.5 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cn[nH]c(=O)c1C nan
70690499 75718 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057453 75718 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.05.057
70690499 75718 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.12.016
CHEMBL2057453 75718 0 None 9 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 311 2 1 4 3.1 COc1ccc2c(c1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2012.12.016
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
24882561 94897 0 None -2041 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL256637 94897 0 None -2041 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 408 8 0 5 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
44403225 70204 0 None -346 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL194755 70204 0 None -346 5 Pig 5.5 pKi = 5.5 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 421 9 1 5 2.7 COc1ccccc1N1CCN(CCCCNS(=O)(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2005.07.037
44436596 91564 0 None -436 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241631 91564 0 None -436 4 Pig 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 401 5 1 3 3.5 C#Cc1ccc(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
10707972 168490 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
CHEMBL439639 168490 0 None 1 2 Rat 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 10.1021/jm060959i
44567588 189633 0 None -45 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 325 3 2 4 3.6 CCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
CHEMBL517491 189633 0 None -45 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 325 3 2 4 3.6 CCCOc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.bmc.2008.02.038
90644230 111298 0 None -1819 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287406 111298 0 None -1819 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
10479188 201184 0 None -316 4 Bovine 5.5 pKi = 5.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL62602 201184 0 None -316 4 Bovine 5.5 pKi = 5.5 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
44319370 106564 0 None -1 4 Bovine 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 106564 0 None -1 4 Bovine 5.5 pKi = 5.5 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
44380717 119843 0 None -138 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353087 119843 0 None -138 4 Bovine 4.5 pKi = 4.5 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
56926587 68668 0 None -2290 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
CHEMBL1923416 68668 0 None -2290 5 Pig 4.5 pKi = 4.5 Binding
Displacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]WAY100635 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 329 3 0 5 2.3 Fc1ccc(CN2CCN(c3ccc4c(c3)OCCO4)CC2)cn1 10.1021/jm200762g
118711253 113452 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(O)c(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325903 113452 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 268 1 2 3 2.6 CN1CCc2cc(O)c(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm9706832
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm800689g
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0309811
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049629t
112500030 131945 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
CHEMBL3697607 131945 0 None - 1 Human 6.5 pKi = 6.5 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 3 0 5 4.9 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)cnc(=O)n1C nan
135398737 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
38 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
722 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
CHEMBL42 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
DB00363 944 89 None -83 91 Rat 6.5 pKi = 6.5 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm010982y
1353 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
3559 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
86 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
CHEMBL54 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
DB00502 1880 85 None -74 85 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049632c
681 1437 65 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -23 38 Bovine 7.4 pKi = 7.4 Binding
Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
135398745 2869 108 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2869 108 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2869 108 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2869 108 None -26 65 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
117772904 131897 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 5 3.0 Cc1cc(Oc2nccc(C)c2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697560 131897 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 5 3.0 Cc1cc(Oc2nccc(C)c2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
90666903 108961 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
CHEMBL3220219 108961 0 None -4 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 452 4 1 5 5.0 O=C1CC(CN2CCC(c3c[nH]c4cc(F)ccc34)CC2)Cc2nc(N3CCCC3)sc21 10.1039/C1MD00202C
155552185 173489 0 None -660 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
CHEMBL4544086 173489 0 None -660 16 Human 6.4 pKi = 6.4 Binding
Displacement of [3H] SCH23390 from D1 receptor (unknown origin)Displacement of [3H] SCH23390 from D1 receptor (unknown origin)
ChEMBL 491 10 2 5 4.3 COc1ccccc1N1CCN(CCCNC(=O)NN(Cc2ccc(F)cc2)c2ccccc2)CC1 10.1021/acs.jmedchem.9b01085
118709173 112922 0 None -218 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318846 112922 0 None -218 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 944 20 0 10 9.4 O=C(CCN1CCN(CCC(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
72545240 92697 0 None -229 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443007 92697 0 None -229 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 469 12 0 8 3.4 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
52937777 60843 0 None -6165 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
CHEMBL1765630 60843 0 None -6165 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 464 10 1 4 5.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2ncc(Cl)c2C1 10.1021/jm101639t
57395340 68958 0 None -407 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928124 68958 0 None -407 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 469 14 1 6 3.6 CCOCCOCc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
71734029 90624 0 None -10964 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
CHEMBL2397392 90624 0 None -10964 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cnn3ccccc23)CC1 10.1021/jm400520c
14198593 196997 1 None 4 2 Rat 5.4 pKi = 5.4 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
CHEMBL57988 196997 1 None 4 2 Rat 5.4 pKi = 5.4 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
10064053 95461 0 None -1995 6 Rat 5.4 pKi = 5.4 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 311 1 0 1 5.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(-c2ccccc2)c1-3 10.1021/jm960189i
CHEMBL25924 95461 0 None -1995 6 Rat 5.4 pKi = 5.4 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 311 1 0 1 5.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(-c2ccccc2)c1-3 10.1021/jm960189i
10546334 64915 0 None -2187 5 Human 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 358 4 2 4 4.0 c1ccc2c(N3CCN(CCc4ccc5c(c4)NCN5)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
CHEMBL182721 64915 0 None -2187 5 Human 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 358 4 2 4 4.0 c1ccc2c(N3CCN(CCc4ccc5c(c4)NCN5)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
57580939 91769 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425374 91769 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
154726529 175871 1 None -33 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4467486 175871 1 None -33 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596338 175871 1 None -33 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 459 12 1 3 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
15711870 12847 0 None -1 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1189332 12847 0 None -1 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL538520 12847 0 None -1 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
154704418 176013 1 None 1 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4546749 176013 1 None 1 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
CHEMBL4597533 176013 1 None 1 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 458 12 1 6 4.8 Cn1c(SCCCNCC2CC2c2cc(F)ccc2OCCF)nnc1-c1ccccc1 10.1021/acs.jmedchem.9b01835
44567688 191677 0 None -8 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 295 2 1 3 3.5 CCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
CHEMBL520573 191677 0 None -8 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 295 2 1 3 3.5 CCOc1cccc2c1-c1cc(O)cc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2008.06.016
42625293 55956 0 None -912 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL1627319 55956 0 None -912 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 549 8 2 6 3.3 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
3036864 201066 16 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1256645 201066 16 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL1814790 201066 16 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
CHEMBL62 201066 16 None -26 27 Bovine 7.4 pKi = 7.4 Binding
Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid glandAbility to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00164a009
133 2460 48 None -30 42 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2460 48 None -30 42 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2460 48 None -30 42 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2460 48 None -30 42 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2460 48 None -30 42 Human 7.4 pKi = 7.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
24847750 182621 6 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/np50094a001
CHEMBL479587 182621 6 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 361 0 1 2 4.8 CC(C)(C)[C@]1(O)CCN2C[C@@H]3c4ccccc4CCc4cccc(c43)[C@H]2C1 10.1021/np50094a001
5281878 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
5281881 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
948 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
968 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
CHEMBL42055 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
CHEMBL54661 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
DB00875 1630 33 None -11 16 Rat 7.4 pKi = 7.4 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1021/jm9706832
11777127 25606 0 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
CHEMBL135318 25606 0 None 1 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 255 1 2 3 2.7 CN1CCc2cc(O)c(O)cc2C1c1ccccc1 10.1021/jm00051a008
118711256 113455 0 None -37 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1cccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
CHEMBL3325906 113455 0 None -37 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1cccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)c1 10.1016/j.ejmech.2014.07.059
15115516 9676 0 None -1148 2 Human 5.4 pKi = 5.4 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL113527 9676 0 None -1148 2 Human 5.4 pKi = 5.4 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 487 9 2 8 5.4 CCCN(CCc1ccc(Nc2ccc([N+](=O)[O-])c3nonc23)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
53317511 57632 0 None -107 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 329 3 2 4 3.2 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
CHEMBL1672308 57632 0 None -107 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 329 3 2 4 3.2 CN1CCc2cc(OCCF)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
44380816 119845 0 None -77 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL353090 119845 0 None -77 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44448059 94379 0 None 5 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL253530 94379 0 None 5 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
137655451 158307 0 None -288 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4094869 158307 0 None -288 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
3033769 3229 54 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
3299 3229 54 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
94 3229 54 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
CHEMBL8809 3229 54 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
DB12518 3229 54 None -10232 18 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl 10.1016/j.bmc.2007.07.017
10544858 169461 0 None -40 4 Rat 5.4 pKi = 5.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm981094e
CHEMBL444269 169461 0 None -40 4 Rat 5.4 pKi = 5.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm981094e
CHEMBL542181 169461 0 None -40 4 Rat 5.4 pKi = 5.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 336 4 0 4 3.2 COc1ccccc1N1CCN(CC2CC(=O)c3ccccc32)CC1 10.1021/jm981094e
228 441 26 None -35 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
33 441 26 None -35 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
6005 441 26 None -35 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
CHEMBL53 441 26 None -35 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
DB00714 441 26 None -35 24 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assayDisplacement of [3H]SCH23390 from human D1 receptor expressed in L cells incubated for 60 mins by radio ligand binding assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmcl.2020.127053
16573 177045 30 None -18 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
CHEMBL464099 177045 30 None -18 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEKT cell membranes by radioligand binding assay
ChEMBL 341 3 1 5 3.2 COc1cc2c(cc1O)C[C@H]1c3c(cc(OC)c(OC)c3-2)CCN1C 10.1021/np500893h
44320267 204490 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL86576 204490 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
44278297 98619 0 None -2511 3 Rat 4.4 pKi = 4.4 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 382 4 0 2 5.0 O=C(c1cccc(CN2CCC(c3ccc(Cl)cc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
CHEMBL280534 98619 0 None -2511 3 Rat 4.4 pKi = 4.4 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 382 4 0 2 5.0 O=C(c1cccc(CN2CCC(c3ccc(Cl)cc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
130442557 166520 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4289538 166520 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
71110287 145792 0 None - 1 Human 6.4 pKi = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL3921127 145792 0 None - 1 Human 6.4 pKi = 6.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 369 3 0 6 3.1 COc1cc2c(c(OC)c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
235224 127633 24 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
CHEMBL36654 127633 24 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 279 0 0 3 3.2 CN1CCc2cc3c(c4c2C1Cc1ccccc1-4)OCO3 10.1016/j.bmcl.2013.06.078
72708127 91771 0 None -40 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425376 91771 0 None -40 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 283 0 3 4 2.5 Oc1cc2c(cc1O)C1Cc3cccc(O)c3CN1CC2 10.1016/j.ejmech.2013.07.036
44396235 167972 1 None -23 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
CHEMBL435505 167972 1 None -23 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 281 6 0 2 3.8 c1ccc(Cc2ccccc2OCCN2CCCC2)cc1 10.1021/jm049720x
72699718 114696 0 None -11 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 355 3 1 4 4.5 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CCC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344465 114696 0 None -11 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 355 3 1 4 4.5 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CCC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
135458464 80716 0 None -1122 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 486 3 1 5 6.2 FC(F)(F)Oc1cccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c1 10.1016/j.bmcl.2006.06.034
CHEMBL215669 80716 0 None -1122 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 486 3 1 5 6.2 FC(F)(F)Oc1cccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c1 10.1016/j.bmcl.2006.06.034
46231783 198849 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 357 1 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C(=O)O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
CHEMBL598915 198849 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 357 1 2 3 3.7 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(C(=O)O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.094
130442473 166783 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4294397 166783 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.8b01622
86764318 131938 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 349 4 1 5 3.1 Cc1c(-c2ccc(Oc3ncccc3C3CC3)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697600 131938 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 349 4 1 5 3.1 Cc1c(-c2ccc(Oc3ncccc3C3CC3)cc2)n(C)c(=O)[nH]c1=O nan
117773358 131895 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 3 1 5 4.2 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697558 131895 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 3 1 5 4.2 Cc1cc(Oc2ncc(Cl)c(C)c2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
23625925 93138 0 None -18 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
CHEMBL246484 93138 0 None -18 7 Human 7.4 pKi = 7.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 368 3 1 5 3.3 O=C1CC(CN2CCC(c3noc4cc(F)ccc34)CC2)Cc2[nH]ncc21 10.1039/C1MD00202C
10436653 32573 0 None -562 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
CHEMBL141419 32573 0 None -562 5 Human 6.4 pKi = 6.4 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 521 8 1 4 3.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[te]2)CC1 10.1021/jm025558r
147230103 179573 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2020.127563
CHEMBL4748915 179573 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 323 1 1 3 4.8 CN1CC=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CC1 10.1016/j.bmcl.2020.127563
53327908 61280 0 None -3162 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771112 61280 0 None -3162 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 470 8 0 5 4.4 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccncc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
3082625 193060 6 None -199 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL53510 193060 6 None -199 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm060959i
53327665 66147 0 None -38 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
CHEMBL1852240 66147 0 None -38 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
CHEMBL3216759 66147 0 None -38 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 400 4 3 7 2.4 COC(=O)[C@@H](N)CSc1cc2c3c(c1)-c1c(ccc(O)c1O)C[C@H]3N(C)CC2 10.1016/j.ejmech.2011.04.028
128434 194033 8 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 227 1 3 3 2.2 NCC1c2ccccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
CHEMBL55693 194033 8 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 227 1 3 3 2.2 NCC1c2ccccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
10386748 104273 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
CHEMBL310734 104273 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
10386748 104273 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL310734 104273 0 None -15 3 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 408 7 0 4 3.9 O=C(CCCN1CCN(CC2CC(=O)c3ccccc3C2)CC1)c1ccc(F)cc1 10.1021/jm981094e
53363199 63521 0 None -457 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803051 63521 0 None -457 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 481 12 0 9 3.2 CCOCCn1cc(COc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
25139477 183663 0 None -870 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL483593 183663 0 None -870 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 486 10 1 2 6.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
49782603 17307 0 None -151 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1257811 17307 0 None -151 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 385 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
137634397 155564 0 None -11748 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 155564 0 None -11748 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
10802235 13148 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1191487 13148 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL542593 13148 0 None -1 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2 10.1021/jm970038v
72545238 92695 0 None -7413 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443005 92695 0 None -7413 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 425 9 0 7 3.3 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
112500028 131943 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697605 131943 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 0 5 3.9 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)ncc(=O)n1C nan
56971032 68907 0 None -114 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccccn1 10.1016/j.ejmech.2011.11.023
CHEMBL1927094 68907 0 None -114 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 382 6 1 5 2.8 N#C/N=C(\NCCCN1CCN(c2cccc(Cl)c2)CC1)c1ccccn1 10.1016/j.ejmech.2011.11.023
3082625 193060 6 None -199 4 Rat 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00004a011
CHEMBL53510 193060 6 None -199 4 Rat 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1Ability to displace [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm00004a011
3082625 193060 6 None -199 4 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL53510 193060 6 None -199 4 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
44582675 189109 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189109 0 None -64 15 Human 5.4 pKi = 5.4 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
10786190 114234 0 None -50 3 Rat 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 383 2 0 4 3.7 CN1CCc2cccc3c2[C@H]1Cc1cccc(OS(=O)(=O)C(F)(F)F)c1-3 10.1021/jm960189i
CHEMBL333836 114234 0 None -50 3 Rat 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 383 2 0 4 3.7 CN1CCc2cccc3c2[C@H]1Cc1cccc(OS(=O)(=O)C(F)(F)F)c1-3 10.1021/jm960189i
44406003 132637 0 None 4 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
CHEMBL370364 132637 0 None 4 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 463 5 2 5 3.5 Cc1ccc(-c2cc3c(=O)n(CCN4CCN(c5ccccc5Cl)CC4)c(=O)[nH]c3[nH]2)cc1 10.1016/j.bmcl.2005.09.027
448537 159703 86 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
CHEMBL411 159703 86 None -28 25 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 nan
10813037 46893 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 439 3 1 3 4.7 COc1ccc(Br)c(CC2c3c(O)ccc(Br)c3CCN2C)c1 10.1021/jm991034o
CHEMBL154301 46893 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 439 3 1 3 4.7 COc1ccc(Br)c(CC2c3c(O)ccc(Br)c3CCN2C)c1 10.1021/jm991034o
90644059 111538 0 None -22 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289643 111538 0 None -22 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 354 4 0 3 3.9 O=C1c2ccccc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
10781204 119544 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 309 3 0 3 4.4 CCCN1CCc2cccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
CHEMBL350457 119544 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 309 3 0 3 4.4 CCCN1CCc2cccc3c2C1Cc1cc(OC)ccc1O3 10.1021/jm991034o
76321556 105896 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 105896 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 105896 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
76325150 105941 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 105941 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 105941 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
44415658 141040 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 527 3 1 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3sccc3-c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL384916 141040 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 527 3 1 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3sccc3-c3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
25110706 12496 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 345 2 3 3 4.4 Cc1cccc(-c2c(O)c(O)cc3c2CCNCC3c2ccccc2)c1 10.1016/j.bmc.2008.09.049
CHEMBL1186960 12496 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 345 2 3 3 4.4 Cc1cccc(-c2c(O)c(O)cc3c2CCNCC3c2ccccc2)c1 10.1016/j.bmc.2008.09.049
CHEMBL484356 12496 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 345 2 3 3 4.4 Cc1cccc(-c2c(O)c(O)cc3c2CCNCC3c2ccccc2)c1 10.1016/j.bmc.2008.09.049
86767096 128906 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C#N nan
CHEMBL3671285 128906 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.3 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncnc1C#N nan
2337 3205 72 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
50 3205 72 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
5002 3205 72 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
CHEMBL716 3205 72 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
DB01224 3205 72 None -53 62 Human 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm0002432
44276572 96200 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL26365 96200 0 None 2 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
53364225 63514 0 None -117 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803027 63514 0 None -117 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 932 25 0 18 5.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCc1cn(CCOCCOCCn2cc(COc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
30133 67296 6 None -6 3 Rat 6.4 pKi = 6.4 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 253 0 3 3 2.5 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm00163a007
CHEMBL190519 67296 6 None -6 3 Rat 6.4 pKi = 6.4 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 253 0 3 3 2.5 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm00163a007
CHEMBL541862 67296 6 None -6 3 Rat 6.4 pKi = 6.4 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 253 0 3 3 2.5 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)NCC3 10.1021/jm00163a007
10667966 56865 0 None -2 4 Bovine 5.4 pKi = 5.4 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
CHEMBL164736 56865 0 None -2 4 Bovine 5.4 pKi = 5.4 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 387 5 0 1 6.1 CCCN(CCC)C1CCC(=C(C#C[Si](C)(C)C)C#C[Si](C)(C)C)CC1 10.1021/jm991098z
44412182 76913 0 None -3890 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL208018 76913 0 None -3890 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1nn(-c2ccccc2)cc1CN1CCN(c2ccccc2)CC1 10.1016/j.bmcl.2006.02.075
122177642 120697 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
CHEMBL3577343 120697 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 551 18 1 8 4.6 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2ccc(OCCCc3cn(CCCC)nn3)c(OC)c2)CO1 10.1021/jm501889t
24823921 97447 0 None -21 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
CHEMBL272395 97447 0 None -21 4 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 371 3 0 5 2.8 Brc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
9995378 5399 0 None -301 4 Bovine 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
CHEMBL107529 5399 0 None -301 4 Bovine 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 307 4 0 4 4.0 c1ccc(CN2CCC(n3ccc(-c4cnco4)c3)CC2)cc1 10.1016/s0960-894x(99)00540-5
10359539 58745 6 None -125 4 Bovine 4.4 pKi = 4.4 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
CHEMBL169459 58745 6 None -125 4 Bovine 4.4 pKi = 4.4 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 334 4 1 4 2.6 c1ccc(C2=NCC[C@@H](CN3CCN(c4ccccc4)CC3)N2)cc1 10.1016/s0960-894x(03)00004-0
91899759 128923 0 None - 1 Human 6.4 pKi = 6.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 342 3 1 6 3.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1C#N nan
CHEMBL3671300 128923 0 None - 1 Human 6.4 pKi = 6.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 342 3 1 6 3.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1C#N nan
57580939 91769 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
CHEMBL2425374 91769 0 None -10 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1cc2c(cc1OC)C1Cc3cccc(OC)c3CN1CC2 10.1016/j.ejmech.2013.07.036
1242 3556 23 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
935 3556 23 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
CHEMBL286080 3556 23 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.bmc.2009.06.019
1242 3556 23 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.ejmech.2014.07.059
935 3556 23 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.ejmech.2014.07.059
CHEMBL286080 3556 23 None -5 17 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1016/j.ejmech.2014.07.059
10333837 113035 0 None -51 3 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 0 2 3.8 COc1c(C)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL332178 113035 0 None -51 3 Rat 6.4 pKi = 6.4 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 0 2 3.8 COc1c(C)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
25130157 102832 0 None -5495 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
CHEMBL3084515 102832 0 None -5495 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 367 3 1 3 5.1 O[C@]1(c2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2Cc1coc2ccccc12 10.1021/jm800532x
135409492 168604 46 None -4 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 0 1 5 3.5 Cc1cc2c(s1)Nc1ccccc1N=C2N1CC[N+](C)([O-])CC1 10.1016/S0960-894X(96)00567-7
CHEMBL440512 168604 46 None -4 3 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 0 1 5 3.5 Cc1cc2c(s1)Nc1ccccc1N=C2N1CC[N+](C)([O-])CC1 10.1016/S0960-894X(96)00567-7
15467370 101848 0 None -3630 4 Bovine 4.4 pKi = 4.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL303538 101848 0 None -3630 4 Bovine 4.4 pKi = 4.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccc(Cl)cc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
76321556 105896 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115578 105896 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139302 105896 0 None -407 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 493 6 2 5 3.1 Oc1ccc2c(c1)O[C@@H](CNCCN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
151086 91546 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
CHEMBL2414991 91546 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
3802 201334 16 None -19 5 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
CHEMBL63329 201334 16 None -19 5 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm960084f
3802 201334 16 None -19 5 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm00067a009
CHEMBL63329 201334 16 None -19 5 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 1 5 2.8 Cc1ccc2c(c1)C(N1CCN(C)CC1)=Nc1cccnc1N2 10.1021/jm00067a009
4302960 100592 57 None -1258 6 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL294747 100592 57 None -1258 6 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 485 10 1 5 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccc(C(C)=O)cc3)cc2)CC1 10.1016/0960-894X(95)00011-H
10247701 85456 0 None -2398 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 4 1 3 4.1 c1ccc2c(N3CCN(CCc4ccc5[nH]cnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
CHEMBL2298806 85456 0 None -2398 5 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 356 4 1 3 4.1 c1ccc2c(N3CCN(CCc4ccc5[nH]cnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
162657175 180251 0 None 41 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 331 2 1 3 5.1 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4756987 180251 0 None 41 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 331 2 1 3 5.1 CCc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
16007117 79626 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212912 79626 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415518 79668 0 None 45 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213084 79668 0 None 45 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(Cl)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415724 79848 0 None 97 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 547 2 1 5 6.4 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cc(Cl)cc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213881 79848 0 None 97 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 547 2 1 5 6.4 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(Cl)cc(Cl)cc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11637457 72740 1 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
CHEMBL201093 72740 1 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2ccsc2CC1 10.1039/C5MD00258C
71562964 87147 0 None 3 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335740 87147 0 None 3 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
37459 735 10 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127305
62 735 10 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127305
CHEMBL8514 735 10 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmcl.2020.127305
16007117 79626 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212912 79626 0 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 479 2 1 5 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
15111049 13842 0 None 1412 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 317 1 2 2 3.4 Oc1cc2c(cc1Br)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL1196674 13842 0 None 1412 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 317 1 2 2 3.4 Oc1cc2c(cc1Br)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL557799 13842 0 None 1412 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 317 1 2 2 3.4 Oc1cc2c(cc1Br)CCNCC2c1ccccc1 10.1021/jm00079a008
74223771 128898 0 None - 1 Human 8.4 pKi = 8.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
CHEMBL3671277 128898 0 None - 1 Human 8.4 pKi = 8.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
86764214 131934 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 4 1 5 4.6 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)(F)F nan
CHEMBL3697596 131934 0 None - 1 Human 8.4 pKi = 8.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 405 4 1 5 4.6 COc1ccnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)c(C)c2)c1C(F)(F)F nan
71109897 87085 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL2334893 87085 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 10.1016/j.bmc.2012.12.016
134145434 148877 0 None 173 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 449 5 2 6 3.6 COCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3945691 148877 0 None 173 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 449 5 2 6 3.6 COCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
45379369 7441 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
CHEMBL1087300 7441 0 None -1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation countingDisplacement of [3H]SCH23390 from human recombinant dopamine D1 receptor expressed in HEK293 cells by microplate scintillation counting
ChEMBL 290 0 1 1 3.8 CN1CCc2ccccc2Cc2c[nH]c3cccc(c23)CC1 10.1021/jm901291r
71109897 87085 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
CHEMBL2334893 87085 0 None 7 2 Human 8.4 pKi = 8.4 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 325 1 1 5 2.8 COc1cc2c(cc1O)[C@@H]1Cc3cc4c(cc3CN1CC2)OCO4 nan
37459 735 10 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2020.115578
62 735 10 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2020.115578
CHEMBL8514 735 10 None -10 24 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting methodDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in HEKT cells incubated for 90 mins by microbeta counting method
ChEMBL 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 10.1016/j.bmc.2020.115578
10518837 100007 0 None 33 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL290842 100007 0 None 33 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2 10.1021/jm970038v
46231924 198894 0 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
CHEMBL599134 198894 0 None 5 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation countingDisplacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting
ChEMBL 370 2 1 4 4.0 CO/N=C/c1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.094
5249956 73048 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
CHEMBL201525 73048 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cellsDisplacement of [3H]SCH 23390 from human cloned dopamine D1 receptor expressed in HEK 293 cells
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1016/j.bmcl.2006.11.093
5249956 73048 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
CHEMBL201525 73048 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1039/C5MD00258C
440229 87083 48 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2334891 87083 48 None 1 5 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
5249956 73048 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
CHEMBL201525 73048 1 None -4 6 Human 8.4 pKi = 8.4 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 251 0 0 1 3.3 CN1CCc2ccccc2Cc2ccccc2CC1 10.1021/jm050846j
74223826 128915 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671293 128915 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 5 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc(=O)n1C nan
228 441 26 None -35 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
33 441 26 None -35 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
6005 441 26 None -35 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL53 441 26 None -35 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
DB00714 441 26 None -35 24 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
86767083 128889 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 4 5.3 [C-]#[N+]c1c[nH]c2ccnc(Oc3ccc(-c4c(C)ncnc4C)c(C)c3)c12 nan
CHEMBL3671268 128889 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 4 5.3 [C-]#[N+]c1c[nH]c2ccnc(Oc3ccc(-c4c(C)ncnc4C)c(C)c3)c12 nan
44323851 205246 0 None 3 4 Rat 8.3 pKi = 8.3 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL91310 205246 0 None 3 4 Rat 8.3 pKi = 8.3 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 302 1 0 2 3.8 C=C1c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
46231770 199625 0 None 213 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NS(C)(=O)=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL604135 199625 0 None 213 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 406 2 2 4 3.4 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NS(C)(=O)=O)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
74223772 128900 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671279 128900 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
25110705 12631 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 409 2 2 3 5.8 Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL1187785 12631 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 409 2 2 3 5.8 Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL520821 12631 0 None 5 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 409 2 2 3 5.8 Cc1cccc(C2CN(C)CCc3c2cc(O)c(O)c3-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2008.09.049
146266 100231 7 None -2 4 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL292418 100231 7 None -2 4 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00079a008
CHEMBL540857 100231 7 None -2 4 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1 10.1021/jm00079a008
11324141 63527 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 303 1 0 5 3.2 CN1CCN(C2=Cn3cccc3Sc3sccc32)CC1 10.1021/jm049629t
CHEMBL180319 63527 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 303 1 0 5 3.2 CN1CCN(C2=Cn3cccc3Sc3sccc32)CC1 10.1021/jm049629t
44386836 62693 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 342 3 0 4 3.6 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
CHEMBL178797 62693 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 342 3 0 4 3.6 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CN(C)CC2 10.1016/s0960-894x(98)00138-3
1153 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
12668023 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
30026874 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
30026875 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
3341 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
6603851 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
933 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
939 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
985 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
CHEMBL1160786 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
CHEMBL1161520 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
CHEMBL588 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
DB00800 1598 53 None -32 10 Human 7.4 pKi = 7.4 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1021/jm9800292
122205438 136875 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
CHEMBL3753266 136875 0 None -26 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 307 0 0 2 4.5 CN1CCc2ccccc2Cc2sc3ccccc3c2CC1 10.1039/C5MD00258C
71722299 102007 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397383 102007 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040217 102007 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
127031398 138278 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 411 8 1 5 5.0 CCCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3781035 138278 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 411 8 1 5 5.0 CCCCCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
14198584 196592 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL57579 196592 0 None 12 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2C1c1ccccc1 10.1016/j.bmc.2009.05.079
86763998 131952 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697614 131952 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 375 3 1 5 3.3 Cc1cc(Oc2ncc(F)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
74223832 128929 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
CHEMBL3671306 128929 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 333 3 2 5 3.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1 nan
53364083 63523 0 None -28 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803053 63523 0 None -28 4 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 658 21 0 11 6.2 CCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
44339992 108697 0 None -501 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 108697 0 None -501 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
49782841 17470 0 None -2511 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
CHEMBL1258382 17470 0 None -2511 5 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 523 7 1 4 6.1 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccccc2s1 10.1021/jm100899z
137633454 156050 0 None -1230 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
CHEMBL4068702 156050 0 None -1230 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 645 16 3 10 4.4 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN3CCCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2OC)nn1 10.1021/acs.jmedchem.7b00363
71454405 78016 0 None -30 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL2111528 78016 0 None -30 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
44319102 204421 0 None -16 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 204421 0 None -16 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
11631892 77757 0 None -30902 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
CHEMBL210283 77757 0 None -30902 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 4 0 6 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(C#N)c3n2)CC1 10.1021/jm060166w
151086 91546 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
CHEMBL2414991 91546 4 None -9 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1-3 10.1016/j.bmcl.2013.06.078
4011 81996 43 None -64 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
CHEMBL21731 81996 43 None -64 23 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1016/j.bmcl.2008.09.012
118717796 114694 0 None -14 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 4 1 4 4.7 CCC(C)Cc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344462 114694 0 None -14 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 4 1 4 4.7 CCC(C)Cc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
11349297 85453 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 372 5 2 4 2.7 O=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298800 85453 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 372 5 2 4 2.7 O=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
72708060 91765 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425370 91765 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
44320123 106599 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL315849 106599 0 None 2 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
72708060 91765 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425370 91765 0 None 1 2 Rat 4.4 pKi = 4.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 477 7 0 4 6.5 COc1ccc2c(c1)CC1c3cc(OCc4ccccc4)c(OCc4ccccc4)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
70692801 76210 0 None -5 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062850 76210 0 None -5 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 362 5 1 3 3.6 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCC1 10.1016/j.ejmech.2012.07.025
118709751 113042 0 None -3162 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
CHEMBL3321792 113042 0 None -3162 10 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 405 6 1 3 5.5 OC1(c2ccc(Cl)cc2)CC2CCC(C1)N2CCCSc1ccccc1F 10.1016/j.bmcl.2014.07.018
156020547 177584 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 387 4 1 3 4.3 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4649012 177584 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 387 4 1 3 4.3 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
74223830 128928 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3671305 128928 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 6 3.1 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)ncc(=O)n1C nan
9909648 203861 1 None -134 12 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
CHEMBL81330 203861 1 None -134 12 Rat 6.4 pKi = 6.4 Binding
Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.Binding affinity of [3H]SCH-23,390 towards Dopamine receptor D1 in cloned mammalian receptor expressed in cultured cells or from rat whole brain.
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm960084f
71463207 83660 0 None -169 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207636 83660 0 None -169 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 357 4 0 4 4.0 COc1ccccc1N1CCN(Cc2cc(C#N)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
137640203 156420 0 None -54 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
CHEMBL4072821 156420 0 None -54 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 452 10 0 8 3.5 CCOC(=O)c1cc2cc(OCCCCN3CCN(c4ccccc4OC)CC3)ccn2n1 10.1021/acs.jmedchem.6b01857
10917920 110958 0 None -5128 10 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 110958 0 None -5128 10 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
45482151 196332 0 None -831 4 Pig 5.4 pKi = 5.4 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
CHEMBL573791 196332 0 None -831 4 Pig 5.4 pKi = 5.4 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 451 8 1 9 1.7 COc1ccccc1N1CCN(CCNC(=O)c2cn(-c3ccc([N+](=O)[O-])cc3)nn2)CC1 10.1016/j.bmc.2009.06.041
44403220 71582 0 None -169 5 Pig 5.4 pKi = 5.4 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL197214 71582 0 None -169 5 Pig 5.4 pKi = 5.4 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(F)n2)CC1 10.1016/j.bmcl.2005.07.037
44380921 58021 0 None -11 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
CHEMBL168274 58021 0 None -11 4 Bovine 5.4 pKi = 5.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 9 2 4 4.7 CCC[C@H]1CN(Cc2ccccc2)C[C@@H]1CNC(=O)c1cc(Cl)c(NC)cc1OC 10.1016/s0960-894x(99)00086-4
9977532 110703 0 None -9999 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 110703 0 None -9999 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
71457844 83662 0 None -2137 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207638 83662 0 None -2137 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 429 6 0 4 5.1 COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
44381117 57526 0 None -120 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL167032 57526 0 None -120 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 415 7 2 4 3.6 COc1cc(NC(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
9909648 203861 1 None -134 12 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
CHEMBL81330 203861 1 None -134 12 Human 6.4 pKi = 6.4 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 340 4 0 3 3.7 Fc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/acs.jmedchem.7b00151
161379 186632 6 None -79 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
CHEMBL492418 186632 6 None -79 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
681 1437 65 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
940 1437 65 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
947 1437 65 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
CHEMBL59 1437 65 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
DB00988 1437 65 None -97 38 Rat 6.4 pKi = 6.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991034o
10085358 109730 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
CHEMBL323771 109730 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
76328713 105923 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3115576 105923 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3139455 105923 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
1816 2504 99 None -323 16 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
4205 2504 99 None -323 16 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
7241 2504 99 None -323 16 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
CHEMBL654 2504 99 None -323 16 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
DB00370 2504 99 None -323 16 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 10.1021/jm049632c
21119297 91768 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425373 91768 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
44299940 100499 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
CHEMBL294186 100499 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 309 1 1 3 3.3 COc1cc2c(cc1O)[C@@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
44415535 79740 0 None 42 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213388 79740 0 None 42 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 5 4.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
24900557 196710 0 None -17 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 409 4 1 7 3.4 CNc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
CHEMBL576756 196710 0 None -17 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 409 4 1 7 3.4 CNc1ncc2c(n1)CC(CN1CCC(c3noc4cc(F)ccc34)CC1)CC2=O 10.1016/j.bmcl.2009.09.041
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00302-9
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(02)00316-5
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm015522j
44393403 64747 0 None -416 6 Pig 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182379 64747 0 None -416 6 Pig 6.4 pKi = 6.4 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1016/j.bmcl.2004.05.052
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(98)00692-1
135398737 944 89 None -37 91 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
38 944 89 None -37 91 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
722 944 89 None -37 91 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
CHEMBL42 944 89 None -37 91 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
DB00363 944 89 None -37 91 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm060166w
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0009989
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(99)00540-5
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmc.2009.05.015
57393628 68971 0 None -1230 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928137 68971 0 None -1230 5 Pig 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 5.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(OCCOCCOCCOCCOc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(01)00814-9
135398737 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
38 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
722 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
CHEMBL42 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
DB00363 944 89 None -204 91 Bovine 6.4 pKi = 6.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/s0960-894x(00)00405-4
44339984 167234 0 None -186 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 167234 0 None -186 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
53362841 63630 0 None -16 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
CHEMBL1806870 63630 0 None -16 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells after 50 mins by beta liquid scintillation counter
ChEMBL 412 5 1 3 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OC(=O)NCc2ccccc2)c1-3 10.1021/jm200347t
53328719 66139 0 None -20 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL1852163 66139 0 None -20 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
CHEMBL3216980 66139 0 None -20 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 386 4 4 6 2.4 CN1CCc2cc(SC[C@H](N)C(=O)O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.ejmech.2011.04.028
70690651 76208 0 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]21 10.1016/j.ejmech.2012.07.025
CHEMBL2062848 76208 0 None -3 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 364 7 1 3 3.8 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]21 10.1016/j.ejmech.2012.07.025
44588932 12500 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 2 3 3 4.2 Oc1cc2c(c(-c3ccc(F)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186975 12500 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 2 3 3 4.2 Oc1cc2c(c(-c3ccc(F)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL485041 12500 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 349 2 3 3 4.2 Oc1cc2c(c(-c3ccc(F)cc3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
68663 27075 17 None -5 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
CHEMBL136711 27075 17 None -5 3 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 10.1016/j.bmc.2007.07.018
2337 3205 72 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
50 3205 72 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
5002 3205 72 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
CHEMBL716 3205 72 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
DB01224 3205 72 None -53 62 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1021/jm030480f
1016 3690 75 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2561 3690 75 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
2733526 3690 75 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
5384 3690 75 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
CHEMBL83 3690 75 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
DB00675 3690 75 None -29 35 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 nan
44582140 181916 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 7 0 4 3.3 COc1cccc(N2CCN(CCCCN3CCc4ccccc4C3=O)CC2)c1 10.1016/j.bmcl.2009.01.067
CHEMBL478688 181916 0 None -10 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 393 7 0 4 3.3 COc1cccc(N2CCN(CCCCN3CCc4ccccc4C3=O)CC2)c1 10.1016/j.bmcl.2009.01.067
44327167 9288 0 None -3 4 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL111393 9288 0 None -3 4 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm981094e
CHEMBL544319 9288 0 None -3 4 Rat 6.4 pKi = 6.4 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 371 4 0 4 4.2 O=C1CC(CN2CCC(C(=O)c3ccc(F)cc3)CC2)Cc2sccc21 10.1021/jm981094e
10516949 47655 0 None 2 2 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1cc2c3c(c1)Oc1ccccc1CC3N(C)CC2 10.1021/jm991034o
CHEMBL154948 47655 0 None 2 2 Rat 5.4 pKi = 5.4 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1cc2c3c(c1)Oc1ccccc1CC3N(C)CC2 10.1021/jm991034o
117774121 131925 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 384 4 1 6 3.0 Cc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C#N)n(C)c(=O)[nH]c1=O nan
CHEMBL3697588 131925 0 None - 1 Human 6.4 pKi = 6.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 384 4 1 6 3.0 Cc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C#N)n(C)c(=O)[nH]c1=O nan
9945168 123148 0 None -41 3 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 325 2 0 5 3.0 CN1CCN(C2=Cn3c(C=O)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
CHEMBL362060 123148 0 None -41 3 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 325 2 0 5 3.0 CN1CCN(C2=Cn3c(C=O)ccc3Sc3ccccc32)CC1 10.1021/jm0309811
76325150 105941 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3115575 105941 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
CHEMBL3139554 105941 0 None -4265 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1cccc(I)c1)CC2 10.1021/jm401384w
135398737 944 89 None -83 91 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
38 944 89 None -83 91 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
722 944 89 None -83 91 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
CHEMBL42 944 89 None -83 91 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
DB00363 944 89 None -83 91 Rat 7.4 pKi = 7.4 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm00043a008
124618 196703 7 None 134 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 243 1 4 4 1.9 NCC1c2cc(O)ccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
CHEMBL57672 196703 7 None 134 2 Rat 7.4 pKi = 7.4 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 243 1 4 4 1.9 NCC1c2cc(O)ccc2-c2c1ccc(O)c2O 10.1021/jm00160a018
86764319 131942 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697604 131942 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 0 5 4.2 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)ncc(=O)n1C nan
127047221 139400 0 None -1 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 139400 0 None -1 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
127046950 139515 0 None -23 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800303 139515 0 None -23 6 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
25071385 158611 0 None -208 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098236 158611 0 None -208 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C=O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
681 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
940 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
947 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
CHEMBL59 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
DB00988 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm9708700
681 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
940 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
947 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
CHEMBL59 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
DB00988 1437 65 None -23 38 Bovine 5.4 pKi = 5.4 Binding
Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retinaBinding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/s0960-894x(00)00633-8
10333842 97979 1 None -31 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
CHEMBL27559 97979 1 None -31 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/ml1001689
44448070 94452 0 None 3 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL254147 94452 0 None 3 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 10.1021/jm060959i
25071691 111295 0 None -2818 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111295 0 None -2818 5 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
72545239 92696 0 None -426 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443006 92696 0 None -426 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 499 14 0 9 3.0 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCOCCOCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
21119297 91768 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425373 91768 0 None 1 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 325 3 0 4 3.4 COc1ccc2c(c1)CC1c3cc(OC)c(OC)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
25186021 187441 0 None -1318 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/jm800689g
CHEMBL497574 187441 0 None -1318 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 10.1021/jm800689g
10333842 97979 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
CHEMBL27559 97979 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390Binding affinity against Dopamine receptor D1 from rat brain corpus striatal preparations using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00402a024
10333842 97979 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
CHEMBL27559 97979 1 None -50 8 Rat 6.4 pKi = 6.4 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
1530 2151 44 None -53 20 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
3827 2151 44 None -53 20 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
7206 2151 44 None -53 20 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
CHEMBL534 2151 44 None -53 20 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
DB00920 2151 44 None -53 20 Human 6.4 pKi = 6.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 nan
76328713 105923 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3115576 105923 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
CHEMBL3139455 105923 0 None -251 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1I)CC2 10.1021/jm401384w
71722291 101987 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397385 101987 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040059 101987 0 None -3 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
11712530 187307 0 None -41686 4 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm800689g
CHEMBL496531 187307 0 None -41686 4 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 10.1021/jm800689g
135398737 944 89 None -44 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
38 944 89 None -44 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
722 944 89 None -44 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
CHEMBL42 944 89 None -44 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
DB00363 944 89 None -44 91 Human 7.4 pKi = 7.4 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2020.127563
44415849 140881 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 509 3 1 6 5.1 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
CHEMBL384069 140881 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 509 3 1 6 5.1 COc1cccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
86764104 131960 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697622 131960 0 None - 1 Human 7.4 pKi = 7.4 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
74223775 128909 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 316 3 1 4 4.4 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
CHEMBL3671288 128909 0 None - 1 Human 7.4 pKi = 7.4 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 316 3 1 4 4.4 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1 nan
681 1437 65 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
940 1437 65 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
947 1437 65 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
CHEMBL59 1437 65 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
DB00988 1437 65 None -23 38 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/j.bmc.2013.01.065
137657115 159208 0 None -173 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4105030 159208 0 None -173 5 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(/C=N/O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
10831251 162623 0 None 4 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL41809 162623 0 None 4 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44340084 9000 0 None -2238 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 9000 0 None -2238 4 Bovine 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
25131137 186964 0 None -190 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 558 9 2 5 7.4 Nc1nc2c(s1)C[C@@H](N(CCC1CCCCC1)CC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
CHEMBL494509 186964 0 None -190 3 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 558 9 2 5 7.4 Nc1nc2c(s1)C[C@@H](N(CCC1CCCCC1)CC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
681 1437 65 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
940 1437 65 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
947 1437 65 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
CHEMBL59 1437 65 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
DB00988 1437 65 None -97 38 Rat 5.4 pKi = 5.4 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm00160a016
70696888 76220 0 None -8 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062860 76220 0 None -8 3 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@H]1[C@H]2CN(Cc3ccccc3)[C@H](c3ccccc3)[C@H]2[C@@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
44329039 206396 0 None -56 3 Bovine 4.4 pKi = 4.4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL98072 206396 0 None -56 3 Bovine 4.4 pKi = 4.4 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
14198585 100334 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 100334 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
14198585 100334 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00118a012
CHEMBL293158 100334 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00118a012
44320076 204700 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87910 204700 0 None 3 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
11282465 192516 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL522746 192516 1 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
11406615 85476 0 None -162 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 388 5 2 4 4.1 S=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
CHEMBL2298832 85476 0 None -162 2 Human 6.4 pKi = 6.4 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 388 5 2 4 4.1 S=c1[nH]c2ccc(OCCN3CCN(c4ccccc4Cl)CC3)cc2[nH]1 10.1007/s00044-012-0055-5
14198585 100334 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 100334 1 None 1 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
14198585 100334 1 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00129a006
CHEMBL293158 100334 1 None -1 4 Human 6.4 pKi = 6.4 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00129a006
44415759 141156 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 3 1 5 6.5 CC(C)(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL385590 141156 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 535 3 1 5 6.5 CC(C)(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
681 1437 65 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
940 1437 65 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
947 1437 65 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
CHEMBL59 1437 65 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
DB00988 1437 65 None -154 38 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm301258w
44276551 96927 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL26965 96927 0 None 10 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
10333842 97979 1 None -31 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmc.2008.08.056
CHEMBL27559 97979 1 None -31 8 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]8OH-DPAT from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmc.2008.08.056
10588327 13669 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL1195441 13669 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
CHEMBL554571 13669 0 None 22 2 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2 10.1021/jm970038v
72699903 114700 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)Cl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344469 114700 0 None -2 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 3 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)Cl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
122197088 131893 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 362 3 1 5 3.4 [C-]#[N+]c1c(C)ccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
CHEMBL3697556 131893 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 362 3 1 5 3.4 [C-]#[N+]c1c(C)ccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
71563082 86853 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2331599 86853 0 None 2 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
9908125 118839 0 None -20 4 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
CHEMBL344270 118839 0 None -20 4 Bovine 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)c2c1 10.1021/jm0009989
11016418 105642 0 None -7244 9 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 105642 0 None -7244 9 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
71456046 83661 0 None -2951 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207637 83661 0 None -2951 7 Pig 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 389 6 0 4 4.2 COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
127045853 139263 0 None -17782 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3798748 139263 0 None -17782 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
137655795 158036 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4091933 158036 0 None -1778 6 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 453 7 2 7 3.0 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5c4OCCO5)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
12050201 201185 0 None -31 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL62624 201185 0 None -31 4 Bovine 5.4 pKi = 5.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 7 1 5 5.3 COc1ccc(Br)cc1-c1nc(CNC2CCN(Cc3ccccc3)CC2)cs1 10.1016/s0960-894x(00)00405-4
44319361 204007 0 None -7 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL82527 204007 0 None -7 4 Bovine 5.4 pKi = 5.4 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 337 4 0 4 3.4 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CS2)cc1 10.1016/s0960-894x(01)00484-x
44264629 96917 0 None -316 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL269576 96917 0 None -316 4 Bovine 4.4 pKi = 4.4 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4c3ccc3ccccc34)CC2)cc1 10.1016/s0960-894x(98)00692-1
72545011 92694 0 None -3162 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443004 92694 0 None -3162 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 411 8 0 7 2.9 COc1ccccc1N1CCN(Cc2cn(-c3ccc(OCCF)cc3)nn2)CC1 10.1016/j.bmcl.2013.09.026
42606339 17749 0 None -97 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1259241 17749 0 None -97 5 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 397 5 1 4 4.3 Cc1ccc(CNCC2(F)CCN(C(=O)c3csc4ccccc34)CC2)nc1 10.1021/jm100835q
71734126 90623 0 None -4466 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
CHEMBL2397391 90623 0 None -4466 4 Pig 4.4 pKi = 4.4 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 378 9 1 4 3.7 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm400520c
2812 4711 96 None -32 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4711 96 None -32 34 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
127027737 137460 0 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 342 6 1 4 2.2 O=C(NCCCN1CCN(c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
CHEMBL3764420 137460 0 None -4 2 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysisDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum incubated for 15 mins by liquid scintillation counting analysis
ChEMBL 342 6 1 4 2.2 O=C(NCCCN1CCN(c2ccc(F)cc2)CC1)c1ccncc1 10.1016/j.ejmech.2016.01.021
44399174 67670 0 None -870 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatumInhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatum
ChEMBL 449 6 0 5 3.0 O=C1C2C3C=CC(C3)C2C(=O)N1OCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm050246k
CHEMBL191226 67670 0 None -870 4 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatumInhibition of [3H]SCH-23,390 binding to Dopamine D1 receptor from rat striatum
ChEMBL 449 6 0 5 3.0 O=C1C2C3C=CC(C3)C2C(=O)N1OCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1021/jm050246k
44282127 116069 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 309 3 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL1743804 116069 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 309 3 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL33644 116069 0 None -1 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 309 3 0 3 4.0 COc1cc2c(cc1OC)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
3083157 62707 2 None -229 2 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 277 2 1 2 3.7 C=CCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
CHEMBL1788212 62707 2 None -229 2 Rat 6.3 pKi = 6.3 Binding
Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 277 2 1 2 3.7 C=CCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm00105a005
15711852 13228 0 None 5 3 Goldfish 6.3 pKi = 6.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL1192193 13228 0 None 5 3 Goldfish 6.3 pKi = 6.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
CHEMBL543389 13228 0 None 5 3 Goldfish 6.3 pKi = 6.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 317 5 2 3 4.3 CCCNC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(C)c2O 10.1021/jm00114a002
176 394 63 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 394 63 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 394 63 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 394 63 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 394 63 None -4 31 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
145968810 164486 0 None -120 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 164486 0 None -120 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
15937731 116987 6 None 5 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 211 0 1 2 2.1 CN1CCc2cc(O)c(Cl)cc2CC1 10.1016/S0960-894X(00)80155-9
CHEMBL340006 116987 6 None 5 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 211 0 1 2 2.1 CN1CCc2cc(O)c(Cl)cc2CC1 10.1016/S0960-894X(00)80155-9
24766199 97075 0 None -1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm701045j
CHEMBL270426 97075 0 None -1 5 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm701045j
24766199 97075 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm9015763
CHEMBL270426 97075 0 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 281 1 1 3 3.2 COc1cc2c3c(c1)-c1c(O)cccc1C[C@H]3N(C)CC2 10.1021/jm9015763
44301054 194474 0 None -218 6 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
CHEMBL56118 194474 0 None -218 6 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 266 3 1 3 2.2 N#Cc1c[nH]c(CN2CCN(c3ccccc3)CC2)c1 10.1016/s0960-894x(02)00316-5
25139481 184257 0 None -32 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
CHEMBL485227 184257 0 None -32 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 392 10 1 2 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCCCC1 10.1021/jm800895v
25186569 176408 0 None -45708 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
CHEMBL462508 176408 0 None -45708 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
122177643 120698 0 None -2884 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
CHEMBL3577344 120698 0 None -2884 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 632 20 3 9 5.1 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)CCc3ccc(O)c4[nH]c(=O)ccc34)cc2OC)nn1 10.1021/jm501889t
3198 203802 73 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 203802 73 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 203802 73 None -31 34 Human 5.3 pKi = 5.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
10803661 110433 0 None -2 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 1 1 3 3.3 CC(=O)c1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL326159 110433 0 None -2 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 293 1 1 3 3.3 CC(=O)c1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
25141534 55942 0 None -2238 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627305 55942 0 None -2238 7 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 460 7 3 4 3.8 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
76314268 105953 0 None -2630 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3115577 105953 0 None -2630 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
CHEMBL3139633 105953 0 None -2630 4 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 450 3 1 4 3.5 Oc1ccc2c(c1)O[C@@H](CN1CCN(c3ccc(I)cc3)CC1)CC2 10.1021/jm401384w
1353 1880 85 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
3559 1880 85 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
86 1880 85 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
CHEMBL54 1880 85 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
DB00502 1880 85 None -74 85 Rat 6.3 pKi = 6.3 Binding
Tested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligandTested for binding affinity towards rat striatal dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00047a010
10042602 65958 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1016/j.bmcl.2004.06.005
CHEMBL184770 65958 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1016/j.bmcl.2004.06.005
3106 48256 14 None -87 3 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL15564 48256 14 None -87 3 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
10042602 65958 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1007/s00044-012-0055-5
CHEMBL184770 65958 0 None -912 5 Human 5.3 pKi = 5.3 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 335 4 1 4 2.9 Cc1cccc(N2CCN(CCc3ccc4[nH]nnc4c3)CC2)c1C 10.1007/s00044-012-0055-5
10683943 113883 0 None -81 3 Rat 5.3 pKi = 5.3 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 277 1 0 2 3.6 CC(=O)c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL333134 113883 0 None -81 3 Rat 5.3 pKi = 5.3 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 277 1 0 2 3.6 CC(=O)c1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
135398745 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
47 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
CHEMBL715 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
DB00334 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2020.127563
1353 1880 85 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
3559 1880 85 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
86 1880 85 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
CHEMBL54 1880 85 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
DB00502 1880 85 None -74 85 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligandBinding affinity was measured against dopamine receptor D1 in rat using [3H]SCH-23390 as radioligand
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00039a008
46869265 16081 0 None -4 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2012.08.058
CHEMBL1224527 16081 0 None -4 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21 10.1016/j.bmc.2012.08.058
44415839 79487 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212402 79487 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415345 80902 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
CHEMBL215885 80902 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
44415517 79667 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213083 79667 0 None 19 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 463 2 1 5 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(F)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
44415345 80902 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
CHEMBL215885 80902 0 None 64 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
11186086 63043 0 None -12 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 313 1 0 3 3.2 CN1CCN(C2=Cc3cc(Cl)ccc3Cn3cccc32)CC1 10.1021/jm049629t
CHEMBL179557 63043 0 None -12 4 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 313 1 0 3 3.2 CN1CCN(C2=Cc3cc(Cl)ccc3Cn3cccc32)CC1 10.1021/jm049629t
45482153 196361 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
CHEMBL574030 196361 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 502 9 1 7 3.9 COc1ccc(-n2cc(C(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)nn2)cc1 10.1016/j.bmc.2009.06.041
137644833 157594 0 None -87 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4087187 157594 0 None -87 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3nc(C=O)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
44436606 91565 0 None -1445 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241641 91565 0 None -1445 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 505 7 1 3 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
44339992 108697 0 None -501 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL321492 108697 0 None -501 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
9977532 110703 0 None -9999 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL326454 110703 0 None -9999 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
71734129 90630 0 None -10964 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397480 90630 0 None -10964 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
137654675 158088 0 None -1230 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
CHEMBL4092441 158088 0 None -1230 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 433 7 2 7 2.9 O=c1ccc2c(N3CCN(CCCCOc4ccn5nccc5c4)CC3)ccc(O)c2[nH]1 10.1021/acs.jmedchem.7b00363
11652518 165379 0 None -16 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL425064 165379 0 None -16 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1ccc(N2CCN(Cc3cn4cccnc4n3)CC2)cc1 10.1021/jm060166w
44329090 206286 0 None -26 3 Bovine 4.3 pKi = 4.3 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97436 206286 0 None -26 3 Bovine 4.3 pKi = 4.3 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2c(C=O)ccc2C1 10.1016/s0960-894x(01)00564-9
134 2478 19 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2478 19 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2478 19 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2478 19 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2478 19 None -263 67 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
14787976 195305 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL56666 195305 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
44320303 163415 0 None 2 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420788 163415 0 None 2 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
11358377 200652 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
CHEMBL610449 200652 0 None -2 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 295 0 0 3 3.5 CN1CCCc2cc3c(cc2-c2ccccc2CC1)OCO3 10.1016/j.bmc.2009.08.028
44415646 139248 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 635 4 1 7 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OC(F)(F)O4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL379862 139248 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 635 4 1 7 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OC(F)(F)O4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
10264969 48031 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
CHEMBL155352 48031 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
15696487 163247 1 None 9 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL420604 163247 1 None 9 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
15654858 101830 0 None 2 2 Rat 4.3 pKi = 4.3 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3cccnc3N(C=O)c3ccccc32)CC1 10.1021/jm00067a009
CHEMBL303435 101830 0 None 2 2 Rat 4.3 pKi = 4.3 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 321 1 0 5 2.0 CN1CCN(C2=Nc3cccnc3N(C=O)c3ccccc32)CC1 10.1021/jm00067a009
44415807 141104 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccccc1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL385295 141104 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccccc1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
15111052 12666 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 279 3 1 2 3.6 C=CCN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1187965 12666 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 279 3 1 2 3.6 C=CCN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
CHEMBL534678 12666 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 279 3 1 2 3.6 C=CCN1CCc2ccc(O)cc2C(c2ccccc2)C1 10.1021/jm00079a008
156017805 177252 0 None 5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 343 4 1 3 4.2 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Cl)C1 10.1016/j.bmcl.2020.127305
CHEMBL4643886 177252 0 None 5 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 343 4 1 3 4.2 C=CCN1CCc2cc(OC)c(O)cc2C(c2ccccc2Cl)C1 10.1016/j.bmcl.2020.127305
21171 186393 27 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL490533 186393 27 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
46893146 61278 0 None -3981 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 61278 0 None -3981 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
53363202 63525 0 None -26 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803055 63525 0 None -26 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 961 28 0 15 8.7 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(C5CCCCC5)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
122191605 123203 0 None -23 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
CHEMBL3622097 123203 0 None -23 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 426 7 2 3 4.2 Brc1ccc(NCCN2CCN(CCc3c[nH]c4ccccc34)CC2)cc1 10.1021/acsmedchemlett.5b00131
44319370 106564 0 None -1 4 Bovine 6.3 pKi = 6.3 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
CHEMBL315564 106564 0 None -1 4 Bovine 6.3 pKi = 6.3 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 443 5 0 5 3.8 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)[C@@H](C)O1 10.1016/s0960-894x(01)00484-x
10264969 48031 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
CHEMBL155352 48031 0 None -6 2 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
137634397 155564 0 None -11748 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
CHEMBL4063145 155564 0 None -11748 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 480 8 3 10 2.2 O=C1COc2c(N3CCN(CCCCOc4ccn5ncc(/C=N/O)c5c4)CC3)ccc(O)c2N1 10.1016/j.bmc.2017.08.037
24824062 155171 0 None -79 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm701375u
CHEMBL405260 155171 0 None -79 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 354 6 0 5 3.0 FCCOc1ccccc1N1CCN(Cc2cc3ccccn3n2)CC1 10.1021/jm701375u
44372312 53503 0 None -43 3 Bovine 5.3 pKi = 5.3 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL160396 53503 0 None -43 3 Bovine 5.3 pKi = 5.3 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 356 4 1 5 2.8 OCc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
11492 37272 55 None -2 2 Human 4.3 pKi = 4.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 137 2 2 2 0.9 NCCc1cccc(O)c1 10.1021/jm9800292
59111271 37272 55 None -2 2 Human 4.3 pKi = 4.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 137 2 2 2 0.9 NCCc1cccc(O)c1 10.1021/jm9800292
CHEMBL145584 37272 55 None -2 2 Human 4.3 pKi = 4.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 137 2 2 2 0.9 NCCc1cccc(O)c1 10.1021/jm9800292
42606573 17664 0 None -81 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
CHEMBL1258999 17664 0 None -81 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig cortex membranes
ChEMBL 381 5 1 4 3.9 Cc1ccc(CNCC2(F)CCN(C(=O)c3coc4ccccc34)CC2)nc1 10.1021/jm100835q
136043859 138376 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 430 2 1 4 5.9 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
CHEMBL378301 138376 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 430 2 1 4 5.9 Cc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(C)c1 10.1016/j.bmcl.2006.06.034
10618131 28291 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 354 6 2 4 3.4 CN(C)CCCCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL137583 28291 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 354 6 2 4 3.4 CN(C)CCCCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
10518820 109911 0 None -31 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 307 2 0 3 3.7 COc1c(C(C)=O)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL324372 109911 0 None -31 3 Rat 5.3 pKi = 5.3 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23,390 displacement.
ChEMBL 307 2 0 3 3.7 COc1c(C(C)=O)ccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
12049521 201501 0 None -13 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64288 201501 0 None -13 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 427 5 0 5 4.4 COc1ccc(Br)cc1-c1nc(CN2CCN(c3ccccc3)CC2)co1 10.1016/s0960-894x(00)00405-4
117773325 131899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 5 2.7 Cc1cc(Oc2ncccc2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697562 131899 0 None - 1 Human 6.3 pKi = 6.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 341 3 1 5 2.7 Cc1cc(Oc2ncccc2F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44582517 181057 0 None -4 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.3 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL477446 181057 0 None -4 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 431 5 0 3 4.3 O=C1c2ccccc2CCCN1CCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2009.01.067
154726792 176010 1 None -1202 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 176010 1 None -1202 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 176010 1 None -1202 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
9841398 99058 3 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
CHEMBL28338 99058 3 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm00018a002
9841398 99058 3 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL28338 99058 3 None -3 4 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
44276552 99418 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
CHEMBL285924 99418 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1016/s0960-894x(99)00214-0
1353 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
3559 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
86 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
CHEMBL54 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
DB00502 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
Compound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assayCompound was tested for the binding affinity against human cloned Dopamine receptor D1 by radioligand ([3H]SCH-23390) binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm9601720
44415822 168276 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(F)cc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL437917 168276 0 None 33 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 531 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(F)cc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
10409038 84818 0 None -41 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
CHEMBL225853 84818 0 None -41 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 405 2 2 5 3.6 COc1cc2c(cc1O)C[C@H]1c3c(c(Br)c(O)c(OC)c3-2)CCN1C 10.1021/jm060959i
118709176 112925 0 None -34 4 Pig 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318849 112925 0 None -34 4 Pig 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1106 29 0 14 11.8 O=C(CCc1cn(CCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9952858 7473 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
CHEMBL108764 7473 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
9952858 7473 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL108764 7473 0 None 117 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 8 1 3 5.2 CN(C)CCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
167715 2832 12 None -194 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
969 2832 12 None -194 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL225230 2832 12 None -194 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
11504230 77840 0 None -870 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 77840 0 None -870 7 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
10830557 31086 0 None -4 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL140165 31086 0 None -4 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(F)cc4)CC3)c2c1 10.1021/jm0009989
46905072 10082 0 None -28 2 Human 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL1159663 10082 0 None -28 2 Human 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 323 6 1 2 4.5 CCCN(CCc1ccc(C)cc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
25131138 186966 0 None -9549 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 480 8 2 6 5.4 CCCN(CC[C@H]1CC[C@H](NC(=O)c2cc3ccccc3o2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL494511 186966 0 None -9549 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 480 8 2 6 5.4 CCCN(CC[C@H]1CC[C@H](NC(=O)c2cc3ccccc3o2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
49782602 16987 0 None -162 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256169 16987 0 None -162 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 583 6 1 3 7.4 O=C(CCCN1CCC(O)(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
57390117 68957 0 None -346 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
CHEMBL1928123 68957 0 None -346 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 455 13 1 6 3.2 CCOCCOCc1ccc(C(=O)NCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2011.10.063
70690653 76221 0 None -32 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
CHEMBL2062861 76221 0 None -32 3 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 376 5 1 3 4.0 OC[C@@H]1[C@@H]2CN(Cc3ccccc3)[C@@H](c3ccccc3)[C@@H]2[C@H]1N1CCCCC1 10.1016/j.ejmech.2012.07.025
45481890 197338 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 9 2 9 4.4 COc1ccccc1N1CCN(CCCn2cc(CN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL585742 197338 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 9 2 9 4.4 COc1ccccc1N1CCN(CCCn2cc(CN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
228 441 26 None -35 24 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
33 441 26 None -35 24 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
6005 441 26 None -35 24 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
CHEMBL53 441 26 None -35 24 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
DB00714 441 26 None -35 24 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2013.05.014
15225750 140853 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 383 1 1 5 3.2 CC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL383869 140853 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 383 1 1 5 3.2 CC(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
57391216 69825 0 None -23 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940416 69825 0 None -23 8 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 332 6 0 5 2.9 Fc1ccc(SCCCN2CCN(c3ncccn3)CC2)cc1 10.1016/j.bmc.2014.04.026
44304603 201448 0 None -43 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
CHEMBL64139 201448 0 None -43 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 471 8 1 5 5.2 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)cs1 10.1016/s0960-894x(00)00405-4
42625211 55946 0 None -81 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 450 10 3 5 3.3 CCCOc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627309 55946 0 None -81 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 450 10 3 5 3.3 CCCOc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm900095y
14138285 144622 4 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
CHEMBL3912178 144622 4 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2 nan
5016 108682 8 None 125 2 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL32145 108682 8 None 125 2 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
CHEMBL544114 108682 8 None 125 2 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1 10.1021/jm00116a004
74223772 128900 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671279 128900 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 2 4 4.0 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
86767101 128914 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 393 4 1 5 4.4 Cc1ncnc(N2CC(F)C2)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671292 128914 0 None - 1 Human 8.3 pKi = 8.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 393 4 1 5 4.4 Cc1ncnc(N2CC(F)C2)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1F nan
6852376 91167 11 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
CHEMBL1467585 91167 11 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
CHEMBL24077 91167 11 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
CHEMBL503958 91167 11 None -3 5 Human 8.3 pKi = 8.3 Binding
Binding affinity against Dopamine receptor D1 in rat radioligandBinding affinity against Dopamine receptor D1 in rat radioligand
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00170a025
15711869 13229 0 None 6 6 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL1192194 13229 0 None 6 6 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
CHEMBL543390 13229 0 None 6 6 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 333 2 2 3 3.5 NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(Br)c2O 10.1021/jm00114a002
15937729 117659 0 None 301 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 277 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL340855 117659 0 None 301 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 277 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2C(C2=CCCC2)C1 10.1016/S0960-894X(00)80155-9
70690500 75720 0 None - 1 Human 8.3 pKi = 8.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
CHEMBL2057455 75720 0 None - 1 Human 8.3 pKi = 8.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 nan
44401164 69473 0 None -19 9 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL193639 69473 0 None -19 9 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.5 CN(C)C[C@H]1CC2c3ccccc3Sc3ccc(F)cc3[C@H]2O1 10.1021/jm049632c
15115525 109202 0 None 134 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 509 4 2 8 5.0 CN1CCc2cc(Br)c(O)cc2C(c2ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc2)C1 10.1021/jm00115a012
CHEMBL322760 109202 0 None 134 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 509 4 2 8 5.0 CN1CCc2cc(Br)c(O)cc2C(c2ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc2)C1 10.1021/jm00115a012
134155502 150896 0 None 20 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 341 3 2 5 3.2 CCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3961827 150896 0 None 20 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 341 3 2 5 3.2 CCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
15696466 4202 0 None 208 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00114a002
CHEMBL100572 4202 0 None 208 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1O[C@H](C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00114a002
44320050 106348 0 None 138 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL314459 106348 0 None 138 3 Rat 8.3 pKi = 8.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
86764106 131911 0 None - 1 Human 8.3 pKi = 8.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 4 4.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697574 131911 0 None - 1 Human 8.3 pKi = 8.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 355 3 1 4 4.5 Cc1cc(Oc2nccc(C)c2Cl)ccc1-c1c(C)n[nH]c(=O)c1C nan
44356291 22534 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 269 1 3 3 2.7 C[C@@]1(N)Cc2cc(O)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm960318v
CHEMBL132766 22534 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement.
ChEMBL 269 1 3 3 2.7 C[C@@]1(N)Cc2cc(O)c(O)cc2[C@@]1(C)c1ccccc1 10.1021/jm960318v
162643108 181074 0 None 83 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 335 1 1 3 5.0 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4776090 181074 0 None 83 2 Human 8.3 pKi = 8.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 335 1 1 3 5.0 Cc1ccc2c(c1)N=C(C1=C[C@H](C)N(C)CC1)c1cc(F)ccc1N2 10.1016/j.bmcl.2020.127563
71563083 87144 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
CHEMBL2335737 87144 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in CHO cell membranes after 60 mins
ChEMBL 343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2 10.1016/j.bmcl.2012.12.046
10742 3560 27 None -2 7 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00116a004
1225 3560 27 None -2 7 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00116a004
CHEMBL35354 3560 27 None -2 7 Human 8.3 pKi = 8.3 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at Dopamine receptor D1
ChEMBL 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O 10.1021/jm00116a004
5290 198350 32 None 17 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)C1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL595489 198350 32 None 17 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)C1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
46231769 199372 0 None 371 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)C4CC4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL602659 199372 0 None 371 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 396 2 2 3 4.3 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)C4CC4)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
15937718 114734 0 None 48 2 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 251 2 1 2 3.2 C=CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL334728 114734 0 None 48 2 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 251 2 1 2 3.2 C=CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
10732044 83992 0 None 41 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114440 83992 0 None 41 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219804 83992 0 None 41 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
46231771 199295 0 None 107 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
CHEMBL602052 199295 0 None 107 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 420 3 2 4 3.7 CCS(=O)(=O)Nc1cccc2c1CC[C@H]1[C@H]2c2cc(O)c(Cl)cc2CCN1C 10.1016/j.bmcl.2009.12.100
11727683 61720 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 345 1 0 4 4.2 CN1CCCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
CHEMBL177455 61720 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 345 1 0 4 4.2 CN1CCCN(C2=Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm0309811
6917970 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.ejmech.2016.09.036
8370 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.ejmech.2016.09.036
CHEMBL487387 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.ejmech.2016.09.036
6917970 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
8370 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
CHEMBL487387 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in CHO cells by scintillation counting
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2009.08.028
161665 172016 33 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL448891 172016 33 None 1 5 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
2389 3279 114 None -331 67 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
5073 3279 114 None -331 67 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
96 3279 114 None -331 67 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
CHEMBL85 3279 114 None -331 67 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
DB00734 3279 114 None -331 67 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm800689g
2726 906 64 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
621 906 64 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
83 906 64 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
CHEMBL71 906 64 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
DB00477 906 64 None -18 72 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm00118a012
71109989 153241 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
CHEMBL3982119 153241 0 None 6 2 Human 7.3 pKi = 7.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2 nan
2407 3320 73 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
59227 3320 73 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
941 3320 73 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
CHEMBL1303 3320 73 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
DB05271 3320 73 None -60 7 Bovine 6.3 pKi = 6.3 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1021/jm020990u
3716121 83667 14 None -1258 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207643 83667 14 None -1258 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 332 4 0 3 4.1 COc1ccccc1N1CCN(Cc2ccc3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
145986441 166619 0 None -147 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4291172 166619 0 None -147 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 432 7 2 4 3.7 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Br)cc1)CC2 10.1021/acsmedchemlett.8b00229
71454294 83663 0 None -1096 7 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207639 83663 0 None -1096 7 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 431 6 0 5 4.0 COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
1577 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
164512405 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
2537 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5355 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
5501 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
643497 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
688272 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
958 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
960 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL196677 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL26 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
CHEMBL267044 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB00391 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
DB16021 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(99)00086-4
1577 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
164512405 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
2537 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5355 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
5501 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
643497 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
688272 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
958 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
960 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL196677 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL26 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
CHEMBL267044 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB00391 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
DB16021 3647 104 None -50 25 Bovine 4.3 pKi = 4.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N 10.1016/s0960-894x(00)00405-4
10827222 6907 1 None -457 5 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligandBinding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
CHEMBL108463 6907 1 None -457 5 Rat 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligandBinding affinity against Dopamine receptor D1 in rat brain membrane using [3H]-SCH- 23390 as radioligand
ChEMBL 288 3 0 2 3.6 C(#Cc1cccnc1)CCN1CC=C(c2ccccc2)CC1 10.1021/jm950721m
45481875 196442 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574595 196442 0 None -12 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
10939222 202697 1 None -1000 5 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
CHEMBL71960 202697 1 None -1000 5 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissueBinding affinity towards D1 receptor using [3H]-SCH- 23390 in rat striatal tissue
ChEMBL 445 8 1 4 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(Br)cc2)CC1 10.1016/0960-894X(95)00011-H
44415825 80704 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 573 4 1 5 6.8 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccccc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL215641 80704 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 573 4 1 5 6.8 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccccc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
44415786 79640 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 549 6 1 5 6.9 CCC(CC)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212966 79640 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 549 6 1 5 6.9 CCC(CC)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
25141538 55948 0 None -2089 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
CHEMBL1627311 55948 0 None -2089 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 440 8 3 5 2.6 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3cc(F)ccc3[nH]2)CC1 10.1021/jm900095y
154705884 175789 1 None -15 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4469584 175789 1 None -15 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4595726 175789 1 None -15 6 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
11522476 74174 0 None 4 3 Human 6.3 pKi = 6.3 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
CHEMBL202924 74174 0 None 4 3 Human 6.3 pKi = 6.3 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 311 2 0 3 3.3 COc1cc2c(cc1OC)Cc1ccccc1CCN(C)CC2 10.1021/jm050846j
162660874 181301 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4779001 181301 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
86764103 131915 7 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
CHEMBL3697578 131915 7 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acsmedchemlett.9b00050
75201899 171350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
CHEMBL4469983 171350 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assayDisplacement of [3H]-SCH23390 from wild type human D1R expressed in HEK293 cell membranes incubated for 90 mins by scintillation counting based competition radioligand binding assay
ChEMBL 351 3 1 5 4.1 Cc1n[nH]c(=O)c(C)c1-c1ccc(Oc2nccc3occc23)cc1F 10.1021/acsmedchemlett.9b00050
44415838 138550 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL378648 138550 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 504 2 1 6 5.0 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415560 79960 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 4 1 6 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Oc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL214407 79960 0 None 8 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 4 1 6 6.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Oc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
9883454 113467 0 None -2 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL332600 113467 0 None -2 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
10758745 99967 0 None 18 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 99967 0 None 18 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 99967 0 None 18 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
9883454 113467 0 None -2 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL332600 113467 0 None -2 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat tissue homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
56833378 67991 0 None -281 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
CHEMBL1916549 67991 0 None -281 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 1121 39 2 14 10.7 CCCN(CCCCNC(=O)c1ccc(OCCCc2cn(CCCCCCCCn3cc(CCCOc4ccc(C(=O)NCCCCN(CCC)C5Cc6ccccc6C5)cc4OC)nn3)nn2)c(OC)c1)C1Cc2ccccc2C1 10.1021/jm2009919
10665598 34857 1 None -30 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
CHEMBL143355 34857 1 None -30 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccccc4Cl)CC3)c2c1 10.1021/jm0009989
164609519 183869 0 None -426 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4846574 183869 0 None -426 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1cccc(C#N)c1)CC2 10.1016/j.bmcl.2021.128047
44454685 94610 0 None -63 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
CHEMBL255163 94610 0 None -63 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 348 6 0 3 4.0 FCCOc1cccc(CN2CCN(c3ccc(Cl)cc3)CC2)c1 10.1016/j.bmcl.2007.12.026
44380715 58704 0 None -269 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL169222 58704 0 None -269 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
155569483 175625 0 None -154 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 2 2 5 2.9 CCNc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
CHEMBL4593728 175625 0 None -154 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 303 2 2 5 2.9 CCNc1nc(C#Cc2ccc(Cl)s2)nc2[nH]cnc12 10.1039/C8MD00317C
14787977 197204 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
CHEMBL58422 197204 1 None 1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
14787976 195305 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL56666 195305 0 None 1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
44405965 74663 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 449 5 2 5 3.2 O=c1[nH]c2[nH]c(-c3ccccc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
CHEMBL203362 74663 0 None -3 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 449 5 2 5 3.2 O=c1[nH]c2[nH]c(-c3ccccc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
135398745 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
47 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
CHEMBL715 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
DB00334 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmc.2008.06.030
44320092 161339 0 None 39 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL415080 161339 0 None 39 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
57401820 69818 0 None -6 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940409 69818 0 None -6 7 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 364 6 0 3 4.8 Fc1ccc(SCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
135398745 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
47 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
CHEMBL715 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
DB00334 2869 108 None -26 65 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation countingDisplacement of [3H]SCH23390 from human dopamine D1 receptor by liquid scintillation counting
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1016/j.bmcl.2014.07.018
10592479 99801 0 None 48 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL288846 99801 0 None 48 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
21302490 112308 26 None -8 9 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3233142 112308 26 None -8 9 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
CHEMBL3306803 112308 26 None -8 9 Human 7.3 pKi = 7.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 10.1021/jm401958n
74223829 128926 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 351 3 1 5 4.5 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1Cl nan
CHEMBL3671303 128926 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 351 3 1 5 4.5 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1Cl nan
70686343 75719 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057454 75719 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 371 4 1 6 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)c(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
56971028 68903 0 None -3 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 392 8 1 6 2.5 CCOc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1016/j.ejmech.2011.11.023
CHEMBL1927090 68903 0 None -3 2 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation countingDisplacement of [3H]SCH-23390 from rat corpora striatum dopamine D1 receptor after 15 mins by liquid scintillation counting
ChEMBL 392 8 1 6 2.5 CCOc1ccccc1N1CCN(CCCN/C(=N\C#N)c2ccccn2)CC1 10.1016/j.ejmech.2011.11.023
15711865 13064 0 None 1 2 Goldfish 7.3 pKi = 7.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL1190906 13064 0 None 1 2 Goldfish 7.3 pKi = 7.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
CHEMBL541838 13064 0 None 1 2 Goldfish 7.3 pKi = 7.3 Binding
In vitro inhibition of dopamine stimulated adenylate cyclaseIn vitro inhibition of dopamine stimulated adenylate cyclase
ChEMBL 255 2 2 3 2.7 NC[C@@H]1O[C@H](c2ccccc2)Cc2c(O)cccc21 10.1021/jm00114a002
117774289 131890 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.1 CCc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
CHEMBL3697553 131890 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 351 4 1 5 3.1 CCc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
164585473 183979 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 183979 0 None 2 5 Human 6.3 pKi = 6.3 Binding
Binding affinity to D1 receptor (unknown origin)Binding affinity to D1 receptor (unknown origin)
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
44393372 65994 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL184993 65994 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 549 8 1 5 4.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3s2)CC1 10.1016/j.bmcl.2004.05.052
1257607 154773 2 None 4 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 433 4 0 5 4.2 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL403032 154773 2 None 4 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 433 4 0 5 4.2 COc1cc2c(cc1OC)-c1c(OC)c(OC)c(Br)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
45268293 194461 0 None -20 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL561123 194461 0 None -20 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 408 4 1 7 1.4 Cn1c(N2CCOCC2)nc2c(CN3CCN(c4ccccc4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10854877 141483 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL38757 141483 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
44454711 97070 0 None -3311 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
CHEMBL270408 97070 0 None -3311 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 344 7 0 4 3.4 COc1ccccc1N1CCN(Cc2cccc(OCCF)c2)CC1 10.1016/j.bmcl.2007.12.026
10001207 164769 0 None -114 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL423440 164769 0 None -114 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 402 6 1 3 3.7 COc1ccc(Br)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
44567597 168897 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 592 5 4 8 5.5 CN1CCc2cc(OCCOc3cc4c5c(c3)-c3c(ccc(O)c3O)C[C@H]5N(C)CC4)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL442926 168897 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 592 5 4 8 5.5 CN1CCc2cc(OCCOc3cc4c5c(c3)-c3c(ccc(O)c3O)C[C@H]5N(C)CC4)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
90644063 111543 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 111543 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
14198596 101173 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 101173 0 None 2 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
135221 144686 4 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3912606 144686 4 None - 1 Human 6.3 pKi = 6.3 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
90644063 111543 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
CHEMBL3289648 111543 0 None -22 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 327 6 0 3 3.7 Cc1ccc(N2CCN(CCCCc3ccc(F)cc3)CC2)nc1 10.1016/j.bmc.2014.04.026
10826687 50676 0 None -4 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1ccc2c(c1)CC1c3c(cccc3O2)CCN1C 10.1021/jm991034o
CHEMBL157799 50676 0 None -4 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 0 3 3.6 COc1ccc2c(c1)CC1c3c(cccc3O2)CCN1C 10.1021/jm991034o
44569447 178178 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 323 2 0 4 3.4 COc1cc2c3c(c1)-c1c(cccc1OC(C)=O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.11.025
CHEMBL468677 178178 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 323 2 0 4 3.4 COc1cc2c3c(c1)-c1c(cccc1OC(C)=O)C[C@H]3N(C)CC2 10.1016/j.bmcl.2008.11.025
1152279 30520 6 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL1395394 30520 6 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(O)c3CN1CC2 10.1016/j.bmc.2012.12.016
135398737 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
38 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
722 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
CHEMBL42 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
DB00363 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm0002432
135398737 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 944 89 None -44 91 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
228 441 26 None -30 24 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
33 441 26 None -30 24 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
6005 441 26 None -30 24 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
CHEMBL53 441 26 None -30 24 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
DB00714 441 26 None -30 24 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00160a018
11782988 11536 0 None -1 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL118092 11536 0 None -1 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
14198586 200148 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
CHEMBL60706 200148 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity of compound towards dopamine (D1) receptor using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
14198586 200148 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00118a012
CHEMBL60706 200148 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00118a012
14198586 200148 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Compound was evaluated for the binding affinity against dopamine (D1) receptorCompound was evaluated for the binding affinity against dopamine (D1) receptor
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
CHEMBL60706 200148 0 None 2 2 Rat 7.3 pKi = 7.3 Binding
Compound was evaluated for the binding affinity against dopamine (D1) receptorCompound was evaluated for the binding affinity against dopamine (D1) receptor
ChEMBL 287 2 1 2 3.8 CN1CCc2cc(Cl)c(O)cc2C1Cc1ccccc1 10.1021/jm00051a008
11782988 11536 0 None -1 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
CHEMBL118092 11536 0 None -1 3 Rat 7.3 pKi = 7.3 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 1 0 4 4.0 CN1CCCN(C2Cn3cccc3Sc3ccc(Cl)cc32)CC1 10.1021/jm010982y
86767100 123919 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)c(F)c1F nan
CHEMBL3639701 123919 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)c(F)c1F nan
44320256 204590 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL87172 204590 0 None 5 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
188442 87081 5 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3O)C[C@@H]21 10.1016/j.bmc.2012.12.016
CHEMBL2334887 87081 5 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1O)CCN1Cc3c(ccc(OC)c3O)C[C@@H]21 10.1016/j.bmc.2012.12.016
15467371 100538 0 None -912 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294458 100538 0 None -912 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 351 4 1 4 3.4 N#CC(C#N)=Cc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
10831735 31540 0 None -2511 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL140594 31540 0 None -2511 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(Cl)cc4)CC3)cc2c1 10.1021/jm0009989
10567430 118788 1 None -1445 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL343880 118788 1 None -1445 4 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 316 3 1 3 3.4 N#Cc1ccc2cc(CN3CCN(c4ccccc4)CC3)[nH]c2c1 10.1021/jm0009989
44340097 9349 0 None -4365 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL111749 9349 0 None -4365 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.6 CNc1cc(OC)c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
44567595 174705 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 327 3 3 5 2.2 CN1CCc2cc(OCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL457275 174705 0 None -15 2 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 327 3 3 5 2.2 CN1CCc2cc(OCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
137645830 157310 0 None -131 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
CHEMBL4083727 157310 0 None -131 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 424 7 1 8 2.8 Oc1ccc(N2CCN(CCCCOc3ccn4nccc4c3)CC2)c2c1OCCO2 10.1021/acs.jmedchem.7b00363
11615489 69100 1 None -588 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL193337 69100 1 None -588 4 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@H]1CCn2nccc2C1 10.1021/jm101639t
14787976 195305 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00170a025
CHEMBL56666 195305 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@@H]21 10.1021/jm00170a025
14787977 197204 1 None -1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
CHEMBL58422 197204 1 None -1 3 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
156012880 176868 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 364 4 0 5 3.4 C#CCOc1c(OC)cc2c3c1-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4638749 176868 0 None -2 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 364 4 0 5 3.4 C#CCOc1c(OC)cc2c3c1-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
10809188 9185 0 None -83 4 Rat 5.3 pKi = 5.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL110847 9185 0 None -83 4 Rat 5.3 pKi = 5.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
CHEMBL540822 9185 0 None -83 4 Rat 5.3 pKi = 5.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 370 5 0 5 3.7 COc1ccccc1N1CCN(CCC2CCc3sccc3C2=O)CC1 10.1021/jm981094e
150 2473 18 None -43 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2473 18 None -43 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2473 18 None -43 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2473 18 None -43 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2473 18 None -43 15 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
135398737 944 89 None -83 91 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
38 944 89 None -83 91 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
722 944 89 None -83 91 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
CHEMBL42 944 89 None -83 91 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
DB00363 944 89 None -83 91 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm049632c
44415824 80800 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 3 1 5 5.5 CCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL215842 80800 0 None 13 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 493 3 1 5 5.5 CCN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
117772871 131959 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697621 131959 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 4 1 5 3.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
86767099 128912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1cc(F)c(Oc2nccc3[nH]ccc23)cc1F nan
CHEMBL3671290 128912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 352 3 1 4 4.7 Cc1ncnc(C)c1-c1cc(F)c(Oc2nccc3[nH]ccc23)cc1F nan
135398737 944 89 None -44 91 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
38 944 89 None -44 91 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
722 944 89 None -44 91 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
CHEMBL42 944 89 None -44 91 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
DB00363 944 89 None -44 91 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm030480f
57390118 68960 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928126 68960 0 None -616 5 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 953 32 2 13 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
12997400 100535 7 None -53 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
CHEMBL294394 100535 7 None -53 4 Bovine 5.3 pKi = 5.3 Binding
Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1Ability to displace [3H]SCH-23,390 radioligand from bovine Dopamine receptor D1
ChEMBL 241 3 1 2 2.3 c1ccc(N2CCN(Cc3ccc[nH]3)CC2)cc1 10.1016/s0960-894x(02)00316-5
122132 200877 14 None -87 4 Human 5.3 pKi = 5.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm9800292
CHEMBL611801 200877 14 None -87 4 Human 5.3 pKi = 5.3 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm9800292
44454735 94873 0 None -2951 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL256492 94873 0 None -2951 5 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 374 8 0 5 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
25131136 186928 0 None -7244 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 504 9 2 5 6.2 CCCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
CHEMBL494308 186928 0 None -7244 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 504 9 2 5 6.2 CCCCN(CC[C@H]1CC[C@H](NC(=O)c2ccc3ccccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm800471h
49782837 17403 0 None -44 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1258154 17403 0 None -44 5 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 472 6 0 3 6.0 O=C(CCCN1CCN(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
137645574 157261 0 None -5754 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
CHEMBL4083239 157261 0 None -5754 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 462 7 3 6 3.1 O=C1CCc2ccc(OCCCCN3CCN(c4ccc(O)c5[nH]c(=O)ccc45)CC3)cc2N1 10.1021/acs.jmedchem.7b00363
72545009 92692 0 None -109 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443002 92692 0 None -109 5 Pig 4.3 pKi = 4.3 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)nn2)CC1 10.1016/j.bmcl.2013.09.026
145970938 164604 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4228054 164604 0 None -4 5 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 233 5 1 2 3.4 CCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
11698732 72400 0 None 2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccc(Cl)cc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
CHEMBL199876 72400 0 None 2 4 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccc(Cl)cc3)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
44304643 201584 0 None -8 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64668 201584 0 None -8 4 Bovine 5.3 pKi = 5.3 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 8 0 5 5.1 COc1ccc(Br)cc1-c1nc(CN(C)C[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
3168 9172 84 None -89 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
CHEMBL1108 9172 84 None -89 21 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 nan
162665267 181600 0 None 21 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.6 CN1CCC(C2=Nc3cc(Cl)ccc3Nc3ccccc32)=CC1(C)C 10.1016/j.bmcl.2020.127563
CHEMBL4782694 181600 0 None 21 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 351 1 1 3 5.6 CN1CCC(C2=Nc3cc(Cl)ccc3Nc3ccccc32)=CC1(C)C 10.1016/j.bmcl.2020.127563
1353 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
3559 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
86 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
CHEMBL54 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
DB00502 1880 85 None -38 85 Human 7.3 pKi = 7.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl nan
117774669 131958 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.0 CCn1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)c(C)c(=O)[nH]c1=O nan
CHEMBL3697620 131958 0 None - 1 Human 7.3 pKi = 7.3 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 4.0 CCn1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)c(C)c(=O)[nH]c1=O nan
71454927 84169 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 311 1 4 4 3.0 Oc1ccc([C@H]2CN[C@@H]3CCc4cc(O)c(O)cc4[C@H]3C2)cc1 10.1016/j.bmc.2012.08.058
CHEMBL2158636 84169 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 311 1 4 4 3.0 Oc1ccc([C@H]2CN[C@@H]3CCc4cc(O)c(O)cc4[C@H]3C2)cc1 10.1016/j.bmc.2012.08.058
CHEMBL2221040 84169 0 None -10 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 311 1 4 4 3.0 Oc1ccc([C@H]2CN[C@@H]3CCc4cc(O)c(O)cc4[C@H]3C2)cc1 10.1016/j.bmc.2012.08.058
10641637 118275 0 None -19 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
CHEMBL342001 118275 0 None -19 4 Bovine 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]cc(CN3CCN(c4ccc(Cl)cc4)CC3)c2c1 10.1021/jm0009989
118709172 112920 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
CHEMBL3318844 112920 0 None -10 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 493 8 0 4 6.6 Cc1ccc(C(=O)OC2(c3ccc(Cl)cc3)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 10.1016/j.bmcl.2014.06.079
10336538 1595 44 None -5495 8 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
974 1595 44 None -5495 8 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
CHEMBL310843 1595 44 None -5495 8 Bovine 5.3 pKi = 5.3 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm015522j
10336538 1595 44 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
974 1595 44 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
CHEMBL310843 1595 44 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1016/j.bmcl.2007.12.026
44436597 91368 0 None -251 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241210 91368 0 None -251 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 477 5 1 3 4.9 O=C(NCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(C#Cc2ccccc2)cc1 10.1016/j.bmc.2007.08.038
11559581 78009 0 None -2754 6 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL211135 78009 0 None -2754 6 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 361 3 0 5 3.4 Clc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
11654739 176274 0 None -20417 4 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
CHEMBL461236 176274 0 None -20417 4 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 10.1021/jm800689g
71734031 90629 0 None -22908 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
CHEMBL2397479 90629 0 None -22908 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 394 9 1 3 5.2 C#CC1=CC[C@H](N(CCC)CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm400520c
10336538 1595 44 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm701375u
974 1595 44 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm701375u
CHEMBL310843 1595 44 None -5495 8 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/jm701375u
10336538 1595 44 None -5495 8 Human 5.3 pKi = 5.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/acs.jmedchem.7b00151
974 1595 44 None -5495 8 Human 5.3 pKi = 5.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/acs.jmedchem.7b00151
CHEMBL310843 1595 44 None -5495 8 Human 5.3 pKi = 5.3 Binding
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
ChEMBL 326 3 0 4 3.3 Clc1ccc(cc1)N1CCN(CC1)Cc1cc2n(n1)cccc2 10.1021/acs.jmedchem.7b00151
44537919 196459 0 None -28 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL574700 196459 0 None -28 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCc2cn(CCCN3CCc4cc(O)c(O)cc4C(c4ccccc4C)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
10811026 28335 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 9 2 3 4.3 O=CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL137636 28335 0 None 3 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 400 9 2 3 4.3 O=CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
2801 161325 56 None -10 28 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL1200710 161325 56 None -10 28 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
CHEMBL415 161325 56 None -10 28 Human 6.3 pKi = 6.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 nan
6852376 91167 11 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL1467585 91167 11 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL24077 91167 11 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
CHEMBL503958 91167 11 None -3 5 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cellsBinding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00018a002
44415802 79797 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213668 79797 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415383 81039 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 5 1 6 5.4 COc1ccc(CCC(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1Cl 10.1016/j.bmcl.2006.06.022
CHEMBL215950 81039 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 537 5 1 6 5.4 COc1ccc(CCC(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1Cl 10.1016/j.bmcl.2006.06.022
25110708 12501 0 None 6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 381 2 3 3 5.2 Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL1186978 12501 0 None 6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 381 2 3 3 5.2 Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
CHEMBL485207 12501 0 None 6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 381 2 3 3 5.2 Oc1cc2c(c(-c3ccc4ccccc4c3)c1O)CCNCC2c1ccccc1 10.1016/j.bmc.2008.09.049
130442561 166340 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286110 166340 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
44276405 99647 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
CHEMBL287513 99647 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4 10.1016/s0960-894x(99)00214-0
44412191 137847 0 None -107 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
CHEMBL377200 137847 0 None -107 4 Pig 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 332 4 0 4 3.5 Cc1c(CN2CCN(c3ccccc3)CC2)cnn1-c1ccccc1 10.1016/j.bmcl.2006.02.075
11071135 206268 0 None -2570 8 Rat 5.3 pKi = 5.3 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 206268 0 None -2570 8 Rat 5.3 pKi = 5.3 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
11661609 79283 0 None -5623 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
CHEMBL211539 79283 0 None -5623 4 Pig 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 414 4 0 5 3.7 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(Br)c3n2)CC1 10.1021/jm060166w
44339879 171716 0 None -186 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL447476 171716 0 None -186 4 Bovine 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)N[C@H]2CCCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(03)00678-4
44327153 108723 0 None -3 4 Rat 6.3 pKi = 6.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm981094e
CHEMBL321682 108723 0 None -3 4 Rat 6.3 pKi = 6.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm981094e
CHEMBL558817 108723 0 None -3 4 Rat 6.3 pKi = 6.3 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine 1 (D1) receptor in rat striatal membrane.
ChEMBL 385 5 0 4 4.6 O=C(c1ccc(F)cc1)C1CCN(CCC2CCc3ccsc3C2=O)CC1 10.1021/jm981094e
10738274 164339 0 None -2 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(Br)cc(OC)c2C1Cc1ccccc1O 10.1021/jm991034o
CHEMBL422169 164339 0 None -2 2 Rat 5.3 pKi = 5.3 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 4 1 3 4.3 CCN1CCc2cc(Br)cc(OC)c2C1Cc1ccccc1O 10.1021/jm991034o
145982261 166179 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
CHEMBL4283176 166179 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C 10.1021/acs.jmedchem.8b01622
155195311 173775 0 None -1778 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assayDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assay
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acsmedchemlett.9b00660
CHEMBL4551160 173775 0 None -1778 5 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assayDisplacement of [3H]-SCH23390 from human D1 receptor expressed in HEK293 cells after 60 mins by microbeta counting based assay
ChEMBL 433 7 3 5 3.4 C[C@H]1CO[C@@H](c2ccc(N)nc2)CN1C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acsmedchemlett.9b00660
24949693 181722 0 None -7244 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 10.1021/jm800176x
CHEMBL478413 181722 0 None -7244 3 Rat 5.3 pKi = 5.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 10.1021/jm800176x
14198593 196997 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
CHEMBL57988 196997 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00051a008
36791366 87076 1 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL2334880 87076 1 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
14198593 196997 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00118a012
CHEMBL57988 196997 1 None 4 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CNCC2c1ccccc1 10.1021/jm00118a012
44405985 168993 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccccc3Cl)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
CHEMBL443567 168993 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 483 5 2 5 3.8 O=c1[nH]c2[nH]c(-c3ccccc3Cl)cc2c(=O)n1CCN1CCN(c2ccccc2Cl)CC1 10.1016/j.bmcl.2005.09.027
122132 200877 14 None 4 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm00160a018
CHEMBL611801 200877 14 None 4 4 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 207 1 2 3 1.5 CN(C)C1CCc2cc(O)c(O)cc2C1 10.1021/jm00160a018
11720302 165705 0 None -301 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL426863 165705 0 None -301 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 503 7 1 3 5.2 O=C(NCCCCN1CCN(c2cccc(F)c2F)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
10939167 9409 0 None -165 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL112065 9409 0 None -165 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
CHEMBL129483 9409 0 None -165 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 443 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm101639t
44454710 155125 0 None -478 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
CHEMBL404888 155125 0 None -478 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 378 7 0 4 4.0 COc1cc(CN2CCN(c3ccc(Cl)cc3)CC2)ccc1OCCF 10.1016/j.bmcl.2007.12.026
137631036 160604 0 None -28 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 420 6 1 5 2.6 O=C(NCCCCN1CC[N+]2(CCOc3ccccc32)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4060837 160604 0 None -28 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 420 6 1 5 2.6 O=C(NCCCCN1CC[N+]2(CCOc3ccccc32)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4117325 160604 0 None -28 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 420 6 1 5 2.6 O=C(NCCCCN1CC[N+]2(CCOc3ccccc32)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
44415623 137726 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 599 4 1 7 6.4 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL377043 137726 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 599 4 1 7 6.4 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3cccc4c3OCO4)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
44316058 203826 0 None -64 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL80974 203826 0 None -64 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
10316297 123531 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
CHEMBL363124 123531 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1016/j.bmcl.2004.06.005
10316297 123531 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
CHEMBL363124 123531 0 None -549 5 Human 5.2 pKi = 5.2 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 357 4 1 4 3.5 c1ccc2c(N3CCN(CCc4ccc5[nH]nnc5c4)CC3)cccc2c1 10.1007/s00044-012-0055-5
53946796 67425 1 None -5248 2 Rat 4.2 pKi = 4.2 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
CHEMBL1907969 67425 1 None -5248 2 Rat 4.2 pKi = 4.2 Binding
In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate.
ChEMBL 235 3 2 3 2.7 CCCN1CCC[C@H](c2ccc(O)c(O)c2)C1 10.1021/jm00160a016
44427970 152078 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
CHEMBL397207 152078 0 None -1 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 325 2 0 3 3.7 COc1cc2c(cc1OC)Cc1ccccc1CCCN(C)CC2 10.1021/jm070388+
156010592 176554 0 None 14 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 376 4 1 4 3.4 C#CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4633772 176554 0 None 14 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 376 4 1 4 3.4 C#CCOc1c(OC)cc2c3c1-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
86764321 131950 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 399 5 1 5 4.3 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C1CC1 nan
CHEMBL3697612 131950 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 399 5 1 5 4.3 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C1CC1 nan
117773598 131953 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.7 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2C)c(C)c(=O)[nH]c1=O nan
CHEMBL3697615 131953 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 4 1 5 3.7 CCn1c(-c2ccc(Oc3ncccc3Cl)cc2C)c(C)c(=O)[nH]c1=O nan
164626655 186011 0 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
CHEMBL4878587 186011 0 None -16 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 441 7 1 5 4.1 COc1cc2c(cc1OC)CN(Cc1ccccc1CNC(=O)c1ccc(C#N)cc1)CC2 10.1016/j.bmcl.2021.128047
44287454 13117 0 None -1 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL1191276 13117 0 None -1 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL542351 13117 0 None -1 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
1353 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
3559 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
86 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
CHEMBL54 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
DB00502 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat brainDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat brain
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmc.2007.07.018
2389 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
5073 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
96 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
CHEMBL85 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
DB00734 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmc.2008.06.030
54580906 61276 0 None -2754 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 61276 0 None -2754 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
57391895 68959 0 None -301 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928125 68959 0 None -301 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 925 30 2 13 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
3156990 8046 19 None -28 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
CHEMBL109173 8046 19 None -28 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1cccn1C1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(99)00540-5
25139478 184373 0 None -446 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
CHEMBL485384 184373 0 None -446 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 510 10 0 4 7.5 CCCN(CCCCn1cc(-c2ccc(-c3ccccc3)cc2)nn1)C1CC=C(C#C[Si](C)(C)C)CC1 10.1021/jm800895v
15467369 100461 0 None -6165 3 Bovine 4.2 pKi = 4.2 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL293956 100461 0 None -6165 3 Bovine 4.2 pKi = 4.2 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1ccc(CN2CCN(c3ccccc3)CC2)[nH]1 10.1016/s0960-894x(99)00302-9
136043854 79777 0 None -20 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 460 2 1 6 5.1 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc4c(c3)OCCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
CHEMBL213577 79777 0 None -20 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 460 2 1 6 5.1 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc4c(c3)OCCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
77974401 113461 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 252 1 1 2 2.9 CN1CCc2ccc(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325920 113461 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 252 1 1 2 2.9 CN1CCc2ccc(N)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
154727843 175859 1 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4448853 175859 1 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
CHEMBL4596221 175859 1 None -5 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 486 13 0 6 5.6 CCN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1c1cc(F)ccc1OCCF 10.1021/acs.jmedchem.9b01835
71086428 151021 0 None -66 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3963122 151021 0 None -66 2 Mouse 5.2 pKi = 5.2 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 373 6 0 5 2.9 Clc1cncc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
3108374 91545 19 None -3 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
CHEMBL2414990 91545 19 None -3 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
107715 199260 18 None -144 20 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 199260 18 None -144 20 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 199260 18 None -144 20 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
57401819 69817 0 None -75 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL1940408 69817 0 None -75 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 346 6 0 2 4.6 Fc1ccc(CCCCN2CCN(c3ccc(Cl)cc3)CC2)cc1 10.1016/j.bmc.2014.04.026
23364995 112921 0 None -13 4 Pig 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318845 112921 0 None -13 4 Pig 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 417 7 0 4 5.0 CC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
86764104 131960 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697622 131960 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 4 4.5 Cc1cc(Oc2ncccc2C(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
156020558 177472 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 1 2 3 3.5 CN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
CHEMBL4647167 177472 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 1 2 3 3.5 CN1CCc2cc(O)c(O)cc2C(c2ccccc2Br)C1 10.1016/j.bmcl.2020.127305
44436617 91129 0 None -20 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL240584 91129 0 None -20 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 481 9 1 4 4.8 COc1ccccc1N1CCN(CCCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
49782604 17341 0 None -19 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1257927 17341 0 None -19 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 379 6 1 3 4.9 Cc1ccc(C)c(C(=O)CCCN2CCC(O)(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
49782836 17370 0 None -58 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
CHEMBL1258036 17370 0 None -58 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 456 6 0 3 5.5 O=C(CCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1ccc(F)cc1 10.1021/jm100899z
24841480 183317 0 None -2951 20 Human 5.2 pKi = 5.2 Binding
Antagonist activity at dopamine D1 receptor (unknown origin) by PDSP assayAntagonist activity at dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183317 0 None -2951 20 Human 5.2 pKi = 5.2 Binding
Antagonist activity at dopamine D1 receptor (unknown origin) by PDSP assayAntagonist activity at dopamine D1 receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
44436603 144683 0 None -269 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
CHEMBL391257 144683 0 None -269 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 467 8 1 4 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cccc(C#Cc3ccccc3)c2)CC1 10.1016/j.bmc.2007.08.038
11655570 79316 0 None -11220 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
CHEMBL211590 79316 0 None -11220 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 462 4 0 5 3.6 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(I)c3n2)CC1 10.1021/jm060166w
45267409 194487 0 None -1513 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL561262 194487 0 None -1513 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 351 4 0 6 2.7 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)ncn23)CC1 10.1016/j.bmc.2009.05.015
71212556 143030 0 None -120 6 Human 6.2 pKi = 6.2 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
CHEMBL3899169 143030 0 None -120 6 Human 6.2 pKi = 6.2 Binding
Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.Binding Assay or Functional Activity Assay: Further, the compounds of the invention may be tested in binding assays and functional activity assays by well known methods for other physiologically important receptors such as, but not limited to, the hERG channel, other serotonin receptors (specifically 5-HT1B, 5-HT1D, receptors, lack of agonist activity at 5-HT2B receptors, 5-HT2C, 5-HT5, 5-HT6, and 5-HT7 receptors), dopaminergic receptors (specifically D1, D2, and D3), GABAA receptors, adrenergic receptors and monoamine transporters.
ChEMBL 433 3 1 6 4.6 Cc1ccc2c(c1)Oc1sc(Cl)cc1C(N1CCN(CC(C)(C)C(=O)O)CC1)=N2 nan
8447 188362 80 None -8 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
CHEMBL508112 188362 80 None -8 13 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1 nan
3191 102385 93 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102385 93 None -12 25 Human 6.2 pKi = 6.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
145969934 164493 0 None -54 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4226336 164493 0 None -54 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 261 7 1 2 4.2 CCCCCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
14198573 196406 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 1 2 3.6 COc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL574340 196406 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 273 2 1 2 3.6 COc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1016/j.bmc.2009.05.079
130424 202642 11 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 327 1 1 3 4.4 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2cccc3ccoc23)C1 10.1021/jm00170a025
CHEMBL71600 202642 11 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 327 1 1 3 4.4 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2cccc3ccoc23)C1 10.1021/jm00170a025
44415827 80647 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
CHEMBL215414 80647 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 505 4 1 7 4.5 COc1cccc(OC)c1C(=O)NN1c2ccccc2N=C(N2CCN(C)CC2)c2cc(Cl)ccc21 10.1016/j.bmcl.2006.06.034
11619691 154517 0 None 138 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 467 3 1 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(O)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
CHEMBL401690 154517 0 None 138 2 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 467 3 1 5 3.8 COc1cc2c(cc1OC)-c1c(OC)c(O)c(I)c3c1[C@H](C2)N(C)CC3 10.1021/jm060959i
5311428 99645 7 None 32 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL1744078 99645 7 None 32 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
CHEMBL287504 99645 7 None 32 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 253 1 1 2 3.0 CN1CCc2ccc(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00079a008
56589560 70253 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949725 70253 0 None -1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
1353 1880 85 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
3559 1880 85 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
86 1880 85 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
CHEMBL54 1880 85 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
DB00502 1880 85 None -38 85 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2009.09.041
6603820 95330 13 None -4 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.ejmech.2011.11.039
CHEMBL25856 95330 13 None -4 13 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 10.1016/j.ejmech.2011.11.039
440229 87083 48 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
CHEMBL2334891 87083 48 None 1 5 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hrDisplacement of [3H]SCH23390 from human 3HA-tagged dopamine D1 receptor expressed in HEK293 cells after 1 hr
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmcl.2017.01.090
6917970 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
8370 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
CHEMBL487387 3635 54 None -1 34 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O 10.1016/j.bmc.2012.05.057
3246443 37453 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL1457510 37453 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
9869262 104382 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL310997 104382 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
3246443 37453 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
CHEMBL1457510 37453 2 None 2 6 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hrDisplacement of [3H]SCH23390 from human dopamine D1 receptor after 1 hr
ChEMBL 325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmcl.2017.01.090
10709445 100893 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 100893 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 100893 0 None 26 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10107367 101961 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL303993 101961 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
71261649 87084 7 None 15 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
CHEMBL2334892 87084 7 None 15 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 341 3 1 5 3.1 COc1cc2c(cc1O)[C@H]1Cc3ccc(OC)c(OC)c3CN1CC2 10.1016/j.bmc.2012.12.016
10640108 83990 0 None 208 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2114441 83990 0 None 208 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
CHEMBL2219802 83990 0 None 208 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21 10.1021/jm970038v
10107367 101961 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
CHEMBL303993 101961 1 None -7 4 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00118a012
14198585 100334 1 None 1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL293158 100334 1 None 1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
10107367 101961 1 None 7 4 Human 8.2 pKi = 8.2 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
CHEMBL303993 101961 1 None 7 4 Human 8.2 pKi = 8.2 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00129a006
127031399 138213 0 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 2 6 2.8 COc1cc2c(cc1O)C1Cc3ccc(OCCCO)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780268 138213 0 None 16 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 385 6 2 6 2.8 COc1cc2c(cc1O)C1Cc3ccc(OCCCO)c(OC)c3CN1CC2 10.1016/j.bmc.2016.03.037
71109797 145363 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
CHEMBL3917753 145363 0 None - 1 Human 8.2 pKi = 8.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
71109797 145363 0 None - 1 Human 8.2 pKi = 8.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
CHEMBL3917753 145363 0 None - 1 Human 8.2 pKi = 8.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2 nan
130442514 165979 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4279267 165979 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12 10.1021/acs.jmedchem.8b01622
25110709 12498 0 None 17 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 373 2 2 3 5.0 Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL1186967 12498 0 None 17 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 373 2 2 3 5.0 Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1 10.1016/j.bmc.2008.09.049
CHEMBL484538 12498 0 None 17 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 373 2 2 3 5.0 Cc1cccc(-c2c(O)c(O)cc3c2CCN(C)CC3c2cccc(C)c2)c1 10.1016/j.bmc.2008.09.049
86764103 131915 7 None - 1 Human 8.2 pKi = 8.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697578 131915 7 None - 1 Human 8.2 pKi = 8.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 389 5 1 6 3.1 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44415600 79375 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 461 4 1 6 4.8 COc1ccccc1CNN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL211910 79375 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 461 4 1 6 4.8 COc1ccccc1CNN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
122205437 136787 0 None -19 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
CHEMBL3752512 136787 0 None -19 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor incubated for 90 mins by radioligand binding assay
ChEMBL 257 0 0 2 3.4 CN1CCc2ccccc2Cc2sccc2CC1 10.1039/C5MD00258C
12313091 86051 3 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1ccc2c(c1O)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL2314732 86051 3 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 325 1 1 5 2.8 COc1ccc2c(c1O)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
11023546 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
11023546 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
10071501 9786 0 None 10 2 Rat 7.2 pKi = 7.2 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL114228 9786 0 None 10 2 Rat 7.2 pKi = 7.2 Binding
Compound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assayCompound was tested for the Binding affinity against Human cloned Dopamine receptor D1 by Radio ligand ([3H]SCH-23390) binding assay
ChEMBL 432 5 1 3 5.8 CN(C)c1ccc(/C=C/CN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
44393415 64899 0 None -251 5 Pig 6.2 pKi = 6.2 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
CHEMBL182652 64899 0 None -251 5 Pig 6.2 pKi = 6.2 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 499 8 1 5 3.7 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)s2)CC1 10.1016/j.bmcl.2004.05.052
137638973 156332 0 None -1479 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4071868 156332 0 None -1479 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 10 2 7 4.3 CCCN(CCCCOc1ccc2c(/C=N/O)cnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
56837419 68962 0 None -2630 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928128 68962 0 None -2630 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 997 35 2 14 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
46917563 67993 0 None -8511 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
CHEMBL1916551 67993 0 None -8511 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 561 18 1 7 5.5 CCCCn1cc(CCCOc2ccc(C(=O)NCCCCN(CCC)C3Cc4ccccc4C3)cc2OC)nn1 10.1021/jm2009919
2780 110040 32 None -138 11 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
CHEMBL325109 110040 32 None -138 11 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1016/s0960-894x(03)00678-4
137634153 155891 0 None -54 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 236 1 2 5 0.6 Oc1ccc(N2CCNCC2)c2c1OCCO2 10.1016/j.bmc.2017.08.037
CHEMBL4066916 155891 0 None -54 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 236 1 2 5 0.6 Oc1ccc(N2CCNCC2)c2c1OCCO2 10.1016/j.bmc.2017.08.037
10775901 35551 0 None -70 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cc(C)cc(C)c2)C1 10.1021/jm9708700
CHEMBL144114 35551 0 None -70 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cc(C)cc(C)c2)C1 10.1021/jm9708700
10609576 118247 0 None -42 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cccc(C)c2C)C1 10.1021/jm9708700
CHEMBL341825 118247 0 None -42 2 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2cccc(C)c2C)C1 10.1021/jm9708700
72545008 92691 0 None -89 5 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443001 92691 0 None -89 5 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 451 15 0 9 1.6 COc1ccccc1N1CCN(Cc2cn(CCOCCOCCOCCF)nn2)CC1 10.1016/j.bmcl.2013.09.026
15654859 201343 0 None 4 2 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3N(C)c3ccccc32)CC1 10.1021/jm00067a009
CHEMBL63390 201343 0 None 4 2 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 307 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3N(C)c3ccccc32)CC1 10.1021/jm00067a009
13994412 11060 1 None -117 3 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL117841 11060 1 None -117 3 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
10689791 164329 0 None 12 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 4 2 3 3.3 NCCCC(=O)N1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL422086 164329 0 None 12 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 358 4 2 3 3.3 NCCCC(=O)N1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
490 190 5 None -60255 12 Rat 5.2 pKi = 5.2 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
9890547 190 5 None -60255 12 Rat 5.2 pKi = 5.2 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
CHEMBL268758 190 5 None -60255 12 Rat 5.2 pKi = 5.2 Binding
Ancillary Binding affinity to rat Dopamine receptor D1Ancillary Binding affinity to rat Dopamine receptor D1
ChEMBL 462 6 1 7 3.2 COc1ccccc1N1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)c(cs2)c1ccccc1 10.1016/s0960-894x(01)00159-7
10015045 13541 1 None -6 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm9015763
CHEMBL119455 13541 1 None -6 6 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm9015763
9992499 73039 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
CHEMBL201483 73039 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 254 0 0 2 2.6 CN1CCc2ccccc2Cc2ccn(C)c2CC1 10.1021/jm050846j
72699816 114689 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 329 3 1 4 4.1 CCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344457 114689 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 329 3 1 4 4.1 CCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
145966311 163481 0 None -3388 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cells
ChEMBL 378 5 1 4 2.9 O=C(NCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccccn1 10.1016/j.bmc.2017.09.018
CHEMBL4208744 163481 0 None -3388 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cells
ChEMBL 378 5 1 4 2.9 O=C(NCCN1CCN(c2ccc(Cl)c(Cl)c2)CC1)c1ccccn1 10.1016/j.bmc.2017.09.018
57402366 68973 0 None -1230 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928139 68973 0 None -1230 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1033 32 2 17 5.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
44340333 9571 0 None -1071 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL112833 9571 0 None -1071 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 384 5 1 3 3.8 C#Cc1cc(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)c(OC)c2ccccc12 10.1016/s0960-894x(03)00678-4
44340227 110152 0 None -2137 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL325772 110152 0 None -2137 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 486 5 1 3 4.5 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(I)c2ccccc12 10.1016/s0960-894x(03)00678-4
10265732 94408 0 None 2 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253738 94408 0 None 2 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
2477 734 54 None -28 28 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
36 734 54 None -28 28 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
437 734 54 None -28 28 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
CHEMBL49 734 54 None -28 28 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
DB00490 734 54 None -28 28 Bovine 5.2 pKi = 5.2 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950759z
15508242 164697 0 None -64 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
CHEMBL422959 164697 0 None -64 4 Bovine 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1Displacement of [3H]SCH-23390 from bovine striatal membrane Dopamine receptor D1
ChEMBL 268 4 0 3 3.1 O=Cc1ccn(C2CCN(Cc3ccccc3)CC2)c1 10.1016/s0960-894x(99)00540-5
838674 106941 10 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL318111 106941 10 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
CHEMBL542493 106941 10 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00163a007
44316331 203788 0 None -41 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL80686 203788 0 None -41 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
10378389 201554 1 None -14454 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 201554 1 None -14454 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 201554 1 None -14454 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
838674 106941 10 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL318111 106941 10 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
CHEMBL542493 106941 10 None -2570 2 Rat 6.2 pKi = 6.2 Binding
Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390Compound was evaluated for its ability to inhibit Dopamine receptor D1 in rat striatum using [3H]SCH-23390
ChEMBL 293 2 2 3 3.4 C=CCN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00105a005
71817345 91547 0 None -158 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
CHEMBL2414992 91547 0 None -158 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
44415567 79625 0 None 58 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212905 79625 0 None 58 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccc(C#N)c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415579 79435 0 None 61 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 542 4 2 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3NC3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212186 79435 0 None 61 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 542 4 2 6 6.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3NC3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
72699817 114690 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
CHEMBL3344458 114690 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 343 4 1 4 4.5 CCCCc1cc2c(s1)C[C@H]1c3cc(O)c(OC)cc3CCN1C2 10.1016/j.bmc.2014.09.024
46931072 200360 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
CHEMBL608530 200360 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligandBinding affinity towards human D1 dopamine receptor was determined by using [3H]-SCH- 23390 as radioligand
ChEMBL 386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21 10.1016/j.bmcl.2004.06.078
2389 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
5073 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
96 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
CHEMBL85 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
DB00734 3279 114 None -467 67 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1021/jm030480f
122189391 122730 0 None -72 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
CHEMBL3613877 122730 0 None -72 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assayDisplacement of [3H]SCH23990 from human dopamine D1 receptor expressed in CHO cell membranes by radioligand competition binding assay
ChEMBL 431 7 0 9 2.1 COc1ccccc1N1CCN(CCc2cn(-c3ccn4ncc(C=O)c4c3)nn2)CC1 10.1016/j.bmc.2015.07.050
44264742 96726 0 None -13 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
CHEMBL268190 96726 0 None -13 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 298 3 0 4 2.8 c1ccn2ncc(CN3CCN(C4CCCCC4)CC3)c2c1 10.1016/s0960-894x(98)00692-1
2 3210 19 None -977 28 Human 7.2 pKi = 7.2 Binding
Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cellsBinding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 3210 19 None -977 28 Human 7.2 pKi = 7.2 Binding
Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cellsBinding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 3210 19 None -977 28 Human 7.2 pKi = 7.2 Binding
Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cellsBinding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
11023546 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
9839050 111886 0 None -131 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
CHEMBL329566 111886 0 None -131 9 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 293 2 0 2 3.8 CN(C)C[C@H]1C[C@@H]2c3ccccc3Cc3ccccc3[C@H]2O1 10.1021/jm049632c
117773522 131922 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 6 3.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697585 131922 0 None - 1 Human 7.2 pKi = 7.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 407 4 1 6 3.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
24863698 176124 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 253 0 2 2 2.7 Oc1ccc2c(c1)CCNCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
CHEMBL459871 176124 0 None -1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human cloned dopamine D1 receptorDisplacement of [3H]SCH23390 from human cloned dopamine D1 receptor
ChEMBL 253 0 2 2 2.7 Oc1ccc2c(c1)CCNCCc1ccccc1C2 10.1016/j.bmcl.2008.04.081
11023546 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL2111783 78069 0 None -5 4 Rat 7.2 pKi = 7.2 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 317 1 0 4 3.1 CN1CCN([C@H]2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
3108374 91545 19 None -3 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
CHEMBL2414990 91545 19 None -3 2 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 295 2 0 3 3.5 COc1cc2c3c(c1OC)-c1ccccc1CC3N(C)CC2 10.1016/j.bmcl.2013.06.078
44400626 70059 0 None -999 5 Pig 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL194555 70059 0 None -999 5 Pig 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
44403214 72148 0 None -446 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
CHEMBL198993 72148 0 None -446 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 386 8 1 5 2.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(F)nc2)CC1 10.1016/j.bmcl.2005.07.037
44448063 154706 0 None 3 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
CHEMBL402736 154706 0 None 3 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 10.1021/jm060959i
154727713 175790 1 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514586 175790 1 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4595727 175790 1 None -7 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 426 10 1 6 4.5 COc1ccc(F)cc1C1CC1CNCCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
118717797 114695 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 2 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344463 114695 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 357 2 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC(C)(C)C)cc3CN1CC2 10.1016/j.bmc.2014.09.024
10758760 22301 0 None 3 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 329 4 1 2 4.8 CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL132545 22301 0 None 3 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 329 4 1 2 4.8 CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
161379 186632 6 None -79 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
CHEMBL492418 186632 6 None -79 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 293 3 0 3 3.8 CN(C)CCc1cc2c(c3c1ccc1ccccc13)OCO2 10.1016/j.bmcl.2013.06.078
154703438 175807 1 None -26 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4475699 175807 1 None -26 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
CHEMBL4595859 175807 1 None -26 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 496 12 0 6 6.1 COc1ccc(Cl)cc1C1CC1CN(CCCSc1nnc(-c2ccccc2)n1C)CC1CC1 10.1021/acs.jmedchem.9b01835
136043857 79376 0 None -7 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 5.0 Clc1ccc2c(c1)N=C(N1CCN(Cc3cccc4c3OCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
CHEMBL211915 79376 0 None -7 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 5.0 Clc1ccc2c(c1)N=C(N1CCN(Cc3cccc4c3OCO4)CC1)c1ccccc1N2 10.1016/j.bmcl.2006.06.034
44281881 99387 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL1743774 99387 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
CHEMBL285717 99387 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards Dopamine receptor D1Binding affinity towards Dopamine receptor D1
ChEMBL 281 1 2 3 3.4 Oc1cc2c(cc1O)[C@@H]1CCCN1C[C@H]2c1ccccc1 10.1021/jm00391a028
1242 3556 23 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
935 3556 23 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
CHEMBL286080 3556 23 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
44415743 79698 0 None 30 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213201 79698 0 None 30 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc(C#N)cc3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
6852376 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
CHEMBL1467585 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
CHEMBL24077 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
CHEMBL503958 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00114a002
6852376 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL1467585 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL24077 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
CHEMBL503958 91167 11 None -4 5 Rat 7.2 pKi = 7.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/jm00112a034
1242 3556 23 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
935 3556 23 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
CHEMBL286080 3556 23 None 1 17 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 10.1021/jm00173a005
70684206 75712 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
CHEMBL2057442 75712 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2 10.1016/j.bmc.2012.05.057
70692653 75713 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL2057443 75713 0 None - 1 Human 7.2 pKi = 7.2 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
70692652 75711 0 None 8 2 Human 7.2 pKi = 7.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
CHEMBL2057441 75711 0 None 8 2 Human 7.2 pKi = 7.2 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2 nan
54580905 61274 0 None -2570 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 61274 0 None -2570 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
56594533 70254 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
CHEMBL1949726 70254 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in human HEK293 cells
ChEMBL 304 0 1 1 4.2 C[C@@H]1Cc2c([nH]c3ccccc23)Cc2ccccc2CCN1C 10.1021/jm200676f
56837634 68964 0 None -1479 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928130 68964 0 None -1479 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1041 38 2 15 6.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
9796958 146045 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115374 146045 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL39230 146045 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL544814 146045 0 None 25 4 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
11633170 78003 0 None -2818 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
CHEMBL211118 78003 0 None -2818 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 421 5 0 7 2.8 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(N4CCOCC4)c3n2)CC1 10.1021/jm060166w
11583188 138752 0 None -19498 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
CHEMBL379125 138752 0 None -19498 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 448 4 0 5 3.3 COc1ccccc1N1CCN(Cc2cn3cc(I)ccc3n2)CC1 10.1021/jm060166w
10355510 155121 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL404865 155121 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
71461481 83656 0 None -676 5 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
CHEMBL2207632 83656 0 None -676 5 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 356 4 0 3 4.1 C#Cc1cc(CN2CCN(c3ccccc3OC)CC2)c2cccccc1-2 10.1016/j.bmcl.2012.09.064
71450707 83664 0 None -1698 7 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207640 83664 0 None -1698 7 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 444 6 0 5 3.9 COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
25131135 186965 0 None -8511 3 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 448 6 3 5 4.7 Nc1nc2c(s1)C[C@@H](NCC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
CHEMBL494510 186965 0 None -8511 3 Rat 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatumDisplacement of [3H]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum
ChEMBL 448 6 3 5 4.7 Nc1nc2c(s1)C[C@@H](NCC[C@H]1CC[C@H](NC(=O)c3ccc4ccccc4c3)CC1)CC2 10.1021/jm800471h
90644058 111537 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 111537 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
90644058 111537 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
CHEMBL3289642 111537 0 None -104 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 372 4 0 3 4.0 O=C1c2ccc(F)cc2CC1CCN1CCN(c2ccc(Cl)cc2)CC1 10.1016/j.bmc.2014.04.026
130907 193017 5 None -3311 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm701045j
CHEMBL53294 193017 5 None -3311 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm701045j
64143 197186 57 None -1 8 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
CHEMBL584 197186 57 None -1 8 Human 5.2 pKi = 5.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C nan
154725277 175858 1 None -25 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4472900 175858 1 None -25 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4596220 175858 1 None -25 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01835
10015860 98820 0 None 38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
CHEMBL281932 98820 0 None 38 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2 10.1016/s0960-894x(99)00214-0
44415598 77664 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccc(S(=O)(=O)N2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
CHEMBL209805 77664 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccc(S(=O)(=O)N2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.034
44415612 138426 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 6 6.0 CCOc1ccc2ccccc2c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
CHEMBL378512 138426 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 539 4 1 6 6.0 CCOc1ccc2ccccc2c1C(=O)NN1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.022
134149077 147791 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 4 2 5 3.9 CCC(C)Oc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3936976 147791 0 None 1 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 369 4 2 5 3.9 CCC(C)Oc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
681 1437 65 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -23 38 Bovine 6.2 pKi = 6.2 Binding
Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site.
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
228 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
33 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
6005 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
CHEMBL53 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
DB00714 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Binding affinity to dopamine D1 receptor low binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor low binding site by radioligand displacement assay
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/ml1001689
117774495 131902 0 None - 1 Human 6.2 pKi = 6.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 396 4 1 6 2.7 Cc1cc(Oc2ncccc2N2CC(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697565 131902 0 None - 1 Human 6.2 pKi = 6.2 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 396 4 1 6 2.7 Cc1cc(Oc2ncccc2N2CC(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
40152769 200123 1 None -107 2 Human 5.2 pKi = 5.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL606939 200123 1 None -107 2 Human 5.2 pKi = 5.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)[C@@H]1CCc2c(O)cccc2C1 10.1021/jm00115a012
45481888 197336 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
CHEMBL585740 197336 0 None -5 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 610 11 2 9 4.8 COc1ccccc1N1CCN(CCCn2cc(CCCN3CCc4cc(O)c(O)cc4C(c4cccc(C)c4)C3)nn2)CC1 10.1016/j.bmc.2009.06.019
21171 186393 27 None 1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
CHEMBL490533 186393 27 None 1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.12.016
135515431 4182 30 None -10 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 1 2 6 2.6 CN1CCN(C2=Nc3ccccc3Nc3sc(CO)cc32)CC1 10.1016/S0960-894X(96)00567-7
CHEMBL100454 4182 30 None -10 3 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1In vitro binding affinity of compound against dopamine neuronal Dopamine receptor D1
ChEMBL 328 1 2 6 2.6 CN1CCN(C2=Nc3ccccc3Nc3sc(CO)cc32)CC1 10.1016/S0960-894X(96)00567-7
72699818 114697 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 341 3 1 4 4.1 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344466 114697 0 None -5 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 341 3 1 4 4.1 COc1cc2c(cc1O)[C@@H]1Cc3sc(CC4CC4)cc3CN1CC2 10.1016/j.bmc.2014.09.024
11504230 77840 0 None -870 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL210567 77840 0 None -870 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
228 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
33 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
6005 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
CHEMBL53 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
DB00714 441 26 None -35 24 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2012.07.025
44448061 94406 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253736 94406 0 None 1 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 10.1021/jm060959i
45270813 195014 0 None -776 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
CHEMBL564709 195014 0 None -776 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccc(N2CCN(Cc3c(C)nc4cc(C)nc(C)n34)CC2)cc1 10.1016/j.bmc.2009.05.015
71457956 78015 0 None -87 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111527 78015 0 None -87 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
76325152 105890 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 105890 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 105890 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
10037962 204980 0 None -51 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1ABinding affinity against dopamine receptor D1A
ChEMBL 254 0 1 2 3.4 c1cc2c3c(c1)c1c(n3CCNC2)CCCCCC1 10.1016/j.bmcl.2004.02.100
CHEMBL89738 204980 0 None -51 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1ABinding affinity against dopamine receptor D1A
ChEMBL 254 0 1 2 3.4 c1cc2c3c(c1)c1c(n3CCNC2)CCCCCC1 10.1016/j.bmcl.2004.02.100
118711254 113453 0 None -147 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 358 4 2 3 4.6 CN1CCc2cc(NCc3ccccc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
CHEMBL3325904 113453 0 None -147 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 358 4 2 3 4.6 CN1CCc2cc(NCc3ccccc3)c(O)cc2C(c2ccccc2)C1 10.1016/j.ejmech.2014.07.059
42626315 55957 0 None -1445 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 439 8 2 6 3.2 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL1627320 55957 0 None -1445 2 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 439 8 2 6 3.2 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
10363751 162530 0 None -1584 3 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 402 6 0 4 3.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(F)cc2)C1 10.1016/s0960-894x(99)00201-2
CHEMBL417661 162530 0 None -1584 3 Rat 5.2 pKi = 5.2 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 402 6 0 4 3.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCC(c2ccc(F)cc2)C1 10.1016/s0960-894x(99)00201-2
45269974 13511 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1194307 13511 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL550792 13511 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 371 3 2 3 5.3 CCCN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
91899756 128917 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cc(=O)[nH]nc1C nan
CHEMBL3671295 128917 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 332 3 2 4 3.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cc(=O)[nH]nc1C nan
9888555 165052 11 None -3235 8 Human 6.2 pKi = 6.2 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 165052 11 None -3235 8 Human 6.2 pKi = 6.2 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
25071691 111295 0 None -2818 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287403 111295 0 None -2818 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
6469918 79481 13 None -954 6 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL212370 79481 13 None -954 6 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
71450812 78013 0 None -338 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL2111525 78013 0 None -338 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 455 8 1 5 4.7 COc1ccc(Br)cc1-c1nc(CNCC2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
3036864 201066 16 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1256645 201066 16 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL1814790 201066 16 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
CHEMBL62 201066 16 None -2 27 Rat 6.2 pKi = 6.2 Binding
Binding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranesBinding affinity towards dopamine (D1) receptor using [3H]spiperone was determined in rat striatal membranes
ChEMBL 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 10.1021/jm00051a008
10360174 167685 1 None -2 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 344 0 0 5 3.5 CN1CCN(C2=Nc3cccnc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
CHEMBL433744 167685 1 None -2 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 344 0 0 5 3.5 CN1CCN(C2=Nc3cccnc3Sc3ccc(Cl)cc32)CC1 10.1021/jm00030a011
10660476 47109 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
CHEMBL154468 47109 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm991034o
15654856 201335 0 None 2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 311 0 1 5 2.6 CN1CCN(C2=Nc3cccnc3Nc3ccc(F)cc32)CC1 10.1021/jm00067a009
CHEMBL63347 201335 0 None 2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 311 0 1 5 2.6 CN1CCN(C2=Nc3cccnc3Nc3ccc(F)cc32)CC1 10.1021/jm00067a009
42625207 55941 0 None -257 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL1627304 55941 0 None -257 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 421 7 1 5 4.0 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
44323890 205190 0 None 1 4 Rat 7.2 pKi = 7.2 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL90977 205190 0 None 1 4 Rat 7.2 pKi = 7.2 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 316 1 0 2 4.2 C/C=C1/c2ccccc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
3039881 173685 6 None 4 3 Human 7.2 pKi = 7.2 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
CHEMBL45491 173685 6 None 4 3 Human 7.2 pKi = 7.2 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1Binding affinity determined in radioreceptor binding assay by using [3H]SCH-23390 radioligand against dopamine receptor D1
ChEMBL 337 1 0 1 5.0 CN(C)C1C=CC2(CC1)c1ccccc1CCc1ccc(Cl)cc12 10.1021/jm00109a026
44415638 79474 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212334 79474 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C#N)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415490 138708 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL378886 138708 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 513 2 1 5 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc(C(F)(F)F)cc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
134150645 151113 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 475 7 2 5 5.5 CCCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3963862 151113 0 None 10 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 475 7 2 5 5.5 CCCCCCOc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
44300069 194443 0 None 35 2 Rat 7.2 pKi = 7.2 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL56100 194443 0 None 35 2 Rat 7.2 pKi = 7.2 Binding
In vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenatesIn vitro affinity of compound towards dopamine (D1) receptor was determined by measuring their ability to displace [3H]SCH-23,390 from rat striatal homogenates
ChEMBL 295 0 2 3 3.0 CN1CCc2cc(O)c(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
41532205 77880 1 None -954 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL210717 77880 1 None -954 4 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 336 4 0 4 3.3 Fc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
11504230 77840 0 None -1023 7 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
CHEMBL210567 77840 0 None -1023 7 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 497 8 1 4 4.9 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm100899z
145990141 166226 0 None -323 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4283982 166226 0 None -323 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 388 7 2 4 3.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(Cl)cc1)CC2 10.1021/acsmedchemlett.8b00229
44454709 97069 0 None -5248 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
CHEMBL270406 97069 0 None -5248 5 Pig 5.2 pKi = 5.2 Binding
Binding affinity to pig cortical membrane dopamine D1 receptorBinding affinity to pig cortical membrane dopamine D1 receptor
ChEMBL 404 9 0 6 3.4 COc1cc(CN2CCN(c3ccccc3OC)CC2)c(OCCF)cc1OC 10.1016/j.bmcl.2007.12.026
12888943 9478 0 None -812 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL112395 9478 0 None -812 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 6 2 4 3.8 CNc1cc(OC)c(C(=O)NC2CCN(Cc3ccccc3)CC2)cc1Cl 10.1016/s0960-894x(03)00678-4
10660476 47109 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
CHEMBL154468 47109 0 None - 1 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 10.1021/jm060959i
25139332 183737 0 None -7 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL484204 183737 0 None -7 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 352 11 1 2 5.0 CCCN(CCC)CCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
16121920 194202 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL558838 194202 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 380 5 1 6 2.7 COc1ccccc1N1CCN(Cc2c(C)[nH]c3nc(N(C)C)ncc23)CC1 10.1016/j.bmc.2009.05.015
45267435 194317 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
CHEMBL559868 194317 0 None -1047 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1nccc2c(CN3CCN(c4ccccc4)CC3)c[nH]c12 10.1016/j.bmc.2009.05.015
52937776 60842 0 None -9549 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765629 60842 0 None -9549 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)C1CCn2nccc2C1 10.1021/jm101639t
127046948 139540 0 None -295 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800468 139540 0 None -295 6 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 488 12 4 6 4.1 COc1cc(CCNC[C@@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
118709168 112916 0 None -33 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318840 112916 0 None -33 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1000 29 0 8 14.4 O=C(CCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12050200 101620 0 None -128 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL302186 101620 0 None -128 4 Bovine 5.2 pKi = 5.2 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 6 1 4 4.6 c1ccc(CN2CCC(NCc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
11708363 71558 1 None -23 4 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL197159 71558 1 None -23 4 Pig 4.2 pKi = 4.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 minsDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine cerebral cortex after 60 mins
ChEMBL 221 5 0 3 2.3 CCCN(CCC)[C@@H]1CCn2nccc2C1 10.1021/jm101639t
44329057 206256 0 None -93 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97283 206256 0 None -93 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
86767109 128924 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 6 3.5 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
CHEMBL3671301 128924 0 None - 1 Human 7.2 pKi = 7.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 346 3 1 6 3.5 Cc1ncnc(C#N)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
52940985 17404 0 None -69 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
CHEMBL1258155 17404 0 None -69 5 Pig 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 369 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3ccc(Cl)cc3)CC2)c1 10.1021/jm100899z
10666053 99921 0 None -1 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL289927 99921 0 None -1 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
156013324 176919 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 310 2 1 4 3.0 COc1cc2c3c(c1OC)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4639398 176919 0 None -4 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 310 2 1 4 3.0 COc1cc2c3c(c1OC)-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
76325152 105890 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3115579 105890 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
CHEMBL3139262 105890 0 None -645 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 359 9 2 4 4.0 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(OCCCCF)cc1)CC2 10.1021/jm401384w
90140337 128892 0 None - 1 Human 6.2 pKi = 6.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 4 2 6 3.1 COc1cnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c2c[nH]nc12 nan
CHEMBL3671271 128892 0 None - 1 Human 6.2 pKi = 6.2 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 363 4 2 6 3.1 COc1cnc(Oc2ccc(-c3c(C)n[nH]c(=O)c3C)cc2)c2c[nH]nc12 nan
10333842 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
CHEMBL27559 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from dopamine D1 receptor in rat striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm701045j
10333842 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.06.016
CHEMBL27559 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat corpus striatum
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.06.016
10333842 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.11.025
CHEMBL27559 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrainDisplacement of [3H]SCH23390 from dopamine D1 receptor in rat forebrain
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1016/j.bmcl.2008.11.025
681 1437 65 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
940 1437 65 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
947 1437 65 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
CHEMBL59 1437 65 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
DB00988 1437 65 None -23 38 Bovine 8.2 pKi = 8.2 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm991098z
14371639 102648 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00170a025
CHEMBL307790 102648 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00170a025
46231646 198781 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(N)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL598515 198781 0 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 328 0 2 3 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccc(N)cc3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
14371639 102648 0 None - 1 Human 8.2 pKi = 8.2 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00081a010
CHEMBL307790 102648 0 None - 1 Human 8.2 pKi = 8.2 Binding
Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1
ChEMBL 299 0 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3C[C@@H]21 10.1021/jm00081a010
44415826 79981 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL214503 79981 0 None 32 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 571 2 1 5 5.1 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccccc3I)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415705 138137 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 2 2 6 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL377756 138137 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 2 2 6 5.1 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3c(N)cccc3C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
1218 3559 24 None -11 7 Human 8.2 pKi = 8.2 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/jm00116a004
938 3559 24 None -11 7 Human 8.2 pKi = 8.2 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/jm00116a004
CHEMBL353335 3559 24 None -11 7 Human 8.2 pKi = 8.2 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 10.1021/jm00116a004
11306892 199621 0 None 79 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)Nc4c(Cl)cccc4Cl)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
CHEMBL604129 199621 0 None 79 2 Human 8.2 pKi = 8.2 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 515 2 3 3 6.9 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3cccc(NC(=O)Nc4c(Cl)cccc4Cl)c3CC[C@@H]21 10.1016/j.bmcl.2009.12.100
15069446 197034 0 None 213 2 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 293 0 1 2 3.6 Cc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
CHEMBL58205 197034 0 None 213 2 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 293 0 1 2 3.6 Cc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1N(C)CC2 10.1021/jm00128a038
44415594 79849 0 None 177 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL213882 79849 0 None 177 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 495 2 1 5 5.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccc4ccccc4c3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
135398737 944 89 None -44 91 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
38 944 89 None -44 91 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
722 944 89 None -44 91 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
CHEMBL42 944 89 None -44 91 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
DB00363 944 89 None -44 91 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1007/s00044-012-0055-5
71109804 87078 0 None 12 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 10.1016/j.bmc.2012.12.016
CHEMBL2334882 87078 0 None 12 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin) expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 323 1 1 4 3.0 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCC4 10.1016/j.bmc.2012.12.016
71109805 87077 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
CHEMBL2334881 87077 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4 nan
15937727 116078 0 None 158 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 307 1 1 2 4.6 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCCC2)C1 10.1016/S0960-894X(00)80155-9
CHEMBL336532 116078 0 None 158 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 307 1 1 2 4.6 CN1CCc2cc(Cl)c(O)cc2C(C2CCCCCC2)C1 10.1016/S0960-894X(00)80155-9
11536995 139025 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL379662 139025 1 None 3 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1cccc2c1Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
86764210 131916 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 1 4 4.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697579 131916 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 347 4 1 4 4.4 Cc1cc(Oc2ncccc2C2CC2)ccc1-c1c(C)n[nH]c(=O)c1C nan
44415552 79830 0 None 194 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
CHEMBL213795 79830 0 None 194 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 459 2 1 5 4.8 Cc1ccc(C(=O)NN2c3ccc(Cl)cc3N=C(N3CCN(C)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2006.06.022
134157446 153252 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 371 5 2 6 2.8 COCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3982215 153252 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 371 5 2 6 2.8 COCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
9901453 127966 0 None -2 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 315 1 0 4 3.3 CN1CCN(C2=Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm0309811
CHEMBL366679 127966 0 None -2 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 315 1 0 4 3.3 CN1CCN(C2=Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm0309811
44415595 79483 0 None 27 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 3 1 6 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212383 79483 0 None 27 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 528 3 1 6 5.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3N3CCCCC3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
127031423 138233 0 None 6 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 369 5 1 5 3.9 CCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
CHEMBL3780506 138233 0 None 6 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 369 5 1 5 3.9 CCCOc1ccc2c(c1OC)CN1CCc3cc(OC)c(O)cc3C1C2 10.1016/j.bmc.2016.03.037
162672733 182437 0 None 102 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 317 1 1 3 4.8 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
CHEMBL4793813 182437 0 None 102 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 317 1 1 3 4.8 Cc1ccc2c(c1)C(C1=C[C@H](C)N(C)CC1)=Nc1ccccc1N2 10.1016/j.bmcl.2020.127563
44316024 203742 0 None -2 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 249 5 2 3 2.9 CCCCN1CCCC1Cc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL80369 203742 0 None -2 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390
ChEMBL 249 5 2 3 2.9 CCCCN1CCCC1Cc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
70690498 75714 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
CHEMBL2057445 75714 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2 10.1016/j.bmc.2012.05.057
74223774 128903 0 None - 1 Human 8.1 pKi = 8.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 5 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc2nccn12 nan
CHEMBL3671282 128903 0 None - 1 Human 8.1 pKi = 8.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 355 3 1 5 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)ncc2nccn12 nan
17756213 149172 1 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
CHEMBL394779 149172 1 None -1 5 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 281 0 1 2 3.4 CN1CCCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm070388+
135398745 2869 108 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
47 2869 108 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
CHEMBL715 2869 108 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
DB00334 2869 108 None -26 65 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C5MD00258C
10540201 99765 0 None 4 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL288536 99765 0 None 4 2 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2 10.1021/jm970038v
1353 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
3559 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
86 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
CHEMBL54 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
DB00502 1880 85 None -74 85 Rat 7.2 pKi = 7.2 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm991034o
10333842 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
CHEMBL27559 97979 1 None -50 8 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 2 1 2 3.9 CCCN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3 10.1021/jm060959i
13678336 200297 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 289 1 3 3 3.1 Oc1c(O)c(-c2ccccc2)c2c(c1Cl)CCNCC2 10.1021/jm00160a018
CHEMBL60808 200297 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
ChEMBL 289 1 3 3 3.1 Oc1c(O)c(-c2ccccc2)c2c(c1Cl)CCNCC2 10.1021/jm00160a018
10610641 98462 0 None -47 5 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 249 0 0 1 3.7 Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL27940 98462 0 None -47 5 Rat 6.2 pKi = 6.2 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 249 0 0 1 3.7 Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
11638780 76742 0 None -1737 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL207488 76742 0 None -1737 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 345 3 0 5 2.8 Fc1ccc(N2CCN(Cc3cn4nc(Cl)ccc4n3)CC2)cc1 10.1021/jm060166w
70686495 76216 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccc(Br)cc3)[C@H]21 10.1016/j.ejmech.2012.07.025
CHEMBL2062856 76216 0 None -1 3 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H](CO)[C@H]2CN(Cc3ccccc3)[C@H](c3ccc(Br)cc3)[C@H]21 10.1016/j.ejmech.2012.07.025
44372198 48875 0 None -239 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL156198 48875 0 None -239 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 420 4 0 4 5.1 Fc1ccc(-c2cccc3c(CN4CCN(c5ccc(Cl)cc5)CC4)cnn23)cc1 10.1016/s0960-894x(01)00814-9
44270444 49059 0 None -138 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
CHEMBL156369 49059 0 None -138 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 340 3 0 4 3.6 Cc1cccn2ncc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1016/s0960-894x(01)00814-9
11078813 111526 0 None -19 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
CHEMBL328925 111526 0 None -19 4 Bovine 4.2 pKi = 4.2 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 356 4 1 5 2.8 OCc1cnn2cccc(CN3CCN(c4ccc(Cl)cc4)CC3)c12 10.1021/jm015522j
12928483 13236 0 None 6 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 239 1 2 2 2.7 Oc1ccc2c(c1)C(c1ccccc1)CNCC2 10.1021/jm00079a008
CHEMBL1192258 13236 0 None 6 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 239 1 2 2 2.7 Oc1ccc2c(c1)C(c1ccccc1)CNCC2 10.1021/jm00079a008
CHEMBL543472 13236 0 None 6 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatumInhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 from canine striatum
ChEMBL 239 1 2 2 2.7 Oc1ccc2c(c1)C(c1ccccc1)CNCC2 10.1021/jm00079a008
44320116 163556 0 None 7 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL420972 163556 0 None 7 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
10810641 9302 0 None -21 2 Rat 5.2 pKi = 5.2 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 394 7 0 4 3.8 O=C(CCCN1CCN(CC2CC(=O)c3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL111509 9302 0 None -21 2 Rat 5.2 pKi = 5.2 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 394 7 0 4 3.8 O=C(CCCN1CCN(CC2CC(=O)c3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm981094e
CHEMBL544089 9302 0 None -21 2 Rat 5.2 pKi = 5.2 Binding
In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.In vitro ability to displace [3H]SCH-23390 binding from Dopamine receptor D1 in rat striatal membrane.
ChEMBL 394 7 0 4 3.8 O=C(CCCN1CCN(CC2CC(=O)c3ccccc32)CC1)c1ccc(F)cc1 10.1021/jm981094e
156011233 176725 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 334 3 1 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4636589 176725 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 334 3 1 4 3.0 C#CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
44415599 137922 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccccc1S(=O)(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
CHEMBL377452 137922 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 480 2 0 5 4.8 Cc1ccccc1S(=O)(=O)N1c2ccc(Cl)cc2N=C(N2CCN(C)CC2)c2ccccc21 10.1016/j.bmcl.2006.06.034
9857902 60480 0 None -26 5 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 311 1 0 4 3.5 Cc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
CHEMBL176169 60480 0 None -26 5 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 311 1 0 4 3.5 Cc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
15115512 9307 2 None -104 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 324 6 2 3 3.8 CCCN(CCc1ccc(N)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL111532 9307 2 None -104 2 Human 6.2 pKi = 6.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 324 6 2 3 3.8 CCCN(CCc1ccc(N)cc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
25093832 155339 0 None -2290 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155339 0 None -2290 5 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
11574902 78041 0 None -28183 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
CHEMBL211164 78041 0 None -28183 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 400 4 0 5 3.4 COc1ccccc1N1CCN(Cc2cn3cc(Br)ccc3n2)CC1 10.1021/jm060166w
44339953 109212 0 None -707 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
CHEMBL322802 109212 0 None -707 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 387 5 2 4 3.6 COc1cc(N)c(Cl)cc1C(=O)N[C@H]1CCN(Cc2ccccc2)C[C@@H]1C 10.1016/s0960-894x(03)00678-4
17469721 77671 6 None -22 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL209832 77671 6 None -22 4 Pig 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 320 4 0 6 2.0 c1ccc(-n2cc(CN3CCN(c4ncccn4)CC3)cn2)cc1 10.1016/j.bmcl.2006.02.075
45271691 193880 0 None -107 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
CHEMBL554692 193880 0 None -107 4 Bovine 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 369 3 0 5 3.6 Cc1cc2nc(C)c(CN3CCN(c4ccc(Cl)cc4)CC3)n2c(C)n1 10.1016/j.bmc.2009.05.015
44372338 53563 0 None -2511 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160454 53563 0 None -2511 4 Bovine 5.2 pKi = 5.2 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 398 4 0 4 3.9 C[Si](C)(C)c1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
44329099 206341 0 None -40 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97750 206341 0 None -40 3 Bovine 4.2 pKi = 4.2 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2ccc(C)c2C1 10.1016/s0960-894x(01)00564-9
25186023 187161 0 None -50118 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl 10.1021/jm800689g
CHEMBL495572 187161 0 None -50118 4 Rat 5.2 pKi = 5.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
ChEMBL 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl 10.1021/jm800689g
10527469 155724 1 None -1548 16 Mouse 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 155724 1 None -1548 16 Mouse 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 using [3H]SCH-23390 as radioligand
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
10421583 98726 1 None -9 5 Rat 6.1 pKi = 6.1 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 235 0 0 1 3.4 CN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm960189i
CHEMBL281357 98726 1 None -9 5 Rat 6.1 pKi = 6.1 Binding
In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1In vitro displacement of [3H]SCH-23390 binding to rat striatal Dopamine receptor D1
ChEMBL 235 0 0 1 3.4 CN1CCc2cccc3c2[C@H]1Cc1ccccc1-3 10.1021/jm960189i
CHEMBL4520788 212225 6 None -33 25 Human 6.1 pKi = 6.1 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a DRD1Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a DRD1
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 nan
72699904 114701 0 None -60 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 377 5 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344470 114701 0 None -60 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 377 5 1 4 4.7 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
44385715 60749 0 None 1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 280 1 0 2 3.8 CN1CCc2cccc3c2c(cn3-c2ccc(F)cc2)C1 10.1016/s0960-894x(98)00138-3
CHEMBL176476 60749 0 None 1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 280 1 0 2 3.8 CN1CCc2cccc3c2c(cn3-c2ccc(F)cc2)C1 10.1016/s0960-894x(98)00138-3
156011458 176730 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 2 2 3 3.4 COc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4636741 176730 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 347 2 2 3 3.4 COc1cc2c(cc1O)C(c1ccccc1Br)CNCC2 10.1016/j.bmcl.2020.127305
228 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
33 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
6005 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
CHEMBL53 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
DB00714 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.bmc.2009.04.047
228 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
33 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
6005 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
CHEMBL53 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
DB00714 441 26 None -35 24 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counterDisplacement of [3H]SCH23390 from human D1 dopamine receptor expressed in Ltk fibroblast cells after 60 mins by liquid scintillation counter
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1016/j.ejmech.2011.04.028
13869641 112904 0 None -29 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318824 112904 0 None -29 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 431 8 0 4 5.4 CCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
9819674 12825 0 None -10 5 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL118919 12825 0 None -10 5 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
74223827 128920 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 335 3 1 5 4.0 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
CHEMBL3671298 128920 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 335 3 1 5 4.0 Cc1ncnc(C)c1-c1ccc(Oc2nccc3n[nH]cc23)cc1F nan
9819674 12825 0 None -10 5 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
CHEMBL118919 12825 0 None -10 5 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 347 3 1 5 2.4 OCCN1CCN(C2Cn3cccc3Sc3ccc(F)cc32)CC1 10.1021/jm010982y
11208237 100505 0 None 109 2 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 279 0 1 2 3.3 CN1CCc2ccc(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
CHEMBL294221 100505 0 None 109 2 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 279 0 1 2 3.3 CN1CCc2ccc(O)cc2[C@H]2c3ccccc3CC[C@@H]21 10.1021/jm00128a038
10849018 13824 0 None -120 3 Rat 6.1 pKi = 6.1 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 261 1 0 1 4.1 C=Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
CHEMBL119656 13824 0 None -120 3 Rat 6.1 pKi = 6.1 Binding
Affinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 261 1 0 1 4.1 C=Cc1cccc2c1-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960189i
44400585 68313 0 None -1949 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL191962 68313 0 None -1949 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
10425969 100539 3 None -1862 4 Bovine 5.1 pKi = 5.1 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
CHEMBL294459 100539 3 None -1862 4 Bovine 5.1 pKi = 5.1 Binding
Ability to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determinedAbility to displace D1 selective radioligand [3H]-SCH- 23390 in bovine striatal membrane preparations was determined
ChEMBL 317 4 1 4 2.8 N#CC(C#N)=Cc1cc(CN2CCN(c3ccccc3)CC2)c[nH]1 10.1016/s0960-894x(99)00302-9
14809026 204073 2 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL83080 204073 2 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
14809026 204073 2 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
CHEMBL83080 204073 2 None -4 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)Binding affinity was determined by measuring the ability to displace [125I]SCH-23982 from Dopamine receptor D1 in rat caudate (in vitro)
ChEMBL 271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O 10.1021/jm00173a005
10551026 101146 0 None -4677 6 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 101146 0 None -4677 6 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
44448067 154989 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
CHEMBL404240 154989 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
2 3210 19 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
54562 3210 19 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
CHEMBL240773 3210 19 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm901120h
12050194 201202 1 None -50 4 Bovine 4.1 pKi = 4.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL62703 201202 1 None -50 4 Bovine 4.1 pKi = 4.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 333 5 0 4 3.7 c1ccc(CN2CCN(Cc3coc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
133633 2210 46 None -100 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
177 2210 46 None -100 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
CHEMBL445102 2210 46 None -100 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptorDisplacement of [3H]SCH23390 from dopamine D1 receptor
ChEMBL 340 3 2 2 4.3 Clc1ccc(cc1)C1(O)CCN(CC1)Cc1c[nH]c2c1cccc2 10.1021/jm800532x
10378389 201554 1 None -14454 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL134807 201554 1 None -14454 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
CHEMBL64553 201554 1 None -14454 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 269 4 2 3 2.9 Oc1ccc2c(c1)O[C@@H](CNCc1ccccc1)CC2 10.1021/jm401384w
156020120 177459 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 340 3 0 5 3.4 COc1cc2c3c(c1OC)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4646927 177459 0 None -1 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 340 3 0 5 3.4 COc1cc2c3c(c1OC)-c1cc([N+](=O)[O-])ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
15654860 201966 1 None 2 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ncccc32)CC1 10.1021/jm00067a009
CHEMBL67355 201966 1 None 2 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 293 0 1 5 2.5 CN1CCN(C2=Nc3ccccc3Nc3ncccc32)CC1 10.1021/jm00067a009
45481840 196382 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 267 4 0 2 4.1 CCCCC1c2cc(OC)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
CHEMBL574110 196382 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 267 4 0 2 4.1 CCCCC1c2cc(OC)c(Cl)cc2CCN1C 10.1016/j.bmc.2009.05.079
6852376 91167 11 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
CHEMBL1467585 91167 11 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
CHEMBL24077 91167 11 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
CHEMBL503958 91167 11 None -3 5 Human 7.1 pKi = 7.1 Binding
Agonist activity at dopamine D1 receptor (unknown origin)Agonist activity at dopamine D1 receptor (unknown origin)
ChEMBL 255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 10.1021/ml400373j
10588326 158320 0 None 17 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
CHEMBL40950 158320 0 None 17 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2 10.1021/jm970038v
44436608 146223 0 None -870 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL392437 146223 0 None -870 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1cccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
167715 2832 12 None -954 5 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
969 2832 12 None -954 5 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
CHEMBL225230 2832 12 None -954 5 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm060959i
3033276 13066 1 None -1698 2 Rat 6.1 pKi = 6.1 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 307 2 2 3 3.6 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm00163a007
CHEMBL1190928 13066 1 None -1698 2 Rat 6.1 pKi = 6.1 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 307 2 2 3 3.6 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm00163a007
CHEMBL541867 13066 1 None -1698 2 Rat 6.1 pKi = 6.1 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
ChEMBL 307 2 2 3 3.6 Oc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(CC1CC1)CC3 10.1021/jm00163a007
25139331 169361 0 None -1 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
CHEMBL444128 169361 0 None -1 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 310 9 2 2 3.9 CCCNCCCCNC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800895v
24823920 96997 0 None -26 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
CHEMBL270056 96997 0 None -26 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 311 3 0 5 2.2 Fc1cccc(N2CCN(Cc3cnn4ccccc34)CC2)n1 10.1021/jm701375u
53325137 58286 0 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684128 58286 0 None -37 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 525 10 0 5 6.2 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCCN2CCN(c4ccccc4OC)CC2)c1-3 10.1016/j.bmc.2011.01.053
10324985 76428 7 None -5495 17 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL199824 76428 7 None -5495 17 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
CHEMBL2068762 76428 7 None -5495 17 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 423 7 0 8 1.7 COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1 10.1021/jm050725j
14659294 167426 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 301 0 2 3 3.5 CN1CCc2cc(Cl)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL431946 167426 0 None -3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 301 0 2 3 3.5 CN1CCc2cc(Cl)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
70692653 75713 0 None - 1 Human 7.1 pKi = 7.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
CHEMBL2057443 75713 0 None - 1 Human 7.1 pKi = 7.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 nan
70692653 75713 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
CHEMBL2057443 75713 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1016/j.bmc.2012.05.057
129012255 153844 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)C1Cc3c(c(OC)cc(OC)c3OC)CN1CC2 nan
CHEMBL3987156 153844 0 None - 1 Human 7.1 pKi = 7.1 Binding
Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.Radioligand Binding Assay: The affinity of compounds to D1 and D2 dopamine receptors were determined by competition binding assays. Membrane homogenates of HEK293T cells were stably transfected with D1, or D2 receptors. Duplicated tubes were incubated at 30° C. for 50 mins (for D1, and D2) with increasing concentrations of respective compound and with [3H]SCH23390 (for D1 dopamine receptors), or [3H]Spiperone (for dopamine D2 receptor) in a final volume of 200 μL binding buffer containing 50 mM Tris, 4 mM MgCl2, pH 7.4. Nonspecific binding was determined by parallel incubations with either 10 μM SCH23390 for D1, or Spiperone for D2 receptors respectively. The reaction was started by addition of membranes (15 ng/tube) and stopped by rapid filtration through Whatman GF/B glassfiber filter and subsequently washed with cold buffer (50 mM Tris, 5 mM EDTA, pH 7.4) using a Brandel 24-well cell harvester. Scintillation cocktail was added and the radioactivity was determined in a MicroBeta liquid scintillation counter.
ChEMBL 385 5 0 6 3.4 COc1cc2c(cc1OC)C1Cc3c(c(OC)cc(OC)c3OC)CN1CC2 nan
71454295 83665 0 None -933 7 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207641 83665 0 None -933 7 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 536 8 0 6 5.5 COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
57398875 68972 0 None -213 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928138 68972 0 None -213 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1005 30 2 17 4.7 COc1ccccc1N1CCN(CCCNC(=O)c2cnn3ccc(COCCOCCOCCOCCOCc4ccn5ncc(C(=O)NCCCN6CCN(c7ccccc7OC)CC6)c5c4)cc23)CC1 10.1016/j.bmc.2011.10.063
71474024 143935 0 None - 1 Human 6.1 pKi = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
CHEMBL3906676 143935 0 None - 1 Human 6.1 pKi = 6.1 Binding
Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.Reception Binding Assay: Different concentrations (10^−5 M-10^−11 M) of the compound of the invention and corresponding isotope receptor ligand as well as receptor protein were loaded into the reaction tube and incubated in 30° C. water bath for 60 minutes. The reaction was terminated in a refrigerator. The reaction mixture was put in a Millipore filter (millipore) cell sample collector, filtered through suction filtration using GF/C glass fiber filter paper, and dried. The resulting sample was placed into 0.5 mL tube. 500 μL liquid scintillation fluid was added and intensity of radioactivity was determined by counting. For dopamine D1 receptor: isotope receptor ligands [3H] SCH23390 (85.0 Ci/mmol) (D1-selective, purchased from Amersham Corporation), D1 receptor protein expressed in HEK-293 cells; For D2 dopamine receptor: isotope receptor ligands [3H] Spiperone (77.0 Ci/mmol) (D2-selective, purchased from Amersham Corporation); D2 receptor protein expressed in HEK-293 cells; For 5-HT1A receptor: isotope receptor ligands [3H] 8-OH-DPAT; 5-HT1A receptor protein expressed in HEK-293 cells; For 5-HT2A receptor: isotope receptor ligands [3H]-Ketanserin; 5-HT2A receptor protein expressed in HEK-293 cells.
ChEMBL 327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2 nan
10551026 101146 0 None -4677 6 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL298875 101146 0 None -4677 6 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 438 5 1 3 4.6 COc1c(C(=O)N[C@@H]2CCN(Cc3ccccc3)C2)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
15691846 202953 0 None -10 2 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 335 3 1 3 3.4 O=C1CC(CN2CCC(O)(c3ccccc3)CC2)Cc2ccccc21 10.1021/jm00111a046
CHEMBL73675 202953 0 None -10 2 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 335 3 1 3 3.4 O=C1CC(CN2CCC(O)(c3ccccc3)CC2)Cc2ccccc21 10.1021/jm00111a046
10672006 46556 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 467 5 1 3 5.5 CCCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
CHEMBL154015 46556 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 467 5 1 3 5.5 CCCN1CCc2c(Br)ccc(O)c2C1Cc1cc(OC)ccc1Br 10.1021/jm991034o
14198588 170941 2 None 2 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
CHEMBL446396 170941 2 None 2 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNC2c1ccccc1 10.1021/jm00051a008
14198589 62745 2 None 35 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@@H]2c1ccccc1 10.1021/jm00118a012
CHEMBL1788322 62745 2 None 35 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nMInhibition of [3H]SCH-23,390 binding to Dopamine receptor D1 at 0.25 nM
ChEMBL 259 1 2 2 3.3 Oc1cc2c(cc1Cl)CCN[C@@H]2c1ccccc1 10.1021/jm00118a012
9928332 96732 4 None -371 9 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assayCompound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assay
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/0960-894X(95)00398-D
CHEMBL268258 96732 4 None -371 9 Rat 6.1 pKi = 6.1 Binding
Compound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assayCompound was evaluated for its binding affinity to Dopamine receptor D1 in rat striatum using [3H]- SCH-23390 radioligand assay
ChEMBL 349 6 0 3 5.0 COc1cccc2c1CCC[C@H]2CN(C)CCc1ccc2ccoc2c1 10.1016/0960-894X(95)00398-D
2585 790 100 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 790 100 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 790 100 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 790 100 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 790 100 None -112 22 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
10665177 22941 0 None 56 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 344 5 2 3 3.8 NCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL133094 22941 0 None 56 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 344 5 2 3 3.8 NCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
10620219 6940 0 None 46 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 386 8 2 3 4.8 CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL108480 6940 0 None 46 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 386 8 2 3 4.8 CNCCCCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
1353 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
3559 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
86 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
CHEMBL54 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
DB00502 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00030a011
45482152 196333 0 None -131 4 Pig 6.1 pKi = 6.1 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
CHEMBL573792 196333 0 None -131 4 Pig 6.1 pKi = 6.1 Binding
Binding affinity to pig dopamine D1 receptorBinding affinity to pig dopamine D1 receptor
ChEMBL 517 9 1 8 3.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cn(-c2ccc([N+](=O)[O-])cc2)nn1 10.1016/j.bmc.2009.06.041
4420454 55966 6 None -41 5 Bovine 6.1 pKi = 6.1 Binding
Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
CHEMBL162762 55966 6 None -41 5 Bovine 6.1 pKi = 6.1 Binding
Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.Dissociation constant of compound on one-site model Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site.
ChEMBL 205 5 0 1 3.2 C#CC1=CCC(N(CCC)CCC)CC1 10.1021/jm991098z
44400500 165507 0 None -380 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
CHEMBL425731 165507 0 None -380 5 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL None None None None 10.1021/jm050170s
10980338 167445 0 None -2454 4 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
CHEMBL432059 167445 0 None -2454 4 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390
ChEMBL 326 3 0 4 3.3 Clc1ccc(N2CCN(Cc3ccc4ccnn4c3)CC2)cc1 10.1021/jm015522j
10498094 32102 1 None -5370 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
CHEMBL141035 32102 1 None -5370 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranesDisplacement of [3H]SCH-23390 from Dopamine receptor D1 of bovine striatal membranes
ChEMBL 350 3 1 3 4.0 N#Cc1ccc2[nH]c(CN3CCN(c4ccccc4Cl)CC3)cc2c1 10.1021/jm0009989
44412494 77918 0 None -2630 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210955 77918 0 None -2630 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 352 4 0 4 3.8 Clc1ccc(N2CCN(Cc3cnn(-c4ccccc4)c3)CC2)cc1 10.1016/j.bmcl.2006.02.075
137643132 157506 0 None -6309 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
CHEMBL4085920 157506 0 None -6309 6 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 503 7 1 7 3.8 CC(C)(C)c1nc(N2CCN(CCCCNC(=O)c3cc4ccccn4n3)CC2)cc(C(F)(F)F)n1 10.1016/j.bmc.2017.04.036
44381146 58199 0 None -18 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL168372 58199 0 None -18 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
11639064 189349 0 None -426 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 359 1 3 4 4.2 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL458579 189349 0 None -426 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 359 1 3 4 4.2 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL517028 189349 0 None -426 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 359 1 3 4 4.2 CN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
156012686 176788 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 352 3 1 4 3.4 COc1cc2c3c(c1OC)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4637673 176788 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 352 3 1 4 3.4 COc1cc2c3c(c1OC)-c1cc(NC(C)=O)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
118711258 113457 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)cc1 10.1016/j.ejmech.2014.07.059
CHEMBL3325908 113457 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 372 4 2 3 4.9 Cc1ccc(CNc2cc3c(cc2O)C(c2ccccc2)CN(C)CC3)cc1 10.1016/j.ejmech.2014.07.059
10040938 44109 0 None 1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 308 0 0 5 2.8 Cc1ccc2c(c1)N=C(N1CCN(C)CC1)c1cccnc1O2 10.1021/jm00030a011
CHEMBL151809 44109 0 None 1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 308 0 0 5 2.8 Cc1ccc2c(c1)N=C(N1CCN(C)CC1)c1cccnc1O2 10.1021/jm00030a011
10044041 48678 0 None -8 2 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 359 1 0 3 4.3 COc1ccc2c(c1)CC1c3c(ccc(Br)c3CCN1C)O2 10.1021/jm991034o
CHEMBL156011 48678 0 None -8 2 Rat 5.1 pKi = 5.1 Binding
Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand.
ChEMBL 359 1 0 3 4.3 COc1ccc2c(c1)CC1c3c(ccc(Br)c3CCN1C)O2 10.1021/jm991034o
1353 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
3559 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
86 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
CHEMBL54 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
DB00502 1880 85 None -74 85 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00067a009
156015018 176997 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 337 2 2 3 4.0 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
CHEMBL4640497 176997 0 None -2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 337 2 2 3 4.0 COc1cc2c(cc1O)C(c1c(Cl)cccc1Cl)CNCC2 10.1016/j.bmcl.2020.127305
129103318 166760 0 None -107 14 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
CHEMBL4293999 166760 0 None -107 14 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from dopamine D1 receptor in rat strriatum homogenates after 20 mins by liquid scintillation counting
ChEMBL 475 7 0 5 5.0 O=C(CCCCN1CCC(c2noc3cc(F)ccc23)CC1)c1cc2c3c(c1)CCN3C(=O)CC2 10.1021/acs.jmedchem.8b01096
3038495 700 30 None -616 19 Human 6.1 pKi = 6.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 700 30 None -616 19 Human 6.1 pKi = 6.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 700 30 None -616 19 Human 6.1 pKi = 6.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
3038495 700 30 None -616 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 700 30 None -616 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 700 30 None -616 19 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
3038495 700 30 None -512 19 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 700 30 None -512 19 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 700 30 None -512 19 Pig 6.1 pKi = 6.1 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranesInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 of porcine striatal membranes
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
44263882 96776 0 None -4 3 Bovine 5.1 pKi = 5.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
CHEMBL268558 96776 0 None -4 3 Bovine 5.1 pKi = 5.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 376 3 0 4 4.5 Clc1ccc(N2CCN(Cc3cnn4ccc5ccccc5c34)CC2)cc1 10.1016/s0960-894x(98)00692-1
25333445 77769 5 None -380 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
CHEMBL210318 77769 5 None -380 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membraneDisplacement of [3H]SCH-23390 from dopamine D1 receptor in porcine striatal membrane
ChEMBL 318 4 0 4 3.2 c1ccc(N2CCN(Cc3ccc(-n4cccn4)cc3)CC2)cc1 10.1016/j.bmcl.2006.02.075
44567596 189191 0 None -12 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 371 6 3 6 2.2 CN1CCc2cc(OCCOCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
CHEMBL516151 189191 0 None -12 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
ChEMBL 371 6 3 6 2.2 CN1CCc2cc(OCCOCCO)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2008.02.038
126720252 164123 0 None -269 12 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 164123 0 None -269 12 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
11222444 129662 0 None -27 3 Rat 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 369 4 0 5 4.1 CC(C)OCc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
CHEMBL367875 129662 0 None -27 3 Rat 5.1 pKi = 5.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 369 4 0 5 4.1 CC(C)OCc1ccc2n1C=C(N1CCN(C)CC1)c1ccccc1S2 10.1021/jm0309811
10873978 167921 0 None -18620 6 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
CHEMBL435218 167921 0 None -18620 6 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 445 7 1 4 5.1 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2o1 10.1021/jm0211220
117774120 131930 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 6 3.3 COC(=O)c1cccnc1Oc1ccc(-c2c(C)n[nH]c(=O)c2C)c(C)c1 nan
CHEMBL3697592 131930 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 365 4 1 6 3.3 COC(=O)c1cccnc1Oc1ccc(-c2c(C)n[nH]c(=O)c2C)c(C)c1 nan
26987 936 29 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 936 29 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 936 29 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 936 29 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 936 29 None -245 21 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
11631304 73029 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 330 2 1 1 4.6 c1ccc2c(c1)CCN(CC1CC1)CCc1c([nH]c3ccccc13)C2 10.1021/jm050846j
CHEMBL201432 73029 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Inhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assayInhibition of binding to human D1 receptor expressed in HEK 293 cells by radioligand binding assay
ChEMBL 330 2 1 1 4.6 c1ccc2c(c1)CCN(CC1CC1)CCc1c([nH]c3ccccc13)C2 10.1021/jm050846j
71817345 91547 0 None -158 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
CHEMBL2414992 91547 0 None -158 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation countingDisplacement of [3H]-SCH23390 from D1 receptor of Wistar rat striatal membranes after 1 hr by liquid scintillation counting
ChEMBL 281 3 2 3 3.5 CN(C)CCc1cc(O)c(O)c2c1ccc1ccccc12 10.1016/j.bmcl.2013.06.078
1588 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
28864 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
43 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
CHEMBL157138 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
DB00589 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1021/jm9800292
117949705 114699 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344468 114699 0 None -4 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 363 4 1 4 4.3 COc1cc2c(cc1O)[C@@H]1Cc3sc(CCCCl)cc3CN1CC2 10.1016/j.bmc.2014.09.024
134150400 151448 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 397 7 2 5 4.7 CCCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3966718 151448 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 397 7 2 5 4.7 CCCCCCOc1c(O)ccc2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
44436618 147390 0 None -512 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL393365 147390 0 None -512 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1ccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
11581237 138429 0 None -4897 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
CHEMBL378515 138429 0 None -4897 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 357 4 0 6 2.7 COc1ccccc1N1CCN(Cc2cn3nc(Cl)ccc3n2)CC1 10.1021/jm060166w
137637428 155695 0 None -9 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4064759 155695 0 None -9 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 250 1 1 5 0.9 CN1CCN(c2ccc(O)c3c2OCCO3)CC1 10.1016/j.bmc.2017.08.037
72545010 92693 0 None -229 5 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
CHEMBL2443003 92693 0 None -229 5 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 437 6 3 10 -0.4 COc1ccccc1N1CCN(Cc2cn([C@@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)nn2)CC1 10.1016/j.bmcl.2013.09.026
11091738 117589 0 None -11748 6 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
CHEMBL340641 117589 0 None -11748 6 Rat 5.1 pKi = 5.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2cn1 10.1021/jm0211220
11102533 17873 0 None -27 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 457 8 1 6 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2nc3ccccc3n3cccc23)CC1 10.1021/jm0211220
CHEMBL126590 17873 0 None -27 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 457 8 1 6 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2nc3ccccc3n3cccc23)CC1 10.1021/jm0211220
2274 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
44568533 188257 0 None 8 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 280 1 1 3 3.0 COc1cc2c3c(c1)-c1c(N)cccc1C[C@H]3N(C)CC2 10.1016/j.bmc.2008.05.077
CHEMBL506721 188257 0 None 8 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells
ChEMBL 280 1 1 3 3.0 COc1cc2c3c(c1)-c1c(N)cccc1C[C@H]3N(C)CC2 10.1016/j.bmc.2008.05.077
10758744 100041 0 None 11 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL291100 100041 0 None 11 2 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
162653702 179922 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
CHEMBL4753299 179922 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human dopamine D1 receptorBinding affinity to human dopamine D1 receptor
ChEMBL 337 1 1 3 5.2 C[C@@H]1C=C(C2=Nc3cc(Cl)ccc3Nc3ccccc32)CCN1C 10.1016/j.bmcl.2020.127563
11699469 77299 0 None -48 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
CHEMBL208847 77299 0 None -48 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 537 8 1 5 5.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3c4ccc(c3o2)CCc2ccc(cc2)CC4)CC1 10.1021/jm060138d
49783041 16989 0 None -1949 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1256171 16989 0 None -1949 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 597 7 1 3 6.8 O=C(NCCCCN1CCN(c2cc3ccc2CCc2ccc(cc2)CC3)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
10826543 10006 0 None -85 3 Rat 6.1 pKi = 6.1 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 1 2 3.7 CCc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
CHEMBL115524 10006 0 None -85 3 Rat 6.1 pKi = 6.1 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 279 1 1 2 3.7 CCc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1021/jm960188q
277 1274 55 None -47 45 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1274 55 None -47 45 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1274 55 None -47 45 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1274 55 None -47 45 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1274 55 None -47 45 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
44415382 80695 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 4 1 5 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL215611 80695 0 None 7 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 473 4 1 5 4.8 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)CCc3ccccc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
135398745 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
47 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
CHEMBL715 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
DB00334 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
pKi value for Dopamine receptor D1 binding sitepKi value for Dopamine receptor D1 binding site
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
44241718 193594 0 None -281 4 Bovine 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
CHEMBL551199 193594 0 None -281 4 Bovine 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 393 4 1 7 1.6 Cn1c(N2CCCC2)nc2c(CN3CCN(c4ccccn4)CC3)c[nH]c2c1=O 10.1016/j.bmc.2009.05.015
10709445 100893 0 None 26 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115377 100893 0 None 26 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL296993 100893 0 None 26 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
90644064 111544 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
CHEMBL3289649 111544 0 None -66 4 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 383 7 0 4 5.0 Clc1ccc(N2CCN(CCCCCc3nc4ccccc4o3)CC2)cc1 10.1016/j.bmc.2014.04.026
154724609 176025 1 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4514800 176025 1 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
CHEMBL4597637 176025 1 None -9 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 440 10 0 6 4.8 COc1ccc(F)cc1C1CC1CN(C)CCCSc1nnc(-c2ccccc2)n1C 10.1021/acs.jmedchem.9b01835
53325242 56775 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
CHEMBL1644978 56775 0 None -4 17 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
ChEMBL 537 8 1 2 7.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2018.10.036
15981509 141426 1 None 316 2 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
CHEMBL387250 141426 1 None 316 2 Pig 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenateDisplacement of [3H]SCH-23390 from dopamine D1-like receptor in porcine striata homogenate
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2 10.1021/jm0604979
130907 193017 5 None -7 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
CHEMBL53294 193017 5 None -7 4 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
ChEMBL 325 3 2 4 3.6 CCCN1CCc2cc(OC)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/ml1001689
10448562 114622 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL334350 114622 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
9995986 28058 1 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL137420 28058 1 None - 1 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@H]1c1ccccc1 10.1021/jm00051a008
10448562 114622 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL334350 114622 1 None 12 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 317 1 1 2 3.7 CN1CCc2cc(Br)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
117773687 131907 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.6 C=C(C)c1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
CHEMBL3697570 131907 0 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 363 4 1 5 3.6 C=C(C)c1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1 nan
130442534 166344 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
CHEMBL4286177 166344 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1 10.1021/acs.jmedchem.8b01622
10851849 169366 0 None 16 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
CHEMBL44414 169366 0 None 16 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2 10.1021/jm970038v
86764100 131955 22 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697617 131955 22 None - 1 Human 8.1 pKi = 8.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
86764100 131955 22 None - 1 Human 8.1 pKi = 8.1 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 391 3 1 5 3.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acs.jmedchem.8b01767
CHEMBL3697617 131955 22 None - 1 Human 8.1 pKi = 8.1 Binding
Partial agonist activity at human D1RPartial agonist activity at human D1R
ChEMBL 391 3 1 5 3.6 Cc1cc(Oc2ncccc2C(F)(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C 10.1021/acs.jmedchem.8b01767
9818423 107763 0 None 34 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 281 0 3 3 3.0 Cc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
CHEMBL319707 107763 0 None 34 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 281 0 3 3 3.0 Cc1ccc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/j.ejmech.2011.11.039
15937719 18624 0 None 72 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 249 1 1 2 2.6 C#CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
CHEMBL127843 18624 0 None 72 2 Rat 8.1 pKi = 8.1 Binding
Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.Binding affinity towards Dopamine receptor D1 in rat striatal tissue by [3H]-SCH- 23390 displacement.
ChEMBL 249 1 1 2 2.6 C#CCC1CN(C)CCc2cc(Cl)c(O)cc21 10.1016/S0960-894X(00)80155-9
11522339 74902 1 None -2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
CHEMBL203689 74902 1 None -2 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2c(O)cccc2CC1 10.1021/jm051237e
173871 3557 1 None -4 3 Human 8.1 pKi = 8.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/jm00116a004
936 3557 1 None -4 3 Human 8.1 pKi = 8.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/jm00116a004
CHEMBL1193571 3557 1 None -4 3 Human 8.1 pKi = 8.1 Binding
The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1The compound was evaluated for the dissociation constant for inhibiting the binding of [3H]-SCH- 23390 at dopamine receptor D1
ChEMBL 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 10.1021/jm00116a004
75201901 165872 14 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
CHEMBL4277264 165872 14 None -1 24 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.8b01622
11716438 140351 1 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
CHEMBL382010 140351 1 None 5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 267 0 1 2 3.0 CN1CCc2ccccc2Cc2cc(O)ccc2CC1 10.1021/jm051237e
163091 491 30 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
22 491 30 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
CHEMBL504548 491 30 None -147 10 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assayDisplacement of [3H]SCH-23390 from human cloned D1 dopamine receptor expressed in HEKT cells incubated for 90 mins by scintillation counting based radioligand binding assay
ChEMBL 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 10.1039/C5MD00258C
6603797 67676 3 None -2089 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL1257041 67676 3 None -2089 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL19130 67676 3 None -2089 3 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
44447997 95298 0 None -20 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 4 0 3 3.9 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1cccc(OC=O)c1-3 10.1021/jm060959i
CHEMBL258372 95298 0 None -20 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 325 4 0 3 3.9 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1cccc(OC=O)c1-3 10.1021/jm060959i
9888555 165052 11 None -3235 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
CHEMBL424294 165052 11 None -3235 8 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm900095y
137651936 156850 0 None -1000 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156850 0 None -1000 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
145990453 166392 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287062 166392 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 404 7 2 4 4.1 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc3ccccc3c1)CC2 10.1021/acsmedchemlett.8b00229
145993377 166415 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4287471 166415 0 None -295 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranesDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEKT cell membranes
ChEMBL 430 8 2 4 4.6 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(-c3ccccc3)cc1)CC2 10.1021/acsmedchemlett.8b00229
70690652 76217 0 None -3 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccc(Br)cc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
CHEMBL2062857 76217 0 None -3 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 442 7 1 3 4.6 CCN(CC)[C@@H]1[C@@H]2[C@@H](CN(Cc3ccccc3)[C@H]2c2ccc(Br)cc2)[C@H]1CO 10.1016/j.ejmech.2012.07.025
12050202 201607 0 None -204 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL64752 201607 0 None -204 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 441 7 1 5 4.5 COc1ccc(Br)cc1-c1nc(CN[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
44329067 206266 0 None -154 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2ccc(C=O)c2C1 10.1016/s0960-894x(01)00564-9
CHEMBL97319 206266 0 None -154 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@@H]1CCn2ccc(C=O)c2C1 10.1016/s0960-894x(01)00564-9
1240 8735 15 None -870 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL109684 8735 15 None -870 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
CHEMBL1256754 8735 15 None -870 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 309 6 1 2 4.2 CCCN(CCc1ccccc1)C1CCc2c(O)cccc2C1 10.1021/jm00115a012
44415758 79636 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 521 4 1 5 6.1 CC(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL212950 79636 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 521 4 1 5 6.1 CC(C)CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3Cl)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
57391896 68963 0 None -125 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928129 68963 0 None -125 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 1013 36 2 15 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
10758745 99967 0 None 18 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL2115373 99967 0 None 18 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
CHEMBL290438 99967 0 None 18 2 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligandIn vitro binding affinity against Dopamine receptor D1 like from rat caudate membrane using [125I]-SCH as radioligand
ChEMBL 329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21 10.1021/jm970038v
10427977 54180 0 None -660 4 Bovine 6.1 pKi = 6.1 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
CHEMBL160952 54180 0 None -660 4 Bovine 6.1 pKi = 6.1 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 350 3 0 4 3.3 C#Cc1cccc2c(CN3CCN(c4ccc(Cl)cc4)CC3)cnn12 10.1016/s0960-894x(01)00814-9
57395341 68969 0 None -426 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
CHEMBL1928135 68969 0 None -426 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 495 13 1 8 2.8 CCOCCOCc1ccn2ncc(C(=O)NCCCN3CCN(c4ccccc4OC)CC3)c2c1 10.1016/j.bmc.2011.10.063
9842468 9816 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
CHEMBL114375 9816 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm960143p
9842468 9816 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
CHEMBL114375 9816 0 None 4 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.Binding affinity against dopamine receptor D1 from rat striatal membranes using [3H]-SCH- 23390 as radioligand.
ChEMBL 372 6 1 3 4.4 CN(C)CCCCN1CCc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00021a018
10088453 65744 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1016/j.bmcl.2004.06.005
CHEMBL183776 65744 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1Binding affinity against Dopamine receptor D1
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1016/j.bmcl.2004.06.005
10088453 65744 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1007/s00044-012-0055-5
CHEMBL183776 65744 0 None -151 5 Human 6.1 pKi = 6.1 Binding
Binding affinity to dopamine D1 receptor (unknown origin)Binding affinity to dopamine D1 receptor (unknown origin)
ChEMBL 337 5 1 5 2.3 COc1ccccc1N1CCN(CCc2ccc3[nH]nnc3c2)CC1 10.1007/s00044-012-0055-5
9972693 167960 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cccnc3Sc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL435441 167960 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 310 0 0 5 2.9 CN1CCN(C2=Nc3cccnc3Sc3ccccc32)CC1 10.1021/jm00030a011
76321554 105922 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 105922 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 105922 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
14198577 196439 0 None 2 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 0 2 3.9 COc1cc2c(cc1Cl)CCN(C)C2c1ccccc1 10.1016/j.bmc.2009.05.079
CHEMBL574557 196439 0 None 2 2 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor in Wistar rat striatal membrane by liquid scintillation counting
ChEMBL 287 2 0 2 3.9 COc1cc2c(cc1Cl)CCN(C)C2c1ccccc1 10.1016/j.bmc.2009.05.079
154726353 175749 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4577162 175749 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595382 175749 1 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 467 12 2 3 5.9 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
1353 1880 85 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
3559 1880 85 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
86 1880 85 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
CHEMBL54 1880 85 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
DB00502 1880 85 None -38 85 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm049720x
11500677 140317 1 None -6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
CHEMBL381946 140317 1 None -6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 281 1 0 2 3.3 COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 10.1021/jm051237e
117773662 131917 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 3.7 CCc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)n(C)c(=O)[nH]c1=O nan
CHEMBL3697580 131917 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 387 5 1 5 3.7 CCc1c(-c2ccc(Oc3ncccc3C(F)F)cc2C)n(C)c(=O)[nH]c1=O nan
86764101 131956 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
CHEMBL3697618 131956 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cnc(Oc2ccc(-c3c(C)c(=O)[nH]c(=O)n3C)c(C)c2)c(Cl)c1 nan
117773616 131892 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.1 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697555 131892 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 4 1 5 3.1 CCc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
117773980 131910 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 2 6 2.3 Cc1cc(Oc2ncccc2O)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697573 131910 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 339 3 2 6 2.3 Cc1cc(Oc2ncccc2O)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44393393 123156 0 None -575 5 Pig 6.1 pKi = 6.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
CHEMBL362101 123156 0 None -575 5 Pig 6.1 pKi = 6.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 537 7 1 4 5.0 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)s1 10.1016/j.bmcl.2004.05.052
9888555 165052 11 None -3548 8 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
CHEMBL424294 165052 11 None -3548 8 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm100899z
44340084 9000 0 None -2238 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
CHEMBL109912 9000 0 None -2238 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 401 6 2 4 4.0 CNc1cc(OC)c(C(=O)N[C@H]2CCN(Cc3ccccc3)C[C@@H]2C)cc1Cl 10.1016/s0960-894x(03)00678-4
56597938 3877 1 None -870 9 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
7651 3877 1 None -870 9 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL2165126 3877 1 None -870 9 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 461 7 1 4 5.2 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCCN(CC1)c1cccc(c1Cl)Cl nan
117772974 131906 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 414 4 1 6 3.0 Cc1cc(Oc2ncccc2N2CC(F)(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697569 131906 0 None - 1 Human 6.1 pKi = 6.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 414 4 1 6 3.0 Cc1cc(Oc2ncccc2N2CC(F)(F)C2)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44415648 79760 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213472 79760 0 None 15 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 489 2 1 7 4.2 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3ccc4c(c3)OCO4)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
17755868 142586 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
CHEMBL389559 142586 1 None 1 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptorDisplacement of [3H]SCH 23390 from human dopamine D1 receptor
ChEMBL 295 0 1 2 3.8 CN1CCCc2ccccc2Cc2ccc(O)cc2CCC1 10.1021/jm070388+
44401243 167929 0 None -34 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
CHEMBL435301 167929 0 None -34 9 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to human Dopamine receptor D1
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1CC2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1021/jm049632c
156022132 177643 0 None -3 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 4 1 4 3.6 C=CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
CHEMBL4649785 177643 0 None -3 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 336 4 1 4 3.6 C=CCOc1c(OC)cc2c3c1-c1cc(N)ccc1CC3N(C)CC2 10.1016/j.bmcl.2020.127053
10085358 109730 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
CHEMBL323771 109730 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranesBinding affinity towards dopamine receptor D1 using [3H]SCH-23390 was determined in rat striatal membranes
ChEMBL 285 0 1 2 3.5 Oc1cc2c(cc1Cl)CCN1CCc3ccccc3C21 10.1021/jm00051a008
44448064 94433 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
CHEMBL253947 94433 0 None 1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 10.1021/jm060959i
44264641 203094 1 None -11 3 Bovine 4.1 pKi = 4.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
CHEMBL7505 203094 1 None -11 3 Bovine 4.1 pKi = 4.1 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 230 2 0 4 1.1 CN1CCN(Cc2cnn3ccccc23)CC1 10.1016/s0960-894x(98)00692-1
44329293 109579 0 None -75 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
CHEMBL323557 109579 0 None -75 3 Bovine 4.1 pKi = 4.1 Binding
In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.In vitro ability to displace [3H]SCH-23390 from bovine cloned Dopamine receptor D1 stably expressed in CHO cells.
ChEMBL 234 5 0 2 3.2 CCCN(CCC)[C@@H]1CCn2cc(C)cc2C1 10.1016/s0960-894x(01)00564-9
145968810 164486 0 None -120 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
CHEMBL4226226 164486 0 None -120 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 381 8 2 4 3.5 CN(C)c1ccc(C(=O)NCCCCN2CCC(c3cccc(O)c3)C2)cc1 10.1016/j.bmcl.2018.03.084
154725813 175952 1 None -31 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4568916 175952 1 None -31 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4597047 175952 1 None -31 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 475 12 1 3 6.4 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
127031404 138273 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 4 2 5 3.2 COc1cc2c(cc1O)C(C)N(Cc1cccc(O)c1OC)CC2 10.1016/j.bmc.2016.03.037
CHEMBL3780975 138273 0 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH2390 from human dopamine D1 receptor by PDSP assay
ChEMBL 329 4 2 5 3.2 COc1cc2c(cc1O)C(C)N(Cc1cccc(O)c1OC)CC2 10.1016/j.bmc.2016.03.037
136043856 79697 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 438 2 1 4 5.6 Fc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(F)c1 10.1016/j.bmcl.2006.06.034
CHEMBL213200 79697 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 438 2 1 4 5.6 Fc1ccc(CN2CCN(C3=Nc4cc(Cl)ccc4Nc4ccccc43)CC2)c(F)c1 10.1016/j.bmcl.2006.06.034
71062708 153772 0 None -47 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
CHEMBL3986651 153772 0 None -47 12 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 368 7 0 5 2.8 COc1cccc(OC[C@@H]2CN(CCN3CCc4ccccc43)CCO2)c1 nan
90644060 111539 0 None -64 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
CHEMBL3289644 111539 0 None -64 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor by PDSP assay
ChEMBL 358 4 0 2 4.4 Fc1ccc2c(c1)CC(CCN1CCN(c3ccc(Cl)cc3)CC1)C2 10.1016/j.bmc.2014.04.026
103 4089 56 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
2875 4089 56 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
5736 4089 56 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
CHEMBL285802 4089 56 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
DB09225 4089 56 None -28 53 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1021/jm030480f
1248739 139556 16 None -190 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
CHEMBL380054 139556 16 None -190 6 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 310 3 0 4 2.8 Fc1ccc(N2CCN(Cc3cn4ccccc4n3)CC2)cc1 10.1021/jm060166w
44339984 167234 0 None -186 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
CHEMBL430522 167234 0 None -186 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
ChEMBL 452 5 1 3 4.9 COc1c(C(=O)N[C@H]2CN(Cc3ccccc3)C[C@@H]2C)cc(Br)c2ccccc12 10.1016/s0960-894x(03)00678-4
135524323 193755 0 None -3467 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
CHEMBL552268 193755 0 None -3467 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 382 5 2 6 1.6 COc1ccccc1N1CCN(Cc2cc3c(=O)[nH]c(N(C)C)nc3[nH]2)CC1 10.1016/j.bmc.2009.05.015
45272537 194851 0 None -588 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
CHEMBL563614 194851 0 None -588 4 Bovine 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 365 4 0 6 3.0 COc1ccccc1N1CCN(Cc2c(C)nc3cc(C)nc(C)n23)CC1 10.1016/j.bmc.2009.05.015
135398745 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
47 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
CHEMBL715 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
DB00334 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenateBinding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm9706832
44415804 81063 0 None 147 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL215997 81063 0 None 147 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
135398745 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
47 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
CHEMBL715 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
DB00334 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
135398745 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
47 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
CHEMBL715 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
DB00334 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligandIn vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm0309811
135398745 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
47 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
CHEMBL715 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
DB00334 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Inhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptorInhibition of [3H]-SCH- 23390 binding to rat dopamine D1 receptor
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm049629t
135398745 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
47 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
CHEMBL715 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
DB00334 2869 108 None -23 65 Rat 7.1 pKi = 7.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1021/jm010982y
15627811 193263 1 None -8 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL54183 193263 1 None -8 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 283 0 3 4 2.6 CN1CCc2cc(O)cc3c2[C@@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
44405980 71712 0 None -23 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
CHEMBL197656 71712 0 None -23 3 Human 5.1 pKi = 5.1 Binding
Binding affinity to dopamine D1 receptorBinding affinity to dopamine D1 receptor
ChEMBL 479 6 2 6 3.2 COc1ccccc1-c1cc2c(=O)n(CCN3CCN(c4ccccc4Cl)CC3)c(=O)[nH]c2[nH]1 10.1016/j.bmcl.2005.09.027
1588 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2294 24 None -190 43 Human 7.1 pKi = 7.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
44415606 79706 0 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
CHEMBL213239 79706 0 None 16 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 475 3 1 6 4.5 COc1cccc(C(=O)NN2c3ccccc3N=C(N3CCN(C)CC3)c3cc(Cl)ccc32)c1 10.1016/j.bmcl.2006.06.034
44415823 140925 0 None 331 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccncc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL384248 140925 0 None 331 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 446 2 1 6 3.9 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccncc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.034
44415473 79512 0 None 22 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 437 1 1 5 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212486 79512 0 None 22 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 437 1 1 5 3.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(F)(F)F)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
118709177 112926 0 None -16 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318850 112926 0 None -16 4 Pig 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1135 31 0 14 12.5 O=C(CCc1cn(CCCCCCCCCCn2cc(CCC(=O)OC3(c4ccc(Cl)cc4)CCN(CCCC(=O)c4ccc(F)cc4)CC3)nn2)nn1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
86764213 131928 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 1 5 4.2 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697590 131928 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 1 5 4.2 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
15711850 13128 0 None -1 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL1191350 13128 0 None -1 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
CHEMBL542436 13128 0 None -1 5 Rat 7.1 pKi = 7.1 Binding
Binding affinity for dopamine receptor D1Binding affinity for dopamine receptor D1
ChEMBL 275 2 2 3 3.2 Cc1ccc2c(c1O)C[C@@H](C1CCCCC1)O[C@H]2CN 10.1021/jm00114a002
117949627 114658 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 287 1 1 4 3.1 COc1cc2c(cc1O)[C@@H]1Cc3sccc3CN1CC2 10.1016/j.bmc.2014.09.024
CHEMBL3344356 114658 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysisDisplacement of [3H]SCH23390 from D1 receptor (unknown origin) transfected in HEK293T cells after 50 mins by liquid scintillation counting analysis
ChEMBL 287 1 1 4 3.1 COc1cc2c(cc1O)[C@@H]1Cc3sccc3CN1CC2 10.1016/j.bmc.2014.09.024
44436621 90600 0 None -151 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
CHEMBL239733 90600 0 None -151 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 443 8 1 3 4.7 C#Cc1cccc(C(=O)NCCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c1 10.1016/j.bmc.2007.08.038
71456045 83659 0 None -1202 6 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
CHEMBL2207635 83659 0 None -1202 6 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes after 60 mins by scintillation counting analysis
ChEMBL 362 5 1 4 3.6 COc1ccccc1N1CCN(Cc2cc(CO)c3cccccc2-3)CC1 10.1016/j.bmcl.2012.09.064
127046952 139571 0 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800636 139571 0 None -70 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 421 12 3 5 4.5 COc1cc(CCNCCc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
25093832 155339 0 None -2290 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155339 0 None -2290 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137640391 156164 0 None -1096 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4070091 156164 0 None -1096 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 418 7 1 7 2.8 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
137635364 155719 0 None -2754 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4064974 155719 0 None -2754 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
CHEMBL4074669 155719 0 None -2754 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranesDisplacement of [3H]SCH23990 from human D1 receptor expressed in HEK293T cell membranes
ChEMBL 439 10 1 6 3.0 O=C(NCCCCN1CCN(c2ccccc2OCCF)CC1)c1cc2ccccn2n1 10.1016/j.bmc.2017.04.036
10314824 35153 1 None -8511 5 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
CHEMBL143761 35153 1 None -8511 5 Bovine 5.1 pKi = 5.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm0009989
10314824 35153 1 None -8511 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
CHEMBL143761 35153 1 None -8511 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 334 3 1 3 3.5 N#Cc1ccc2[nH]c(CN3CCN(c4ccc(F)cc4)CC3)cc2c1 10.1021/jm060166w
44448060 154705 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
CHEMBL402735 154705 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 10.1021/jm060959i
137657153 159010 0 None -776 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4102616 159010 0 None -776 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
85658088 164451 0 None -2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
CHEMBL4225830 164451 0 None -2 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cell membranes by radioligand binding assay
ChEMBL 219 4 1 2 3.0 CCCCN1CCC(c2cccc(O)c2)C1 10.1016/j.bmcl.2018.03.084
1043 1552 13 None -9549 28 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1552 13 None -9549 28 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1552 13 None -9549 28 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1552 13 None -9549 28 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1552 13 None -9549 28 Human 6.1 pKi = 6.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
135986088 177541 0 None -263 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
CHEMBL464811 177541 0 None -263 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 543 7 1 6 6.5 Clc1ccc2c(c1)N=C(N1CCN(Cc3ccc(OCCCN4CCCCC4)cc3)CC1)c1ccccc1N2 10.1016/j.bmcl.2008.09.012
76321554 105922 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3115574 105922 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
CHEMBL3139450 105922 0 None -5370 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 2 hrs by scintillation counting analysis
ChEMBL 395 4 2 3 3.5 Oc1ccc2c(c1)O[C@@H](CNCc1ccc(I)cc1)CC2 10.1021/jm401384w
112500029 131944 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 0 6 3.9 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)ncc(=O)n1C nan
CHEMBL3697606 131944 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 373 5 0 6 3.9 Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)ncc(=O)n1C nan
14198596 101173 0 None 2 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
CHEMBL299056 101173 0 None 2 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2C(c2ccccc2)C1 10.1021/jm00051a008
14198597 101654 1 None 3 2 Human 7.1 pKi = 7.1 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00129a006
CHEMBL302393 101654 1 None 3 2 Human 7.1 pKi = 7.1 Binding
Binding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligandBinding potency of compound for Dopamine receptor D1 by displacing [3H]SCH-23390 radioligand
ChEMBL 273 1 1 2 3.6 CN1Cc2cc(Cl)c(O)cc2[C@H](c2ccccc2)C1 10.1021/jm00129a006
117772840 131914 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 343 3 1 5 2.9 Cc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
CHEMBL3697577 131914 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 343 3 1 5 2.9 Cc1c(-c2ccc(Oc3ncccc3Cl)cc2)n(C)c(=O)[nH]c1=O nan
44320129 167331 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
CHEMBL431220 167331 0 None -1 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1 10.1021/jm00112a034
16105548 82286 0 None -2344 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL217964 82286 0 None -2344 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
CHEMBL221652 82286 0 None -2344 5 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from porcine dopamine D1 in porcine striatal membrane
ChEMBL 462 9 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cccc(F)n3)cc2)CC1 10.1021/jm0611152
53363200 63522 0 None -134 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
CHEMBL1803052 63522 0 None -134 4 Pig 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 509 14 0 9 3.7 CCOCCn1cc(CCCOc2ccc(CN3CCN(c4ccccc4OC)CC3)cc2OC)nn1 10.1021/jm2004859
11682812 77835 0 None -5495 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
CHEMBL210551 77835 0 None -5495 4 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
ChEMBL 402 5 0 7 3.2 COc1ccccc1N1CCN(Cc2cn3cc(C)cc(-n4cccn4)c3n2)CC1 10.1021/jm060166w
2 3210 19 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
54562 3210 19 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
CHEMBL240773 3210 19 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2016.04.028
2 3210 19 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
54562 3210 19 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
CHEMBL240773 3210 19 None -977 28 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm501889t
44380716 58778 0 None -12 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
CHEMBL169631 58778 0 None -12 4 Bovine 4.1 pKi = 4.1 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 429 7 1 4 3.6 COc1cc(N(C)C(C)=O)c(Cl)cc1C(=O)NC[C@H]1CCN(Cc2ccccc2)C1 10.1016/s0960-894x(99)00086-4
2 3210 19 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
54562 3210 19 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
CHEMBL240773 3210 19 None -16595 28 Pig 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm400520c
2 3210 19 None -977 28 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
54562 3210 19 None -977 28 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
CHEMBL240773 3210 19 None -977 28 Human 4.1 pKi = 4.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm5004039
44582179 180843 0 None -57 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 379 6 0 5 2.5 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476393 180843 0 None -57 3 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 379 6 0 5 2.5 O=C1c2ccccc2CCCN1CCCCN1CCN(c2ncccn2)CC1 10.1016/j.bmcl.2009.01.067
154706431 176011 1 None -77 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4531363 176011 1 None -77 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597531 176011 1 None -77 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 451 12 2 3 5.3 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
1220 186 46 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
31 186 46 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
7 186 46 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
CHEMBL56 186 46 None -69183 44 Bovine 4.1 pKi = 4.1 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm950759z
44591012 175007 0 None -177 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
CHEMBL457957 175007 0 None -177 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 10.1016/j.bmcl.2008.09.012
44386883 60081 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 328 3 1 4 3.2 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CNCC2 10.1016/s0960-894x(98)00138-3
CHEMBL174949 60081 0 None -1 2 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 328 3 1 4 3.2 COc1cc2c3c(c1OC)N(c1ccc(F)cc1)CC3CNCC2 10.1016/s0960-894x(98)00138-3
44415845 79603 0 None 34 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 511 3 1 7 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3-n3ccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212844 79603 0 None 34 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 511 3 1 7 4.6 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccccc3-n3ccnc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
11515697 177657 0 None -11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL458397 177657 0 None -11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL465054 177657 0 None -11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 343 1 2 3 4.5 CN1CCc2cc(-c3ccccc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
86767093 128901 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
CHEMBL3671280 128901 0 None - 1 Human 7.1 pKi = 7.1 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 330 3 1 4 4.7 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1c(C)cnnc1C nan
10574176 9868 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 420 5 1 3 5.3 CN(C)c1ccc(CCN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
CHEMBL114726 9868 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membraneAffinity for Dopamine receptor D1 binding measured by competition against [3H]-SCH- 23390 to rat striatal membrane
ChEMBL 420 5 1 3 5.3 CN(C)c1ccc(CCN2CCc3cc(Cl)c(O)cc3C(c3ccccc3)C2)cc1 10.1021/jm960143p
44320026 204379 0 None 3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
CHEMBL85689 204379 0 None 3 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1Binding affinity using [125 I] SCH 23982 radioligand competitive binding assay on dopamine receptor D1
ChEMBL 305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O 10.1021/jm00112a034
117774323 131898 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.9 Cc1cc(Oc2ncc(Cl)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697561 131898 0 None - 1 Human 7.1 pKi = 7.1 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 3 1 5 3.9 Cc1cc(Oc2ncc(Cl)cc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
10643780 118890 0 None -97 4 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
CHEMBL344602 118890 0 None -97 4 Bovine 6.1 pKi = 6.1 Binding
Binding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligandBinding affinity against Dopamine receptor D1 from bovine striatal membranes using [3H]SCH-23390 as radioligand
ChEMBL 384 3 1 3 4.7 N#Cc1ccc2cc(CN3CCN(c4ccc(Cl)c(Cl)c4)CC3)[nH]c2c1 10.1021/jm0009989
10276451 198601 33 None -12022 10 Human 5.1 pKi = 5.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL2112910 198601 33 None -12022 10 Human 5.1 pKi = 5.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
CHEMBL59725 198601 33 None -12022 10 Human 5.1 pKi = 5.1 Binding
Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.Binding affinity for porcine Dopamine receptor D1 by [3H]-SCH- 23390 displacement.
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1021/jm025558r
10276451 198601 33 None -32359 10 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL2112910 198601 33 None -32359 10 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
CHEMBL59725 198601 33 None -32359 10 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390Binding affinity towards D1 receptor from porcine striatal membranes using [3H]-SCH- 23390
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2004.05.052
10276451 198601 33 None -32359 10 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL2112910 198601 33 None -32359 10 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
CHEMBL59725 198601 33 None -32359 10 Pig 5.1 pKi = 5.1 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 461 7 1 4 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2005.07.037
137632607 155798 0 None -2344 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
CHEMBL4065797 155798 0 None -2344 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranesDisplacement of [3H]SCH23390 from human D1R expressed in HEK293T cell membranes
ChEMBL 305 3 2 5 1.6 CCCN1CCCN(c2ccc(O)c3c2OCC(=O)N3)CC1 10.1016/j.bmc.2017.08.037
44278298 98707 0 None -2884 3 Rat 4.1 pKi = 4.1 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 348 4 0 2 4.3 O=C(c1cccc(CN2CCC(c3ccccc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
CHEMBL281214 98707 0 None -2884 3 Rat 4.1 pKi = 4.1 Binding
In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390In vitro binding affinity against Dopamine receptor D1 of rat striatum using [3H]SCH-23390
ChEMBL 348 4 0 2 4.3 O=C(c1cccc(CN2CCC(c3ccccc3)C2)c1)N1CCCCC1 10.1016/s0960-894x(99)00201-2
44304652 198638 0 None -28 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL59749 198638 0 None -28 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 363 7 1 4 4.4 c1ccc(CN2CC[C@@H](CNCc3csc(-c4ccccc4)n3)C2)cc1 10.1016/s0960-894x(00)00405-4
44415622 138074 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 591 4 1 5 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc(F)cc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
CHEMBL377564 138074 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 591 4 1 5 7.0 O=C(NN1c2ccc(Cl)cc2N=C(N2CCN(Cc3ccc(F)cc3F)CC2)c2ccccc21)c1ccccc1Cl 10.1016/j.bmcl.2006.06.034
228 441 26 None -30 24 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
33 441 26 None -30 24 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
6005 441 26 None -30 24 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
CHEMBL53 441 26 None -30 24 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
DB00714 441 26 None -30 24 Rat 6.1 pKi = 6.1 Binding
In vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenateIn vitro binding affinity towards Dopamine receptor D1 by displacing [125I]FISCH radioligand in rat striatal homogenate
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1021/jm00127a005
180 397 50 None -109 38 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
200 397 50 None -109 38 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
2160 397 50 None -109 38 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL629 397 50 None -109 38 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
DB00321 397 50 None -109 38 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1016/j.bmcl.2008.09.012
135398737 944 89 None -44 91 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
38 944 89 None -44 91 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
722 944 89 None -44 91 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
CHEMBL42 944 89 None -44 91 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
DB00363 944 89 None -44 91 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1016/j.bmcl.2008.09.012
44276652 99034 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
CHEMBL283247 99034 0 None 2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cellsBinding affinity to Dopamine receptor D1 by using radioligand [125I]SCH-23982 in HEK cells
ChEMBL 324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2 10.1016/s0960-894x(99)00214-0
127045855 139134 0 None -9 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139134 0 None -9 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
44381276 58420 0 None -2 4 Bovine 5.1 pKi = 5.1 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL168541 58420 0 None -2 4 Bovine 5.1 pKi = 5.1 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 348 4 1 4 2.1 O=C1C[C@@H](CN2CCN(c3ccccc3)CC2)N=C(c2ccccc2)N1 10.1016/s0960-894x(03)00004-0
44304644 201560 0 None -8 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
CHEMBL64566 201560 0 None -8 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 454 8 2 4 4.5 COc1ccc(Br)cc1-c1nc(CNC[C@@H]2CCN(Cc3ccccc3)C2)c[nH]1 10.1016/s0960-894x(00)00405-4
154703922 175715 1 None -446 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4590211 175715 1 None -446 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595146 175715 1 None -446 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
154703824 176052 1 None -346 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4456007 176052 1 None -346 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597876 176052 1 None -346 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
181743 177997 3 None -446 22 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH233930 from human dopamine D1 receptorDisplacement of [3H]SCH233930 from human dopamine D1 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 177997 3 None -446 22 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH233930 from human dopamine D1 receptorDisplacement of [3H]SCH233930 from human dopamine D1 receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
242 467 117 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
34 467 117 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
60795 467 117 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
CHEMBL1112 467 117 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
DB01238 467 117 None -281 51 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.Radioligand Binding Assay: Membranes prepared as above were resuspended to 1 ug protein/ul (measured by Bradford assay using BSA as standard), and 50 ul were added to each well of a polypropylene 96-well plate containing (per well): 50 ul of buffer (20 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 100 mM N-methyl-D-gluconate, pH 7.4), 50 ul of 1.5 nM [3H]N-methylspiperone (final concentration 0.3 nM) and reference or D2 test ligand at various concentrations ranging from 50 uM to 50 uM (final concentrations ranging from 10 uM to 10 uM, triplicate determinations for each concentration of D2 test ligand). After a 1.5-hr incubation in the dark at room temperature, the reactions were harvested onto 0.3% PEI-soaked Filtermax GF/A filters (Wallac) and washed three times with ice-cold 50 mM Tris, pH 7.4 using a Perkin-Elmer Filtermate 96-well harvester. The filters were subsequently dried, placed on a hot plate (100° C.), and Melitilex-A (Wallac) scintillant was applied.
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl nan
44304621 201728 0 None -74 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
CHEMBL65641 201728 0 None -74 4 Bovine 5.1 pKi = 5.1 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 469 9 1 5 5.1 COc1ccc(Br)cc1-c1nc(CNCC[C@@H]2CCN(Cc3ccccc3)C2)co1 10.1016/s0960-894x(00)00405-4
6101909 100469 1 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
CHEMBL294012 100469 1 None 1 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00170a025
6101909 100469 1 None -1 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
CHEMBL294012 100469 1 None -1 3 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1
ChEMBL 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2[C@H]2c3ccccc3CC[C@H]21 10.1021/jm00128a038
44455426 154610 0 None -12 12 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 154610 0 None -12 12 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned dopamine D1 receptor by competitive binding experimentInhibition of human cloned dopamine D1 receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44415629 79620 0 None 338 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccsc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL212896 79620 0 None 338 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 451 2 1 6 4.5 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3ccsc3)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
10107367 101961 1 None -7 4 Rat 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
CHEMBL303993 101961 1 None -7 4 Rat 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 273 1 1 2 3.6 CN1CCc2cc(Cl)c(O)cc2[C@@H]1c1ccccc1 10.1021/jm00051a008
44385980 61055 0 None 3 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 268 1 1 2 3.2 Fc1ccc(N2CC3CNCCc4cccc2c43)cc1 10.1016/s0960-894x(98)00138-3
CHEMBL176990 61055 0 None 3 2 Rat 8.0 pKi = 8.0 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
ChEMBL 268 1 1 2 3.2 Fc1ccc(N2CC3CNCCc4cccc2c43)cc1 10.1016/s0960-894x(98)00138-3
11558247 75071 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
CHEMBL204098 75071 0 None 2 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 282 0 2 3 2.6 CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 10.1021/jm051237e
86764211 131924 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697587 131924 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 357 3 1 5 3.2 Cc1cc(Oc2ncccc2Cl)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
11573806 75066 0 None -7 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
CHEMBL204065 75066 0 None -7 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH 23390 from D1 dopamine receptorDisplacement of [3H]SCH 23390 from D1 dopamine receptor
ChEMBL 311 2 0 3 3.3 COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 10.1021/jm051237e
2865 4079 67 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
59 4079 67 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
60854 4079 67 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
CHEMBL708 4079 67 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
DB00246 4079 67 None -114 53 Human 8.0 pKi = 8.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1021/jm0002432
1353 1880 85 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
3559 1880 85 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
86 1880 85 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
CHEMBL54 1880 85 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
DB00502 1880 85 None -30 85 Pig 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/j.bmcl.2014.06.079
10830233 201165 0 None 8 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 329 0 2 1 4.3 CN1CCc2c([nH]c3ccccc23)Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
CHEMBL62529 201165 0 None 8 2 Rat 8.0 pKi = 8.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 329 0 2 1 4.3 CN1CCc2c([nH]c3ccccc23)Cc2[nH]c3ccccc3c2CC1 10.1021/jm9911478
117774170 131913 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 385 3 1 4 4.3 Cc1cc(Oc2ncccc2Br)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697576 131913 0 None - 1 Human 8.0 pKi = 8.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 385 3 1 4 4.3 Cc1cc(Oc2ncccc2Br)ccc1-c1c(C)n[nH]c(=O)c1C nan
134137323 142435 0 None 33 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 4 2 5 4.7 CCC(C)Oc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
CHEMBL3894329 142435 0 None 33 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting methodDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEKT cell membranes after 90 mins by microbeta scintillation counting method
ChEMBL 447 4 2 5 4.7 CCC(C)Oc1c(O)cc(Br)c2c1CN1CCc3cc(OC)c(O)cc3[C@@H]1C2 10.1016/j.ejmech.2016.09.036
74223724 128895 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3671274 128895 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 2 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)n[nH]c(=O)c1C nan
74223777 128913 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 350 3 1 4 5.1 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1Cl nan
CHEMBL3671291 128913 0 None - 1 Human 8.0 pKi = 8.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 350 3 1 4 5.1 Cc1ncnc(C)c1-c1ccc(Oc2nccc3[nH]ccc23)cc1Cl nan
44393403 64747 0 None -891 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
CHEMBL182379 64747 0 None -891 6 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 533 8 1 5 4.4 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3cc(I)ccc3o2)CC1 10.1021/jm900095y
137655735 158446 0 None -1230 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4096353 158446 0 None -1230 5 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 436 8 2 8 2.7 COc1ccccc1N1CCN(CCCC(=O)Nc2ccn3ncc(/C=N\O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
52943802 17436 0 None -199 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
CHEMBL1258270 17436 0 None -199 5 Pig 5.1 pKi = 5.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 363 6 0 2 5.8 Cc1ccc(C)c(C(=O)CCCN2CCC(c3cc(C)ccc3C)CC2)c1 10.1021/jm100899z
44319368 105584 0 None -7 4 Bovine 5.1 pKi = 5.1 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
CHEMBL313320 105584 0 None -7 4 Bovine 5.1 pKi = 5.1 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 429 5 0 5 3.4 COc1ccc(Br)cc1C1=N[C@@H](CN2CCN(c3ccccc3)CC2)CO1 10.1016/s0960-894x(01)00484-x
10807793 201290 0 None 7 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 350 2 1 3 3.8 COc1cc2c(cc1OC)Cc1[nH]c3ccccc3c1CCN(C)CC2 10.1021/jm9911478
CHEMBL63063 201290 0 None 7 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390Binding affinity against Dopamine receptor D1 of rat striatal receptor using [3H]SCH-23390
ChEMBL 350 2 1 3 3.8 COc1cc2c(cc1OC)Cc1[nH]c3ccccc3c1CCN(C)CC2 10.1021/jm9911478
164627027 185845 0 None -45 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
CHEMBL4876260 185845 0 None -45 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)Displacement of [3H]SCH23390 from dopamine D1 receptor (unknown origin)
ChEMBL 466 5 3 4 4.3 O=C(NCc1ccccc1CN1CCc2cc(O)c(O)cc2C1)c1cccc(Br)c1 10.1016/j.bmcl.2021.128047
44403224 71571 0 None -102 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
CHEMBL197195 71571 0 None -102 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 424 7 1 4 3.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cccc(F)n1 10.1016/j.bmcl.2005.07.037
44436605 148531 0 None -2951 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 148531 0 None -2951 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranesDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in porcine striatal membranes
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
53318564 58287 0 None -8 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 646 14 0 7 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCN(CCCN2CCN(c4ccccc4OC)CC2)S(C)(=O)=O)c1-3 10.1016/j.bmc.2011.01.053
CHEMBL1684129 58287 0 None -8 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counterDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in human HEK293 cells by liquid scintillation counter
ChEMBL 646 14 0 7 5.5 CCCN1CCc2cccc3c2C1Cc1cccc(OCCCN(CCCN2CCN(c4ccccc4OC)CC2)S(C)(=O)=O)c1-3 10.1016/j.bmc.2011.01.053
57390119 68961 0 None -218 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
CHEMBL1928127 68961 0 None -218 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from pig D1 receptor in striatal membraneDisplacement of [3H]SCH23390 from pig D1 receptor in striatal membrane
ChEMBL 969 33 2 14 5.4 COc1ccccc1N1CCN(CCCNC(=O)c2ccc(COCCOCCOCCOCCOCCOCc3ccc(C(=O)NCCCN4CCN(c5ccccc5OC)CC4)cc3)cc2)CC1 10.1016/j.bmc.2011.10.063
44381286 119861 0 None -4 4 Bovine 5.0 pKi = 5.0 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
CHEMBL353220 119861 0 None -4 4 Bovine 5.0 pKi = 5.0 Binding
In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390In vitro Binding affinity towards dopamine D1 receptor using bovine striatal membrane preparations and antagonist [3H]-SCH- 23390
ChEMBL 442 5 1 5 3.4 COc1ccc(Br)cc1C1=NCC[C@@H](CN2CCN(c3ccccc3)CC2)N1 10.1016/s0960-894x(03)00004-0
118711263 113459 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1ccccc1-c1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
CHEMBL3325914 113459 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cell membranes by liquid scintillation counting based competition binding assay
ChEMBL 343 2 1 2 5.0 Cc1ccccc1-c1cc2c(cc1O)C(c1ccccc1)CN(C)CC2 10.1016/j.ejmech.2014.07.059
10432606 202809 0 None -11 2 Rat 6.0 pKi = 6.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 426 7 0 4 4.0 O=C(CCCN1CCN(CC2CC(=O)c3ccc(F)cc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
CHEMBL72649 202809 0 None -11 2 Rat 6.0 pKi = 6.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the dopamine receptor D1
ChEMBL 426 7 0 4 4.0 O=C(CCCN1CCN(CC2CC(=O)c3ccc(F)cc3C2)CC1)c1ccc(F)cc1 10.1021/jm00111a046
10402195 41285 1 None 1 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3Oc3ccccc32)CC1 10.1021/jm00030a011
CHEMBL149108 41285 1 None 1 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
ChEMBL 294 0 0 5 2.5 CN1CCN(C2=Nc3cccnc3Oc3ccccc32)CC1 10.1021/jm00030a011
6603798 99717 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL1613539 99717 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
CHEMBL288096 99717 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligandBinding affinity at rat striatal Dopamine receptor D1 using [3H]- SCH-23390 radioligand
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm00168a040
117773861 131894 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2ncc(Cl)cc2C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
CHEMBL3697557 131894 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 371 3 1 5 3.5 Cc1cc(Oc2ncc(Cl)cc2C)ccc1-c1c(C)c(=O)[nH]c(=O)n1C nan
44403213 71443 4 None -1737 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
CHEMBL196744 71443 4 None -1737 5 Pig 6.0 pKi = 6.0 Binding
Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand Binding affinity towards Dopamine receptor D1 using porcine striatal membrane and [3H]-SCH- 23390 as radioligand
ChEMBL 423 7 1 3 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(F)cc1 10.1016/j.bmcl.2005.07.037
54581964 61279 0 None -3162 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771111 61279 0 None -3162 5 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH-23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 489 8 0 5 5.4 COc1ccccc1N1CCN(CCCCN2CCCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
6603798 99717 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL1613539 99717 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
CHEMBL288096 99717 5 None -17378 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 311 2 3 4 3.3 CCCN1CCc2cc(O)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1021/jm060959i
137659303 158757 0 None -154 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 158757 0 None -154 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysisDisplacement of [3H]SCH23390 from human Dopamine D1 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
118709163 112910 0 None -338 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318835 112910 0 None -338 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 888 21 0 8 11.3 O=C(CCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
12050196 201428 5 None -15 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
CHEMBL64043 201428 5 None -15 4 Bovine 5.0 pKi = 5.0 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
ChEMBL 349 5 0 4 4.1 c1ccc(CN2CCN(Cc3csc(-c4ccccc4)n3)CC2)cc1 10.1016/s0960-894x(00)00405-4
71462090 84170 0 None -831 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
CHEMBL2158640 84170 0 None -831 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
CHEMBL2221044 84170 0 None -831 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation countingDisplacement of [3H]-SCH-23390 from human dopamine D1 receptor expressed in HEK293 cells after 30 mins by scintillation counting
ChEMBL 353 3 3 4 4.1 CCCN1C[C@H](c2ccc(O)cc2)C[C@@H]2c3cc(O)c(O)cc3CC[C@H]21 10.1016/j.bmc.2012.08.058
24949535 180977 0 None -1122 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
CHEMBL476722 180977 0 None -1122 3 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatumDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat brain striatum
ChEMBL 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 10.1021/jm800176x
177511 101072 20 None -14 2 Rat 5.0 pKi = 5.0 Binding
The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)C(Cc1ccccc1)NCC2 10.1016/s0960-894x(00)00326-7
CHEMBL298285 101072 20 None -14 2 Rat 5.0 pKi = 5.0 Binding
The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.The compound has been evaluated for its binding affinity towards Dopamine receptor D1 by displacing the radioligand [3H]SCH-23390 (1.5 nM) in rat striatal synaptosomes.
ChEMBL 255 2 3 3 2.5 Oc1cc2c(cc1O)C(Cc1ccccc1)NCC2 10.1016/s0960-894x(00)00326-7
156013773 176699 0 None -9 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 280 1 0 3 3.3 CN1CCc2cccc3c2C1Cc1ccc([N+](=O)[O-])cc1-3 10.1016/j.bmcl.2020.127053
CHEMBL4636242 176699 0 None -9 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human D1 receptorBinding affinity to human D1 receptor
ChEMBL 280 1 0 3 3.3 CN1CCc2cccc3c2C1Cc1ccc([N+](=O)[O-])cc1-3 10.1016/j.bmcl.2020.127053
1353 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
3559 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
86 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
CHEMBL54 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
DB00502 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membraneDisplacement of [3H]SCH 23390 from pig dopamine D1 receptor in striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2009919
1353 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
3559 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
86 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
CHEMBL54 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
DB00502 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm2004859
74223773 128902 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)nc[n+]([O-])c1C nan
CHEMBL3671281 128902 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 347 3 1 5 3.4 Cc1cc(Oc2nccc3n[nH]cc23)ccc1-c1c(C)nc[n+]([O-])c1C nan
154725276 175716 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4456964 175716 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595147 175716 1 None -34 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 478 12 1 3 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(Cl)ccc1OC 10.1021/acs.jmedchem.9b01835
25071692 111297 0 None -2187 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111297 0 None -2187 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
118709169 112917 0 None -6 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
CHEMBL3318841 112917 0 None -6 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assayDisplacement of [3H]SCH23390 from porcine striatal membranes D1 receptor by competitive binding assay
ChEMBL 1029 31 0 8 15.2 O=C(CCCCCCCCCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2014.06.079
44372009 48575 0 None -123 4 Bovine 6.0 pKi = 6.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
CHEMBL155913 48575 0 None -123 4 Bovine 6.0 pKi = 6.0 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 402 4 0 4 5.0 Clc1ccc(N2CCN(Cc3cnn4c(-c5ccccc5)cccc34)CC2)cc1 10.1016/s0960-894x(01)00814-9
42626103 55960 0 None -2137 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
CHEMBL1627323 55960 0 None -2137 4 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 442 6 2 3 4.6 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1021/jm900095y
44241577 13900 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL1197140 13900 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
CHEMBL560721 13900 0 None -46 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting
ChEMBL 387 3 3 4 5.0 CCCN1CCc2cc(-c3ccc(O)cc3)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2009.04.047
117773063 131921 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 4 1 5 4.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
CHEMBL3697584 131921 0 None - 1 Human 7.0 pKi = 7.0 Binding
Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.Competition Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor.D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium.
ChEMBL 391 4 1 5 4.4 Cc1cc(Oc2ncccc2OC(F)(F)F)ccc1-c1c(C)n[nH]c(=O)c1C nan
154725001 176073 1 None -60 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4525624 176073 1 None -60 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598002 176073 1 None -60 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 2 6.5 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
44344506 13716 0 None -8 2 Rat 5.0 pKi = 5.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 327 1 1 2 4.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(-c2ccccc2)c(O)c1-3 10.1021/jm960188q
CHEMBL119577 13716 0 None -8 2 Rat 5.0 pKi = 5.0 Binding
In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.In vitro affinity at Dopamine receptor D1 of rat striatum by [3H]SCH-23390 displacement.
ChEMBL 327 1 1 2 4.8 CN1CCc2cccc3c2[C@H]1Cc1ccc(-c2ccccc2)c(O)c1-3 10.1021/jm960188q
25139479 183735 0 None -1071 4 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 183735 0 None -1071 4 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from D1 receptor in pig striatal membraneDisplacement of [3H]SCH23390 from D1 receptor in pig striatal membrane
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
45483655 196438 0 None -138 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
CHEMBL574534 196438 0 None -138 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 1047 23 2 14 8.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(-c3cn(Cc4ccc(-c5ccc(Cn6cc(-c7ccc(C(=O)NCCCCN8CCN(c9ccccc9OC)CC8)cc7)nn6)cc5)cc4)nn3)cc2)CC1 10.1021/jm901120h
71110301 91766 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
CHEMBL2425371 91766 0 None -13 2 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysisDisplacement of [3H]-SCH 23390 from dopamine D1 receptor in rat striatal membranes after 1 hr by liquid scintillation counting analysis
ChEMBL 297 1 2 4 2.8 COc1ccc2c(c1)CC1c3cc(O)c(O)cc3CCN1C2 10.1016/j.ejmech.2013.07.036
2726 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
621 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
83 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
CHEMBL71 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
DB00477 906 64 None -36 72 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1016/j.bmcl.2008.09.012
127047859 139521 0 None -338 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3800341 139521 0 None -338 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cellsDisplacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells
ChEMBL 476 12 3 6 4.1 COc1cc(CCNCCc2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
45481877 196452 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 10 2 10 3.6 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5ncccn5)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
CHEMBL574627 196452 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]SCH23390 from dopamine D1 receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 582 10 2 10 3.6 Cc1cccc(C2CN(CCCc3cn(CCCN4CCN(c5ncccn5)CC4)nn3)CCc3cc(O)c(O)cc32)c1 10.1016/j.bmc.2009.06.019
3082625 193060 6 None -199 4 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2007.05.057
CHEMBL53510 193060 6 None -199 4 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
ChEMBL 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3 10.1016/j.bmcl.2007.05.057
154705128 175717 1 None -67 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4454872 175717 1 None -67 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4595148 175717 1 None -67 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 462 12 1 3 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
100 3745 52 None -47 55 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
2637 3745 52 None -47 55 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
5452 3745 52 None -47 55 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
CHEMBL479 3745 52 None -47 55 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
DB00679 3745 52 None -47 55 Human 7.0 pKi = 7.0 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 nan
86767094 128904 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cncc2nccn12 nan
CHEMBL3671283 128904 0 None - 1 Human 7.0 pKi = 7.0 Binding
Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.Receptor Binding Assay: The affinity of the compounds described herein was determined by competition binding assays similar to those described in Ryman-Rasmussen et al., Differential activation of adenylate cyclase and receptor internalization by novel dopamine D1 receptor agonists, Molecular Pharmacology 68(4):1039-1048 (2005). This radioligand binding assay used [3H]-SCH23390, a radiolabeled D1 ligand, to evaluate the ability of a test compound to compete with the radioligand when binding to a D1 receptor. D1 binding assays were performed using over-expressing LTK human cell lines. To determine basic assay parameters, ligand concentrations were determined from saturation binding studies where the Kd for [3H]-SCH23390 was found to be 1.3 nM. From tissue concentration curve studies, the optimal amount of tissue was determined to be 1.75 mg/mL per 96 well plate using 0.5 nM of [3H]-SCH23390. These ligand and tissue concentrations were used in time course studies to determine linearity and equilibrium condition.
ChEMBL 341 3 1 5 4.4 Cc1cc(Oc2nccc3[nH]ccc23)ccc1-c1cncc2nccn12 nan
1353 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
3559 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
86 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
CHEMBL54 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
DB00502 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1Compound was evaluated for its affinity (pKi) to inhibit [3H]SCH-23390 binding to the Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00111a046
1353 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
3559 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
86 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
CHEMBL54 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
DB00502 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1Inhibition constant for in vitro inhibition of [3H]-SCH- 23390 binding to striatal membranes Dopamine receptor D1
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1016/0960-894X(95)00076-6
1353 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
3559 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
86 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
CHEMBL54 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
DB00502 1880 85 None -74 85 Rat 7.0 pKi = 7.0 Binding
Inhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membraneInhibition of [3H]-SCH- 23390 binding to dopamine receptor D1 rat striatal membrane
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm00042a009
10454026 17725 0 None -3019 9 Rat 6.0 pKi = 6.0 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
CHEMBL125916 17725 0 None -3019 9 Rat 6.0 pKi = 6.0 Binding
Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.Binding affinity for rat striatum Dopamine receptor D1 by [3H]-SCH- -2339 displacement.
ChEMBL 406 8 2 4 3.5 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3[nH]2)CC1 10.1021/jm0211220
10058098 196930 9 None - 1 Rat 6.0 pKi = 6.0 Binding
Compound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligandCompound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligand
ChEMBL 179 0 3 3 0.8 Oc1cc2c(cc1O)CCNCC2 10.1021/jm00160a018
CHEMBL57873 196930 9 None - 1 Rat 6.0 pKi = 6.0 Binding
Compound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligandCompound was tested for binding affinity against dDopamine receptor D1 using [3H]fenoldopam as a radioligand
ChEMBL 179 0 3 3 0.8 Oc1cc2c(cc1O)CCNCC2 10.1021/jm00160a018
11678172 77678 0 None -2137 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 77678 0 None -2137 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH 23390 from D1 receptor of porcine striatal membraneDisplacement of [3H]SCH 23390 from D1 receptor of porcine striatal membrane
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
25071384 111289 0 None -251 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111289 0 None -251 5 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
44381118 57265 0 None -426 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
CHEMBL166587 57265 0 None -426 4 Bovine 5.0 pKi = 5.0 Binding
Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.Binding affinity towards bovine dopamine D1 receptor by [3H]-SCH- 23390 displacement.
ChEMBL 387 7 2 4 3.6 CNc1cc(OC)c(C(=O)NC[C@H]2CCN(Cc3ccccc3)C2)cc1Cl 10.1016/s0960-894x(99)00086-4
44319102 204421 0 None -16 4 Bovine 5.0 pKi = 5.0 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
CHEMBL86060 204421 0 None -16 4 Bovine 5.0 pKi = 5.0 Binding
In vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cellsIn vitro for its ability to displace [3H]- SCH 23390 from Dopamine receptor D1 in bovine striatal membrane expressed in CHO cells
ChEMBL 321 4 0 4 2.7 c1ccc(C2=N[C@@H](CN3CCN(c4ccccc4)CC3)CO2)cc1 10.1016/s0960-894x(01)00484-x
44582187 180988 0 None -47 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 8 0 4 3.7 COc1ccccc1N1CCN(CCCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
CHEMBL476808 180988 0 None -47 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptorDisplacement of [3H]SCH23390 from human dopamine D1 receptor
ChEMBL 407 8 0 4 3.7 COc1ccccc1N1CCN(CCCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2009.01.067
44323870 111102 0 None 3 4 Rat 7.0 pKi = 7.0 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
CHEMBL328246 111102 0 None 3 4 Rat 7.0 pKi = 7.0 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
ChEMBL 364 1 0 2 5.2 CC(C)=C1c2ccc(Cl)cc2C=C(N2CCN(C)CC2)c2ccccc21 10.1021/jm00043a008
25142456 81994 2 None -48 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
CHEMBL217299 81994 2 None -48 9 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned dopamine D1 receptorBinding affinity to human cloned dopamine D1 receptor
ChEMBL 269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2 10.1021/jm0604979
44415685 79757 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 551 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213466 79757 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 551 2 1 5 5.7 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)c3cc(F)c(F)c(F)c3F)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
44415450 139093 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 425 1 1 5 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(C)(C)C)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
CHEMBL379757 139093 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from human dopamine D1 receptor expressed in CHO cells
ChEMBL 425 1 1 5 4.2 CN1CCN(C2=Nc3cc(Cl)ccc3N(NC(=O)C(C)(C)C)c3ccccc32)CC1 10.1016/j.bmcl.2006.06.022
1353 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
3559 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
86 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
CHEMBL54 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
DB00502 1880 85 None -30 85 Pig 7.0 pKi = 7.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1021/jm100899z
118445551 166761 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
CHEMBL4294009 166761 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation countingDisplacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting
ChEMBL 327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1 10.1021/acs.jmedchem.8b01622
53363201 63524 0 None -114 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
CHEMBL1803054 63524 0 None -114 4 Pig 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
ChEMBL 893 27 0 15 7.0 COc1cc(CN2CCN(C)CC2)ccc1OCCCc1cn(CCCCCCCCn2cc(CCCOc3ccc(CN4CCN(c5ccccc5OC)CC4)cc3OC)nn2)nn1 10.1021/jm2004859
71722297 101999 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL2397382 101999 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
CHEMBL3040156 101999 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysisDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis
ChEMBL 297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3 10.1016/j.bmc.2013.05.014
49782601 17306 0 None -602 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
CHEMBL1257810 17306 0 None -602 5 Pig 5.0 pKi = 5.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranesDisplacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes
ChEMBL 487 6 1 3 6.2 O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm100899z
10561522 35972 0 None -51 2 Bovine 4.0 pKi = 4.0 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2c(C)cccc2C)C1 10.1021/jm9708700
CHEMBL144501 35972 0 None -51 2 Bovine 4.0 pKi = 4.0 Binding
Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand
ChEMBL 231 3 0 1 3.9 CCCN1CCCC(c2c(C)cccc2C)C1 10.1021/jm9708700
154705520 175686 1 None -64 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4452683 175686 1 None -64 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4594959 175686 1 None -64 6 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 448 11 1 3 5.6 CCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
2750 202363 69 None -5 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
CHEMBL7002 202363 69 None -5 12 Human 5.0 pKi = 5 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
ChEMBL 333 5 1 4 3.9 CC1(COc2ccc(CC3SC(=O)NC3=O)cc2)CCCCC1 nan
15115519 205478 0 None -151 2 Human 7.0 pKi = 7 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 677 12 1 10 6.4 O=C(CCCN1CCC2(CC1)C(=O)N(CCc1ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc1)CN2c1ccccc1)c1ccc(F)cc1 10.1021/jm00115a012
CHEMBL92649 205478 0 None -151 2 Human 7.0 pKi = 7 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
ChEMBL 677 12 1 10 6.4 O=C(CCCN1CCC2(CC1)C(=O)N(CCc1ccc(Nc3ccc([N+](=O)[O-])c4nonc34)cc1)CN2c1ccccc1)c1ccc(F)cc1 10.1021/jm00115a012
44415605 79705 0 None 11 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
CHEMBL213238 79705 0 None 11 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cellsDisplacement of [3H]SCH 23390 from dopamine D1 receptor expressed in CHO cells
ChEMBL 470 2 1 6 4.3 CN1CCN(C2=Nc3ccccc3N(NC(=O)c3cccc(C#N)c3)c3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2006.06.034
42625205 55961 0 None -89 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
CHEMBL1627324 55961 0 None -89 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]SCH23390 from D1 receptorDisplacement of [3H]SCH23390 from D1 receptor
ChEMBL 405 7 1 5 3.6 COc1ccccc1N1CCN(C/C=C/CNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm900095y
3303 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
5311200 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
CHEMBL267014 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(98)00692-1
3303 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
5311200 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
CHEMBL267014 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
Displacement of [3H]SCH23390 from bovine dopamine D1 receptorDisplacement of [3H]SCH23390 from bovine dopamine D1 receptor
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/j.bmc.2009.05.015
24824066 156838 0 None -2 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
CHEMBL407818 156838 0 None -2 4 Pig 5.0 pKi = 5 Binding
Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membraneDisplacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane
ChEMBL 308 3 1 5 2.4 Oc1ccc(N2CCN(Cc3cnn4ccccc34)CC2)cc1 10.1021/jm701375u
3303 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
5311200 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
CHEMBL267014 2213 41 None -14454 15 Bovine 5.0 pKi = 5 Binding
In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement.
ChEMBL 326 3 1 3 3.5 Clc1ccc(cc1)N1CCN(CC1)Cc1c[nH]c2c1cccn2 10.1016/s0960-894x(01)00814-9
154706703 175658 1 None -17 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4550187 175658 1 None -17 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
CHEMBL4594691 175658 1 None -17 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 432 11 1 2 6.0 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)CC1CC1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01835
154725749 176114 1 None -91 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4453478 176114 1 None -91 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
CHEMBL4598388 176114 1 None -91 5 Human 6.0 pKi = 6 Binding
Displacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-SCH23390 from recombinant human D1 receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 437 11 2 2 5.8 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)CC1CC1c1cccc(Cl)c1 10.1021/acs.jmedchem.9b01835
240 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 931 39 None - 25 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to dopamine receptor D1Binding affinity to dopamine receptor D1
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
3294 1975 106 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 None - 44 Mouse 8.2 pIC50 = 8.2 Binding
Binding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligandBinding affinity against Dopamine receptor D1 was determined using [3H]SCH-23390 radioligand
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2601 3721 30 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3721 30 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3721 30 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3721 30 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3721 30 None - 21 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligandIn vitro binding activity against Dopamine receptor D1 from homogenized rat brain, using [3H]SCH-23390 as the radioligand
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
100 3745 52 None -16 55 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 None -16 55 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 None -16 55 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 None -16 55 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 None -16 55 Rat 8.1 pIC50 = 8.1 Binding
Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1Affinity for displacement of [3H]WB-4101 labeled Dopamine receptor D1
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5281878 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 None -11 16 Rat 8.0 pIC50 = 8.0 Binding
In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligandIn vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1028 287 69 None -91 29 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 None -91 29 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 None -91 29 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 None -91 29 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 None -91 29 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 None -91 29 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
1960 2815 64 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
439260 2815 64 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
505 2815 64 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL1437 2815 64 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
DB00368 2815 64 None -95 26 Human 8.4 pKd = 8.4 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O None
1153 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1598 53 None -32 10 Human 8.1 pKd = 8.1 Binding
Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cellsEquilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2869 4088 85 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60 4088 85 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60857 4088 85 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
CHEMBL1185 4088 85 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
DB00315 4088 85 None -2 7 Rat 8.0 pKd = 8.0 Binding
Binding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligandBinding affinity against dopamine receptor D1 in rat striatum using [3H]SCH-23390 as radioligand
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
5018 3493 8 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
943 3493 8 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
946 3493 8 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
CHEMBL13668 3493 8 None 2 9 Human 9.5 pKd = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 2168520
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 2 27 Mouse 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
None 214634 0 3H-SCH23390 5495 2 Rat 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 329 1 1 3 3.6 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OCC4)O)Cl None
None 214632 0 3H-SCH23390 165 2 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 327 1 1 3 4.4 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OC=C4)O)Cl None
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1242 3556 23 3H-SCH23390 1 17 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 1 17 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 1 17 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1243 3561 26 3H-SCH23390 3 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
944 3561 26 3H-SCH23390 3 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
CHEMBL324017 3561 26 3H-SCH23390 3 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O None
5281878 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281878 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -4 16 Mouse 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -11 16 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
25058166 214181 0 3H-SCH23390 High -6 26 Bovine 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 High -6 26 Bovine 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
3036864 201066 16 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -26 27 Bovine 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -3 27 Rhesus macaque 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
5018 3493 8 3H-SCH23390 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
5018 3493 8 UNDEFINED 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 3493 8 3H-SCH23390 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 3493 8 UNDEFINED 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 3493 8 3H-SCH23390 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 3493 8 UNDEFINED 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 3493 8 3H-SCH23390 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 3493 8 UNDEFINED 2 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
3036864 201066 16 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
37459 735 10 3H-SCH23390 -2 24 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
37459 735 10 3H-SCH23390 -8 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -2 24 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -8 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -2 24 Mouse 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -8 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
133538 3562 17 3H-SCH23390 1 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O None
8443 3562 17 3H-SCH23390 1 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O None
CHEMBL574558 3562 17 3H-SCH23390 1 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O None
3036864 201066 16 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -3 27 Rhesus macaque 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
3036864 201066 16 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -2 27 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
1218 3559 24 3H-SCH23390 11 7 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
938 3559 24 3H-SCH23390 11 7 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
CHEMBL353335 3559 24 3H-SCH23390 11 7 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
None 214636 0 3H-SCH23390 436 2 Mouse 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 349 1 2 3 3.3 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O.Br None
135398745 2869 108 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -23 65 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6603820 95330 13 3H-SCH23390 1 13 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 1 13 Rat 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
1241 99716 19 3H-SCH23390 -1 7 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL288090 99716 19 3H-SCH23390 -1 7 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL552611 99716 19 3H-SCH23390 -1 7 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
135398745 2869 108 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -23 65 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
100 3745 52 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SCH23390 -47 55 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
202 1480 0 UNDEFINED -9 31 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1480 0 UNDEFINED -9 31 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1480 0 UNDEFINED -9 31 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1480 0 UNDEFINED -9 31 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1480 0 UNDEFINED -9 31 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
2 3210 19 3H-SCH23390 -208 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SCH23390 -208 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SCH23390 -208 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
121881 3434 21 3H-SCH23390 -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
256 3434 21 3H-SCH23390 -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
CHEMBL68131 3434 21 3H-SCH23390 -48977 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 382 6 1 6 3.4 CCCCN1CCC(CC1)COC(=O)c1cc(Cl)c(c2c1OCCO2)N None
46222048 8896 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
CHEMBL1098230 8896 0 UNDEFINED -4365 13 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 260 4 1 2 4.0 CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1 None
18922713 98046 0 3H-SCH23390 -12882 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
CHEMBL276031 98046 0 3H-SCH23390 -12882 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
24840389 114714 3 3H-SCH23390 -741 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 114714 3 3H-SCH23390 -741 15 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
44591098 176188 0 UNDEFINED -288 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL460402 176188 0 UNDEFINED -288 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 508 9 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)c1ccc(OCCCN2CCCCC2)cc1 None
12016890 190182 4 3H-SCH23390 -1698 10 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190182 4 3H-SCH23390 -1698 10 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
5656 201377 82 UNDEFINED -25 40 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201377 82 UNDEFINED -25 40 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
54841 201437 51 UNDEFINED -1 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 201437 51 UNDEFINED -1 28 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 214216 0 3H-SCH23390 -107 10 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.2 C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl None
104911 214249 0 3H-SCH23390 -4168 36 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
3075702 215594 0 3H-SCH23390 -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1574 81 52 3H-SCH23390 -107 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 52 3H-SCH23390 -107 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 52 3H-SCH23390 -107 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
5 139 66 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 66 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-SCH23390 Low -23442 54 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-SCH23390 -16595 54 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1192 147 41 3H-dopamine -162 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 147 41 3H-dopamine -162 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 147 41 3H-dopamine -162 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1220 186 46 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 186 46 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 186 46 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 186 46 3H-SCH23390 -7943 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3153 294 24 3H-SCH23390 Low -39 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 294 24 3H-SCH23390 Low -39 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 294 24 3H-SCH23390 Low -39 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
179 396 107 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
179 396 107 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 396 107 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 396 107 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 396 107 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-SCH23390 -4365 50 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 396 107 3H-SCH23390 -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2554 784 115 3H-SCH23390 -48 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
489 784 115 3H-SCH23390 -48 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
5339 784 115 3H-SCH23390 -48 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
CHEMBL108 784 115 3H-SCH23390 -48 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
DB00564 784 115 3H-SCH23390 -48 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 236 0 1 1 3.4 NC(=O)N1c2ccccc2C=Cc2c1cccc2 None
2147 1374 16 3H-SCH23390 -53 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
5826 1374 16 3H-SCH23390 -53 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
841 1374 16 3H-SCH23390 -53 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
CHEMBL612 1374 16 3H-SCH23390 -53 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
DB01576 1374 16 3H-SCH23390 -53 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 2 1 1 1.6 C[C@@H](Cc1ccccc1)N None
3016 1385 0 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
3364 1385 0 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
852 1385 0 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
CHEMBL12 1385 0 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
DB00829 1385 0 3H-SCH23390 -2454 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 1 0 2 3.2 Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1 None
3151 1434 93 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1434 93 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1434 93 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1434 93 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1434 93 3H-SCH23390 -12882 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
681 1437 65 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
681 1437 65 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 Low -23 38 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 -97 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1209 1628 69 3H-SCH23390 -1862 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1628 69 3H-SCH23390 -1862 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1628 69 3H-SCH23390 -1862 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1628 69 3H-SCH23390 -1862 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1628 69 3H-SCH23390 -1862 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
1067 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
119 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
1262 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
5410 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
6992099 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
CHEMBL96 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
DB02530 1679 121 3H-SCH23390 -10 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 103 3 2 2 -0.2 NCCCC(=O)O None
119376 1811 41 3H-SCH23390 -54954 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1811 41 3H-SCH23390 -54954 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1811 41 3H-SCH23390 -54954 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
1204 1901 114 3H-SCH23390 -1949 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1901 114 3H-SCH23390 -1949 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1901 114 3H-SCH23390 -1949 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1901 114 3H-SCH23390 -1949 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1901 114 3H-SCH23390 -1949 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1901 114 3H-SCH23390 -1949 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
12575 1957 28 3H-SCH23390 -6606 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 1957 28 3H-SCH23390 -6606 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 1957 28 3H-SCH23390 -6606 16 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
1427 1982 50 3H-dopamine -977 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1427 1982 50 3H-SCH23390 -977 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 3H-dopamine -977 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 3H-SCH23390 -977 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 3H-dopamine -977 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 3H-SCH23390 -977 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 3H-dopamine -977 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 3H-SCH23390 -977 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 3H-dopamine -977 26 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 3H-SCH23390 -977 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
1567 2282 106 3H-SCH23390 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 OC(=O)[C@H](Cc1ccc(c(c1)O)O)N None
3639 2282 106 3H-SCH23390 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 OC(=O)[C@H](Cc1ccc(c(c1)O)O)N None
6047 2282 106 3H-SCH23390 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 OC(=O)[C@H](Cc1ccc(c(c1)O)O)N None
6971033 2282 106 3H-SCH23390 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 OC(=O)[C@H](Cc1ccc(c(c1)O)O)N None
CHEMBL1009 2282 106 3H-SCH23390 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 OC(=O)[C@H](Cc1ccc(c(c1)O)O)N None
DB01235 2282 106 3H-SCH23390 1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 197 3 4 4 0.1 OC(=O)[C@H](Cc1ccc(c(c1)O)O)N None
1310 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
1369 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
33032 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
44272391 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
88747398 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
CHEMBL575060 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
DB00142 2286 108 3H-SCH23390 -43 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 147 4 3 3 -0.7 OC(=O)CC[C@@H](C(=O)O)N None
18971832 2385 0 3H-SCH23390 -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 2385 0 3H-SCH23390 -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 2385 0 3H-SCH23390 -1621 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
119192 2446 48 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1582 2446 48 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
CHEMBL506981 2446 48 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
DB06455 2446 48 3H-SCH23390 -2818 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 586 7 2 7 5.8 COc1cccc(c1c1cc(nn1c1ccnc2c1ccc(c2)Cl)C(=O)NC1(C(=O)O)C2CC3CC1CC(C2)C3)OC None
1605 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
1728 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
22267 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
4095 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
4586 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
5458 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
643985 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
CHEMBL159659 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
CHEMBL651 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
DB00333 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
DB13515 2462 21 3H-dopamine -3235 9 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 7 0 2 4.3 CCC(=O)C(c1ccccc1)(c1ccccc1)CC(N(C)C)C None
134 2478 19 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-SCH23390 -263 67 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1782 2482 81 3H-SCH23390 -676 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
241 2482 81 3H-SCH23390 -676 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
4168 2482 81 3H-SCH23390 -676 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
CHEMBL86 2482 81 3H-SCH23390 -676 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
DB01233 2482 81 3H-SCH23390 -676 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 299 7 2 4 2.0 CCN(CCNC(=O)c1cc(Cl)c(cc1OC)N)CC None
1830 2552 39 3H-dopamine -1778 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1830 2552 39 3H-SCH23390 -1778 27 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-dopamine -1778 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 3H-SCH23390 -1778 27 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-dopamine -1778 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 3H-SCH23390 -1778 27 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-dopamine -1778 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 3H-SCH23390 -1778 27 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-dopamine -1778 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 3H-SCH23390 -1778 27 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
1638 2683 33 3H-SCH23390 -5495 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
1676 2683 33 3H-SCH23390 -5495 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
1878 2683 33 3H-SCH23390 -5495 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
5284596 2683 33 3H-SCH23390 -5495 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
CHEMBL80 2683 33 3H-SCH23390 -5495 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
DB01183 2683 33 3H-SCH23390 -5495 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 1.3 C=CCN1CC[C@@]23[C@@]4([C@H]1Cc1c3c(O[C@H]2C(=O)CC4)c(cc1)O)O None
484 2814 45 3H-SCH23390 -223 35 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
484 2814 45 3H-SCH23390 -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 3H-SCH23390 -223 35 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 3H-SCH23390 -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 3H-SCH23390 -223 35 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 3H-SCH23390 -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
15897 2817 0 3H-SCH23390 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2817 0 3H-SCH23390 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2817 0 3H-SCH23390 -354 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
163839 2910 0 3H-SCH23390 -562 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
268 2910 0 3H-SCH23390 -562 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
CHEMBL55171 2910 0 3H-SCH23390 -562 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 391 6 1 4 3.7 Cc1cccc(c1C)N1CCN(CC1)CCCOc1ccc2c(c1)[nH]c(=O)cc2 None
2136 3046 29 3H-dopamine -2187 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
4768 3046 29 3H-dopamine -2187 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
7268 3046 29 3H-dopamine -2187 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
CHEMBL753 3046 29 3H-dopamine -2187 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
DB00925 3046 29 3H-dopamine -2187 4 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 None
2142 3047 54 3H-SCH23390 -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2142 3047 54 3H-dopamine -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
2142 3047 54 3H-SCH23390 -3801 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3047 54 3H-SCH23390 -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3047 54 3H-dopamine -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3047 54 3H-SCH23390 -3801 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3047 54 3H-SCH23390 -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3047 54 3H-dopamine -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3047 54 3H-SCH23390 -3801 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3047 54 3H-SCH23390 -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3047 54 3H-dopamine -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3047 54 3H-SCH23390 -3801 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3047 54 3H-SCH23390 -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3047 54 3H-dopamine -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3047 54 3H-SCH23390 -3801 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3047 54 3H-SCH23390 -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3047 54 3H-dopamine -3801 36 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3047 54 3H-SCH23390 -3801 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
16362 3076 67 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-SCH23390 -52480 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2202 3083 91 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3083 91 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3083 91 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3083 91 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3083 91 3H-SCH23390 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
119570 3110 90 3H-SCH23390 -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570 3110 90 UNDEFINED -7585 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 3H-SCH23390 -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3110 90 UNDEFINED -7585 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 3H-SCH23390 -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3110 90 UNDEFINED -7585 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 3H-SCH23390 -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3110 90 UNDEFINED -7585 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 3H-SCH23390 -7585 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3110 90 UNDEFINED -7585 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2286 3134 48 3H-dopamine -3311 29 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 3H-dopamine -3311 29 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 3H-dopamine -3311 29 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 3H-dopamine -3311 29 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 3H-dopamine -3311 29 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
165193 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
165193 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
2303 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
4946 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
564 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
62882 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
63 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
66366 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
91536 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3138 60 3H-SCH23390 -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3138 60 3H-dopamine -10000 42 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
DB00571 3138 60 3H-SCH23390 -10000 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C None
243 3153 85 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3153 85 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3153 85 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3153 85 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3153 85 3H-SCH23390 -1096 34 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2 3210 19 3H-SCH23390 Low -2089 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
2 3210 19 3H-SCH23390 -977 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SCH23390 Low -2089 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3210 19 3H-SCH23390 -977 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SCH23390 Low -2089 28 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3210 19 3H-SCH23390 -977 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
173 3211 88 3H-SCH23390 -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3211 88 3H-SCH23390 -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3211 88 3H-SCH23390 -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
3033769 3229 54 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3033769 3229 54 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
3299 3229 54 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
94 3229 54 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
CHEMBL8809 3229 54 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SCH23390 -2754 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
DB12518 3229 54 3H-SCH23390 -2754 18 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 346 5 2 4 2.9 CCN1CCC[C@H]1CNC(=O)c1c(O)c(Cl)cc(c1OC)Cl None
2389 3279 114 3H-SCH23390 -331 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -331 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -331 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -331 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -331 67 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2402 3318 58 3H-SCH23390 -74 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3318 58 3H-SCH23390 -74 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3318 58 3H-SCH23390 -74 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3318 58 3H-SCH23390 -74 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3318 58 3H-SCH23390 -74 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
183782 3346 15 3H-SCH23390 -2398 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
237 3346 15 3H-SCH23390 -2398 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL85251 3346 15 3H-SCH23390 -2398 14 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 352 8 1 4 4.4 CCCCN1CCC(CC1)CCC(=O)c1cc(Cl)c(cc1OC)N None
128563 3408 28 3H-SCH23390 -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3408 28 3H-SCH23390 -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3408 28 3H-SCH23390 -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3408 28 3H-SCH23390 -2398 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
221 3435 63 UNDEFINED -478 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3435 63 UNDEFINED -478 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3435 63 UNDEFINED -478 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
1577 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1577 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SCH23390 -50 25 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SCH23390 -389 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SCH23390 -389 25 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 3H-SCH23390 -389 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
1267 3744 43 3H-dopamine -4168 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3744 43 3H-dopamine -4168 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3744 43 3H-dopamine -4168 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
102 4064 44 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4064 44 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4064 44 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4064 44 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4064 44 3H-SCH23390 -25118 49 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
19493 11151 60 3H-SCH23390 -2344 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
CHEMBL1179 11151 60 3H-SCH23390 -2344 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
CHEMBL1255743 11151 60 3H-SCH23390 -2344 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 133 1 1 1 1.5 N[C@@H]1C[C@H]1c1ccccc1 None
2662 11279 124 3H-SCH23390 -3 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11279 124 3H-SCH23390 -3 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
10836 14329 13 3H-SCH23390 -147 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
CHEMBL1201201 14329 13 3H-SCH23390 -147 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 3 1 1 1.8 CN[C@@H](C)Cc1ccccc1 None
671690 26890 32 3H-SCH23390 -10 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
CHEMBL1365455 26890 32 3H-SCH23390 -10 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
10297 26905 29 3H-SCH23390 -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 26905 29 3H-SCH23390 -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
156391 46537 95 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46537 95 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46537 95 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
53321123 58240 0 UNDEFINED -181 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 0 2 4.2 C#CCOc1cccc2c1-c1cccc3c1C(C2)N(CCC)CC3 None
CHEMBL1684022 58240 0 UNDEFINED -181 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 0 2 4.2 C#CCOc1cccc2c1-c1cccc3c1C(C2)N(CCC)CC3 None
10624 69957 17 3H-SCH23390 -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 69957 17 3H-SCH23390 -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 69957 17 3H-SCH23390 -102 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
14659268 79228 2 UNDEFINED -134 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 None
CHEMBL2115032 79228 2 UNDEFINED -134 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 297 1 2 4 2.9 COc1cc2c3c(c1)-c1c(ccc(O)c1O)CC3N(C)CC2 None
108107 79534 30 3H-dopamine -15 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 79534 30 3H-dopamine -15 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 79534 30 3H-dopamine -15 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 79534 30 3H-dopamine -15 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
442108 84213 5 3H-SCH23390 -1 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
CHEMBL222287 84213 5 3H-SCH23390 -1 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
54477 84230 34 3H-SCH23390 -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
54477 84230 34 UNDEFINED -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 3H-SCH23390 -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
CHEMBL22242 84230 34 UNDEFINED -138 22 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 6 1 4 2.7 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(Br)c1OC None
21830793 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91403 5 3H-8-OH-DPAT -66069 46 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
2244 93798 96 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 93798 96 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
44448057 94377 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 1 1 2 3.5 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL253529 94377 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 1 1 2 3.5 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
44448062 94407 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
CHEMBL253737 94407 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 3 0 2 4.2 CCCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
44448066 94434 0 UNDEFINED -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 None
CHEMBL253948 94434 0 UNDEFINED -1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.4 Oc1cc2c3c(c1O)Cc1ccccc1CC3NCC2 None
44448068 94435 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 4 0 3 5.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(Cc1ccccc1)CC2 None
CHEMBL253949 94435 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 4 0 3 5.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(Cc1ccccc1)CC2 None
104870 98423 39 3H-SCH23390 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98423 39 3H-SCH23390 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98423 39 3H-SCH23390 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
3025067 98923 58 3H-dopamine -512 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 98923 58 3H-dopamine -512 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 98923 58 3H-dopamine -512 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
3663 99505 79 3H-SCH23390 -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99505 79 3H-SCH23390 -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
127708 112029 7 UNDEFINED -251 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 112029 7 UNDEFINED -251 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
3452843 119020 13 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
CHEMBL345686 119020 13 3H-SCH23390 -1 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 516 6 2 4 5.5 Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)c3ccccc3C)C2=O)c1 None
446220 132998 13 3H-SCH23390 -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 132998 13 3H-SCH23390 -1778 45 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
44208932 140176 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140176 6 UNDEFINED -120226 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
9669 152654 2 3H-dopamine -3890 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 2 1 2 3.9 CC(C)=CCN1CC[C@@]2(C)c3cc(O)ccc3C[C@@H]1[C@H]2C None
CHEMBL397705 152654 2 3H-dopamine -3890 7 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 285 2 1 2 3.9 CC(C)=CCN1CC[C@@]2(C)c3cc(O)ccc3C[C@@H]1[C@H]2C None
44448058 154665 0 UNDEFINED 2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL402517 154665 0 UNDEFINED 2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 3.8 CCCN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
44448065 154942 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
CHEMBL404037 154942 0 UNDEFINED -2 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 2 2 3 3.6 CCCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
44448069 154990 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 337 4 0 3 4.2 CCCN1CCc2cc(OC)c(OC)c3c2C1Cc1ccccc1C3 None
CHEMBL404241 154990 0 UNDEFINED 1 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 337 4 0 3 4.2 CCCN1CCc2cc(OC)c(OC)c3c2C1Cc1ccccc1C3 None
1615 167228 22 3H-SCH23390 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167228 22 3H-SCH23390 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
4595 176141 102 3H-dopamine -186 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176141 102 3H-dopamine -186 15 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
44581146 176254 0 UNDEFINED -354 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.5 COc1cccc2cc3n(c12)CCN(CCCCNC(=O)C1=Cc2ccccc2CN1)C3 None
CHEMBL461023 176254 0 UNDEFINED -354 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.5 COc1cccc2cc3n(c12)CCN(CCCCNC(=O)C1=Cc2ccccc2CN1)C3 None
24949694 182188 0 UNDEFINED -3981 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 6 0 7 3.4 c1cnc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
CHEMBL479026 182188 0 UNDEFINED -3981 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 6 0 7 3.4 c1cnc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
43815 186337 58 3H-SCH23390 -1995 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186337 58 3H-SCH23390 -1995 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186337 58 3H-SCH23390 -1995 24 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
11676600 187162 0 UNDEFINED -1174 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 442 6 0 5 4.4 COc1cccc2cc3n(c12)CCN(CCCCN1CCn2c(cc4ccccc42)C1=O)C3 None
CHEMBL495573 187162 0 UNDEFINED -1174 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 442 6 0 5 4.4 COc1cccc2cc3n(c12)CCN(CCCCN1CCn2c(cc4ccccc42)C1=O)C3 None
11704609 187440 0 UNDEFINED -2691 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 427 6 0 5 3.6 N#Cc1cccc(N2CCN(CCCCN3CCn4c(cc5ccccc54)C3=O)CC2)c1 None
CHEMBL497573 187440 0 UNDEFINED -2691 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 427 6 0 5 3.6 N#Cc1cccc(N2CCN(CCCCN3CCn4c(cc5ccccc54)C3=O)CC2)c1 None
11596521 187453 0 UNDEFINED -18620 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 402 7 1 5 3.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
CHEMBL497604 187453 0 UNDEFINED -18620 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 402 7 1 5 3.6 N#Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
5280343 187691 119 3H-SCH23390 -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 187691 119 3H-SCH23390 -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 187691 119 3H-SCH23390 -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
44581147 189780 0 UNDEFINED -1659 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.6 COc1cccc2c1C1CCN(CCCCNC(=O)C3=Cc4ccccc4CN3)CC1=N2 None
CHEMBL517730 189780 0 UNDEFINED -1659 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 430 7 2 5 3.6 COc1cccc2c1C1CCN(CCCCNC(=O)C3=Cc4ccccc4CN3)CC1=N2 None
24949388 189934 0 UNDEFINED -6309 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 6 0 6 3.5 c1ccc(N2CCN(CCCSc3nc4ccccc4o3)CC2)nc1 None
CHEMBL517962 189934 0 UNDEFINED -6309 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 6 0 6 3.5 c1ccc(N2CCN(CCCSc3nc4ccccc4o3)CC2)nc1 None
54676228 192874 108 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 192874 108 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
2771 193347 67 3H-SCH23390 -120 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 193347 67 3H-SCH23390 -120 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 193347 67 3H-SCH23390 -120 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 193347 67 3H-SCH23390 -120 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 193347 67 3H-SCH23390 -120 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 193347 67 3H-SCH23390 -120 26 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
4495 194860 87 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 194860 87 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
45112568 197128 0 UNDEFINED -229 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 None
CHEMBL583422 197128 0 UNDEFINED -229 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 9 1 7 3.7 CCOC(=O)c1cc2cc(OCCCN3CCN(Cc4ccc5c(c4)OCO5)CC3)ccc2[nH]1 None
54677470 198867 110 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 198867 110 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 198867 110 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 200587 19 3H-SCH23390 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 200587 19 3H-SCH23390 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 200587 19 3H-SCH23390 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3036864 201066 16 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 3H-SCH23390 -26 27 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
5281600 201336 85 3H-SCH23390 -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 201336 85 3H-SCH23390 -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 201377 82 3H-SCH23390 -25 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 201377 82 3H-SCH23390 -25 40 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 201790 12 3H-SCH23390 -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 201790 12 3H-SCH23390 -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 201790 12 3H-SCH23390 -3 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
1614 201960 22 3H-SCH23390 -81 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 201960 22 3H-SCH23390 -81 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
202478 202981 15 3H-SCH23390 -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 202981 15 3H-SCH23390 -97 25 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
5311189 203133 4 3H-SCH23390 -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 203133 4 3H-SCH23390 -194 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
4158 203630 21 3H-SCH23390 -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 203630 21 3H-SCH23390 -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 203630 21 3H-SCH23390 -141 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 203790 64 3H-SCH23390 -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 203790 64 3H-SCH23390 -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 203790 64 3H-SCH23390 -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
5324346 203870 53 3H-SCH23390 -1 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL1409 203870 53 3H-SCH23390 -1 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
CHEMBL814 203870 53 3H-SCH23390 -1 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 None
7108 204044 105 3H-SCH23390 -8 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 199 0 1 2 3.9 c1ccc2c(c1)Nc1ccccc1S2 None
CHEMBL828 204044 105 3H-SCH23390 -8 5 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 199 0 1 2 3.9 c1ccc2c(c1)Nc1ccccc1S2 None
16231 205776 53 3H-dopamine -7 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 205776 53 3H-dopamine -7 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
12057539 206301 39 3H-SCH23390 -18620 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
3661 206301 39 3H-SCH23390 -18620 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
CHEMBL9751 206301 39 3H-SCH23390 -18620 20 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 4 1 4 1.9 CN1C2CCC1CC(OC(=O)C(CO)c1ccccc1)C2 None
6852400 214160 0 3H-dopamine -14125 21 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
6852400 214160 0 3H-SCH23390 -25118 21 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
6852400 214160 0 3H-SCH23390 -25118 21 Rhesus macaque 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-dopamine -14125 21 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-SCH23390 -25118 21 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-SCH23390 -25118 21 Rhesus macaque 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
57174031 214163 0 3H-SCH23390 -1778 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
None 214166 0 3H-dopamine -7943 10 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
11954224 214174 0 3H-SCH23390 -3467 59 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3246155 214183 0 3H-dopamine -43651 16 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 4 0 2 4.4 CN1C2CCC1CC(C2)OC(C3=CC=CC=C3)C4=CC=CC=C4 None
11954259 214201 0 3H-dopamine -7762 43 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
57525649 214214 0 3H-SCH23390 -1 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 187 4 0 1 2.2 CC(CC1=CC=CC=C1)N(C)CC#C None
44134711 214215 0 3H-SCH23390 -112201 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 340 6 2 4 2.8 CCC1=CC(=C(C(=C1O)C(=O)NCC2CCCN2CC)OC)Cl None
None 214216 0 3H-SCH23390 -1071 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.2 C1CN(CCN1CCCC2=CC=CC=C2)CCOC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F.Cl.Cl None
None 214217 0 3H-SCH23390 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
4528 214218 0 3H-SCH23390 -120 9 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1CC(C2=C(C1)C(=CC=C2)N)C3=CC=CC=C3 None
4528 214218 0 3H-SCH23390 -120 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 238 1 1 2 2.8 CN1CC(C2=C(C1)C(=CC=C2)N)C3=CC=CC=C3 None
5365247 214219 0 3H-SCH23390 -97 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 4 0 2 3.8 CN(C)CC=C(C1=CC=C(C=C1)Br)C2=CN=CC=C2 None
6420041 214219 0 3H-SCH23390 -97 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 4 0 2 3.8 CN(C)CC=C(C1=CC=C(C=C1)Br)C2=CN=CC=C2 None
444 214245 0 3H-SCH23390 -2089 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 239 3 1 2 3.3 CC(C(=O)C1=CC(=CC=C1)Cl)NC(C)(C)C None
104911 214249 0 3H-SCH23390 -41686 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 214256 0 3H-SCH23390 -6309 13 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 453 9 2 6 2.6 COC1=CC(=C(C=C1C(=O)CCC2CCN(CC2)CCNS(=O)(=O)C)Cl)N.Cl None
131632304 214266 0 3H-SCH23390 -70794 13 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 303 4 1 5 0.9 CN1C2CC(CC1C3C2O3)OC(=O)C(CO)C4=CC=CC=C4 None
119380 214359 0 125I-SCH 23982 -1 8 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 166 1 0 3 1.8 CC1=NOC(=C1)C2CCCN2C None
None 214366 0 3H-SCH23390 -10000 23 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
25137849 214425 0 3H-SCH23390 -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 214425 0 3H-SCH23390 -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
3337 214441 0 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
65801 214441 0 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
66264 214441 0 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
91452 214441 0 3H-SCH23390 -1513 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)CC1=CC(=CC=C1)C(F)(F)F None
None 214481 0 3H-SCH23390 -13 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 255 2 1 2 2.4 CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl None
None 214486 0 3H-SCH23390 -95499 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 214502 0 3H-dopamine -8317 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
5372683 214534 0 3H-dopamine -1479 3 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 400 5 1 4 4.2 C1CN(CCN1CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO None
3821 214549 0 3H-SCH23390 -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(CCCCC1=O)C2=CC=CC=C2Cl None
None 214560 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 214561 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 214562 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 214563 0 3H-SCH23390 -1 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 214564 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 117 0 1 3 -0.0 C1CSC(=O)C1N None
None 214565 0 3H-SCH23390 -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 214566 0 3H-SCH23390 -1 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 214567 0 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 214574 0 3H-SCH23390 -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 214575 0 3H-SCH23390 -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
4978 214577 0 3H-SCH23390 -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 214578 0 3H-SCH23390 -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 214579 0 3H-SCH23390 -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 214580 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
None 214591 0 3H-SCH23390 -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 214639 0 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 214640 0 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 214641 0 3H-SCH23390 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
3672 214642 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)CC1=CC=C(C=C1)C(C)C(=O)O None
84003 214643 0 3H-SCH23390 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 214644 0 3H-SCH23390 -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 214645 0 3H-SCH23390 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
5090 214646 0 3H-SCH23390 -1348 31 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
119607 214647 0 3H-SCH23390 -97 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N None
None 214648 0 3H-SCH23390 -7 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
None 214703 0 UNDEFINED -660 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214703 0 UNDEFINED -660 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
None 214747 0 3H-SCH23390 -4570 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
None 214753 0 3H-SCH23390 -1 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 7 4 5 1.8 CN(C)CC(C1=CC=C(C=C1)O)C2(CCCCC2)O.C(CC(=O)O)C(=O)O.O None
None 214827 0 UNDEFINED -549 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
None 214980 0 UNDEFINED -3090 2 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 251 0 2 2 3.1 CC1=C(C2=C(CC3C4=C2C=CC=C4CCN3)C=C1)O None
None 214982 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 601 23 0 3 11.9 CCCCCCCCCCCCCCCCCCCCCC(=O)OC1=CC=CC2=C1C3=C4C(C2)N(CCC4=CC=C3)CCC None
None 214983 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 363 6 0 3 5.3 CCCCC(=O)OC1=CC=CC2=C1C3=C4C(C2)N(CCC4=CC=C3)CCC None
None 214984 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 3 0 3 4.1 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OC(=O)C None
None 214992 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 4.1 CCCN1CCC2=C3C1CC4=C(C=CC(=C4)O)OC3=CC=C2 None
None 214993 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 4.1 CCCN1CCC2=CC(=CC3=C2C1CC4=CC=CC=C4O3)O None
None 215032 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 323 4 1 3 4.3 CCCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
None 215422 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 436 9 2 5 4.7 CCCN(CCCCNC(=O)C1=CC2=CC=CC=C2C=C1)C3CCC4=C(C3)SC(=N4)N None
None 215534 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 4 0 4 4.2 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)OC(=O)C None
None 215535 0 UNDEFINED - 1 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 0 4 5.3 CCCCC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)CCC)OC None
None 215778 0 UNDEFINED -1023 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 291 0 0 2 3.8 CC1CC2=C(O1)C3=C(CC4C5=C3C=CC=C5CCN4C)C=C2 None
None 215779 0 UNDEFINED -69 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 3 1 3 3.9 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)CC=C)O None
None 215780 0 UNDEFINED -151 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 321 4 0 3 4.0 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)OCC=C None
None 215781 0 UNDEFINED -346 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 0 0 2 4.5 CC1=CC2=C(O1)C3=C(CC4C5=C3C=CC=C5CCN4C)C=C2 None
None 215782 0 UNDEFINED -707 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 289 2 0 2 3.5 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC#C None
None 215783 0 UNDEFINED -74 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 291 2 1 2 3.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)CC=C)O None
None 215784 0 UNDEFINED -831 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 291 3 0 2 4.0 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC=C None
None 215785 0 UNDEFINED -19 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 0 2 5.6 CCCN1CCC2=CC=CC3=C2C1CC4=C3C5=C(C=C4)C(=C(O5)C)C None
None 215786 0 UNDEFINED -30 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 2 0 2 5.3 CCCN1CCC2=CC=CC3=C2C1CC4=C3C5=C(C=C4)C=C(O5)C None
None 215787 0 UNDEFINED -79 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 4 0 2 4.6 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC#CC None
None 215788 0 UNDEFINED -15 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 333 2 0 2 4.9 CCCN1CCC2=CC=CC3=C2C1CC4=C3C5=C(CC(O5)(C)C)C=C4 None
None 215789 0 UNDEFINED -12 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 4 1 2 4.7 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)CC=C)O None
None 215790 0 UNDEFINED -67 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 5 0 2 5.6 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC=C(C)C None
None 215791 0 UNDEFINED -26 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 333 5 0 2 5.2 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC(=C)C None
None 215792 0 UNDEFINED -35 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 5 0 2 4.8 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)OCC=C None
None 215800 0 UNDEFINED 1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 4 1 2 5.4 CCCN1CCC2=CC=CC3=C2C1CC4=C(C=CC(=C43)O)CC=C(C)C None
None 215801 0 UNDEFINED 1 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 333 4 1 2 5.0 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)CC(=C)C)O None
1524 2150 89 3H-SCH23390 -323 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-SCH23390 -323 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-SCH23390 -323 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-SCH23390 -323 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-SCH23390 -323 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-SCH23390 -323 51 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
25058166 214181 0 UNDEFINED -147 26 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 UNDEFINED -147 26 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
126968774 214213 0 3H-dopamine -42 7 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O None
1242 3556 23 3H-SCH23390 -6 17 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 -6 17 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 -6 17 Rhesus macaque 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1353 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
45112462 195291 0 UNDEFINED -831 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 None
CHEMBL566533 195291 0 UNDEFINED -831 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 441 8 1 5 4.6 CCOC(=O)c1cc2cc(OCCCN3CCN(c4cccc(Cl)c4)CC3)ccc2[nH]1 None
25058166 214181 0 3H-SCH23390 Low -6 26 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 Low -6 26 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
3153 294 24 3H-dopamine -39 7 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 294 24 3H-dopamine -39 7 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 294 24 3H-dopamine -39 7 Bovine 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
1212 1632 45 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -14 65 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
681 1437 65 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-dopamine -23 38 Bovine 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214979 0 UNDEFINED -190 2 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 237 0 2 2 2.8 C1CNC2CC3=C(C4=C2C1=CC=C4)C(=CC=C3)O None
2726 906 64 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1218 3559 24 3H-SCH23390 -11 7 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
938 3559 24 3H-SCH23390 -11 7 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
CHEMBL353335 3559 24 3H-SCH23390 -11 7 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 None
2726 906 64 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -186 72 Bovine 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
None 215219 0 UNDEFINED 1 3 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 365 5 0 4 4.5 CCCCC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)C)OC None
277 1274 55 3H-SCH23390 -47 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 3H-SCH23390 -47 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 3H-SCH23390 -47 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 3H-SCH23390 -47 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 3H-SCH23390 -47 45 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1353 1880 85 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH233930 -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -26 65 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2435 3533 78 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 UNDEFINED -43 48 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1353 1880 85 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -38 85 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
277 1274 55 3H-dopamine -1445 45 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 3H-dopamine -1445 45 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 3H-dopamine -1445 45 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 3H-dopamine -1445 45 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 3H-dopamine -1445 45 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
4508 3090 91 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
4866774 3090 91 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
509 3090 91 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
838 3090 91 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
CHEMBL1740 3090 91 3H-dopamine -239 13 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O None
4249 77814 30 3H-dopamine -1230 5 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
CHEMBL2104700 77814 30 3H-dopamine -1230 5 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 355 6 1 3 4.1 Cc1ccc(C2(O)CCN(CCCC(=O)c3ccc(F)cc3)CC2)cc1 None
681 1437 65 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 UNDEFINED -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 215627 0 UNDEFINED - 1 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 409 2 3 4 5.0 CCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=C(C=C5)O.Cl None
2337 3205 72 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SCH23390 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
24949690 181024 0 UNDEFINED -1819 3 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 None
CHEMBL477200 181024 0 UNDEFINED -1819 3 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 399 7 0 6 4.6 COc1ccccc1N1CCN(CCCSc2nc3ccccc3s2)CC1 None
2337 3205 72 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SCH233930 -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
681 1437 65 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 125I-SCH 23982 -154 38 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2865 4079 67 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 UNDEFINED -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
None 215034 0 UNDEFINED - 1 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 3.5 CCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
2337 3205 72 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 UNDEFINED -53 62 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2865 4079 67 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-SCH233930 -114 53 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
None 215625 0 UNDEFINED - 1 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 331 1 2 3 4.0 CCN1CCC2=C3C1CC4=C(C3=CC(=C2)C)C(=C(C=C4)O)O.Cl None
1242 3556 23 3H-SCH23390 Low -11 17 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 Low -11 17 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 Low -11 17 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
2105 3005 34 3H-SCH23390 -537 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 3H-SCH23390 -537 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 3H-SCH23390 -537 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 3H-SCH23390 -537 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 3H-SCH23390 -537 33 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
135409468 2004 63 3H-SCH23390 -12 40 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2004 63 3H-SCH23390 -12 40 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2004 63 3H-SCH23390 -12 40 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
37459 735 10 3H-SCH23390 -8 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -8 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -8 24 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1222 1634 44 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1634 44 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1634 44 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1634 44 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1634 44 3H-dopamine -2344 32 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3596 46 3H-dopamine -31622 59 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-dopamine -31622 59 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-dopamine -31622 59 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-dopamine -31622 59 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-dopamine -31622 59 Bovine 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135398737 944 89 3H-SCH23390 -44 91 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -44 91 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -44 91 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -44 91 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -44 91 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
127708 112029 7 UNDEFINED -22 5 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 112029 7 UNDEFINED -22 5 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
135 2496 38 3H-SCH23390 -91 57 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-SCH23390 -91 57 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-SCH23390 -91 57 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-SCH23390 -91 57 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-SCH23390 -91 57 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
16362 3076 67 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-SCH23390 -7413 29 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
681 1437 65 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 -97 38 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
2389 3279 114 3H-SCH23390 -467 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -467 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -467 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -467 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -467 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 215219 0 UNDEFINED -12 3 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 365 5 0 4 4.5 CCCCC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)C)OC None
1353 1880 85 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -74 85 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214995 0 UNDEFINED - 1 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 419 3 1 5 3.9 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)O)Br None
1242 3556 23 3H-SCH23390 -5 17 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 -5 17 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 -5 17 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1890 2718 44 3H-SCH23390 -234 15 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
4449 2718 44 3H-SCH23390 -234 15 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
7247 2718 44 3H-SCH23390 -234 15 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
CHEMBL623 2718 44 3H-SCH23390 -234 15 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
DB01149 2718 44 3H-SCH23390 -234 15 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl None
11954259 214201 0 3H-SCH23390 -5011 43 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
71299720 214172 0 3H-SCH23390 -1202 16 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
1353 1880 85 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -107 85 Rhesus macaque 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
134 2478 19 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-SCH23390 -575 67 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1613 2316 44 3H-SCH23390 -3 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-SCH23390 -3 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-SCH23390 -3 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-SCH23390 -3 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-SCH23390 -3 44 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
681 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
33630 178379 94 3H-dopamine -281 27 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 3H-dopamine -281 27 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
24949534 188927 0 UNDEFINED -2041 3 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 None
CHEMBL514074 188927 0 UNDEFINED -2041 3 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 397 8 0 6 4.5 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3o2)CC1 None
11653679 180609 1 UNDEFINED -24 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
CHEMBL476108 180609 1 UNDEFINED -24 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 374 6 0 3 4.7 O=C(CCCN1CCCN(c2ccc(Cl)cc2)CC1)c1ccc(F)cc1 None
None 215033 0 UNDEFINED - 1 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 309 3 1 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
5018 3493 8 3H-SCH23390 -28 9 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 3493 8 3H-SCH23390 -28 9 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 3493 8 3H-SCH23390 -28 9 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 3493 8 3H-SCH23390 -28 9 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
172286 214637 0 3H-SCH23390 1 2 Mouse 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 331 0 0 4 3.6 CN1CCN(CC1)C2=NC3=C(CC4=C2C=CS4)C=CC(=C3)Cl None
681 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-dopamine -23 38 Bovine 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 214632 0 3H-SCH23390 165 2 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 327 1 1 3 4.4 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OC=C4)O)Cl None
None 214986 0 UNDEFINED - 1 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 343 1 2 3 4.5 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=CC=C4)O)C5=CC=C(C=C5)O None
15443 117307 91 3H-dopamine -257 9 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 None
CHEMBL340211 117307 91 3H-dopamine -257 9 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 327 6 0 4 3.0 O=C(CCCN1CCN(c2ccccn2)CC1)c1ccc(F)cc1 None
5018 3493 8 3H-SCH23390 -28 9 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 3493 8 3H-SCH23390 -28 9 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 3493 8 3H-SCH23390 -28 9 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 3493 8 3H-SCH23390 -28 9 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
3036864 201066 16 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 201066 16 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 201066 16 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 201066 16 125I-Spectramide -2 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
2286 3134 48 3H-SCH23390 -588 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 3H-SCH23390 -588 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 3H-SCH23390 -588 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 3H-SCH23390 -588 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 3H-SCH23390 -588 29 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
100 3745 52 3H-dopamine -309 55 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-dopamine -309 55 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-dopamine -309 55 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-dopamine -309 55 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-dopamine -309 55 Bovine 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1212 1632 45 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 UNDEFINED -51 65 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
11976 907 54 UNDEFINED -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 UNDEFINED -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 UNDEFINED -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 UNDEFINED -12 23 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1212 1632 45 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -288 65 Bovine 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1242 3556 23 3H-SCH23390 -1 17 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1242 3556 23 3H-SCH23390 1 17 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 -1 17 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 1 17 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 -1 17 Mouse 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 1 17 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5281878 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-dopamine -34 16 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1632 45 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-dopamine -288 65 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1621 2396 16 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-SCH23390 -588 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
None 214530 0 3H-dopamine 2 2 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 267 1 2 2 1.5 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)N None
100 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 214990 0 UNDEFINED - 1 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 325 3 2 4 3.6 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O None
100 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-dopamine -309 55 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
30137 2833 0 3H-SCH23390 -676 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2833 0 3H-SCH23390 -676 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2833 0 3H-SCH23390 -676 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
1153 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1598 53 3H-SCH23390 -32 10 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 214619 0 3H-SCH23390 -11220 2 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 487 8 2 4 3.9 CNC1=C(C=C(C(=C1)OC)C(=O)NCCN(C)CC2=CC=C(C=C2)I)Cl None
135398737 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1524 2150 89 3H-SCH23390 -75 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-SCH23390 -75 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-SCH23390 -75 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-SCH23390 -75 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-SCH23390 -75 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-SCH23390 -75 51 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
None 214532 0 3H-dopamine -741 2 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 454 6 1 4 4.8 C1CN(CCN1CCCC2C3=C(C=C(C=C3)F)SC4=C2C=C(C=C4)C(F)(F)F)CCO None
135398737 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -44 91 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
242 467 117 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
242 467 117 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-SCH23390 -281 51 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 UNDEFINED -74 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
4106 2466 16 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-SCH23390 -5 33 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 214998 0 UNDEFINED - 1 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 453 2 2 5 3.5 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)I None
37459 735 10 3H-SCH23390 -53 24 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -53 24 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -53 24 Bovine 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
6603820 95330 13 3H-SCH23390 1 13 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 1 13 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
1238 201484 21 3H-SCH23390 -5 16 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 3H-SCH23390 -5 16 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
3153 294 24 3H-SCH23390 High -39 7 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 294 24 3H-SCH23390 High -39 7 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 294 24 3H-SCH23390 High -39 7 Bovine 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
46780481 107045 18 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-SCH23390 -29 53 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
20840341 214423 0 3H-SCH23390 -3 4 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 451 5 1 3 6.2 C1CN(CCC1CCO)CCC=C2C3=C(C=C(C=C3)F)SC4=C2C=C(C=C4)C(F)(F)F None
6603820 95330 13 3H-SCH23390 -2 13 Rhesus macaque 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 -2 13 Rhesus macaque 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
1524 2150 89 3H-SCH23390 -323 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-SCH23390 -323 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-SCH23390 -323 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-SCH23390 -323 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-SCH23390 -323 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-SCH23390 -323 51 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
484 2814 45 3H-dopamine -4 35 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 3H-dopamine -4 35 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 3H-dopamine -4 35 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
None 214981 0 UNDEFINED -165 2 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 293 2 1 2 4.2 CCCN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)C)O None
24949857 181185 0 UNDEFINED -7413 3 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 None
CHEMBL477765 181185 0 UNDEFINED -7413 3 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 413 8 0 6 5.0 COc1ccccc1N1CCN(CCCCSc2nc3ccccc3s2)CC1 None
25212275 173849 0 UNDEFINED -4897 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL455288 173849 0 UNDEFINED -4897 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 682 13 0 8 7.4 O=C(OCCN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1)c1ccc(OCCCN2CCCCC2)cc1 None
25212276 189473 0 UNDEFINED -575 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL517244 189473 0 UNDEFINED -575 6 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 508 11 0 3 7.4 CN(CCCC12CCC(c3ccccc31)c1ccccc12)Cc1ccc(OCCCN2CCCCC2)cc1 None
3151 1434 93 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1434 93 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1434 93 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1434 93 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1434 93 3H-SCH23390 -2630 26 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
135398737 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-dopamine -204 91 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
126968774 214213 0 3H-SCH23390 -831 7 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C)CC1C(=O)N2CCCC2C3(N1C(=O)C(O3)(C(C)C)NC(=O)C4CN(C5CC6=C(NC7=CC=CC(=C67)C5=C4)Br)C)O None
5475158 66877 20 3H-SCH23390 -489 13 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 66877 20 3H-SCH23390 -489 13 Bovine 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
1212 1632 45 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -51 65 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 3279 114 UNDEFINED -331 67 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 UNDEFINED -331 67 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 UNDEFINED -331 67 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 UNDEFINED -331 67 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 UNDEFINED -331 67 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 3745 52 3H-SCH23390 -16 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SCH23390 -16 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SCH23390 -16 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SCH23390 -16 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SCH23390 -16 55 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
6603820 95330 13 3H-SCH23390 -4 13 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 -4 13 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
None 214635 0 125I-SCH 23982 74 2 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 365 2 3 4 3.7 C1C2CC3CC1CC(C2)(C3)C4CC5=C(C=CC(=C5O)O)C(O4)CN.Cl None
4106 2466 16 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2466 16 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2466 16 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2466 16 3H-dopamine -524 33 Bovine 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2435 3533 78 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 3H-SCH23390 -43 48 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
25058166 214181 0 UNDEFINED -147 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 UNDEFINED -147 26 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 214996 0 UNDEFINED - 1 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 481 4 0 5 4.1 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)OC)I None
None 214590 0 3H-SCH23390 -281 19 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
3294 1975 106 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-SCH23390 -56 44 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
134 2478 19 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-SCH23390 -186 67 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
None 214480 0 3H-SCH23390 -3090 3 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 315 6 1 3 4.3 CCCN(CCC1=CC=CS1)C2CCC3=C(C2)C=CC=C3O None
2801 161325 56 3H-SCH23390 -10 28 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161325 56 3H-SCH23390 -10 28 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161325 56 3H-SCH23390 -10 28 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
10742 3560 27 3H-SCH23390 -2 7 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
1225 3560 27 3H-SCH23390 -2 7 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
CHEMBL35354 3560 27 3H-SCH23390 -2 7 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
2470 3596 46 3H-SCH23390 -4168 59 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SCH23390 -4168 59 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SCH23390 -4168 59 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SCH23390 -4168 59 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SCH23390 -4168 59 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
4382 104301 29 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
86470 104301 29 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
CHEMBL1256484 104301 29 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
CHEMBL31088 104301 29 3H-dopamine 22 2 Bovine 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 167 3 3 3 0.9 CNCCc1ccc(O)c(O)c1 None
1212 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 3279 114 3H-SCH23390 -331 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -331 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -331 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -331 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -331 67 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
44591134 175626 0 UNDEFINED -194 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL459373 175626 0 UNDEFINED -194 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 535 11 0 5 7.7 CN(CCCN1c2ccccc2Sc2ccc(Cl)cc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
681 1437 65 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 -154 38 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1212 1632 45 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -51 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
46780481 107045 18 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-SCH23390 -64 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 214987 0 UNDEFINED - 1 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 341 3 1 5 3.2 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)O None
1212 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-dopamine -288 65 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2181 3079 0 3H-SCH23390 -389 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3079 0 3H-SCH23390 -389 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3079 0 3H-SCH23390 -389 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3079 0 3H-SCH23390 -389 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3079 0 3H-SCH23390 -389 34 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
None 215423 0 UNDEFINED -158 6 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 532 10 0 4 8.0 CN(CCC=C1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl)CC4=CC=C(C=C4)OCCCN5CCCCC5 None
2726 906 64 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 906 64 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -14 72 Mouse 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -18 72 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1353 1880 85 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745 2869 108 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -26 65 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -23 65 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11976 907 54 3H-dopamine -234 23 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 3H-dopamine -234 23 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 3H-dopamine -234 23 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 3H-dopamine -234 23 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -23 65 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135 2496 38 3H-dopamine -457 57 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-dopamine -457 57 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-dopamine -457 57 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-dopamine -457 57 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-dopamine -457 57 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 215220 0 UNDEFINED -7 2 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 339 0 3 6 3.0 CN1CCC2=C3C1CC4=C(C3=CC5=C2SC(=N5)N)C(=C(C=C4)O)O None
None 215036 0 UNDEFINED 1 4 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 251 0 1 2 3.1 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O None
1242 3556 23 3H-SCH23390 1 17 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 1 17 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 1 17 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
73333 5886 23 UNDEFINED -3 8 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL1079935 5886 23 UNDEFINED -3 8 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 401 7 1 2 4.2 CCNC(=O)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
4452 2721 18 3H-SCH23390 -89125 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2721 18 3H-SCH23390 -89125 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2721 18 3H-SCH23390 -89125 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
2337 3205 72 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SCH23390 -134 62 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398737 944 89 3H-SCH23390 -37 91 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -37 91 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -37 91 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -37 91 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -37 91 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3279 114 3H-SCH23390 -467 67 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -467 67 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -467 67 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -467 67 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -467 67 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1353 1880 85 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -30 85 Pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -38 85 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214978 0 UNDEFINED -60 2 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 263 1 0 1 4.0 CCC1=CC=CC2=C1C3=C4C(C2)N(CCC4=CC=C3)C None
None 214161 0 3H-SCH23390 -45708 20 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 215628 0 UNDEFINED - 1 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 345 2 2 3 4.4 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)C)C(=C(C=C4)O)O.Cl None
1153 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1598 53 3H-SCH23390 -32 10 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
2601 3721 30 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3721 30 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3721 30 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3721 30 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3721 30 3H-SCH23390 -16 21 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
1028 287 69 3H-dopamine -52 29 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
139148732 287 69 3H-dopamine -52 29 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
479 287 69 3H-dopamine -52 29 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
5816 287 69 3H-dopamine -52 29 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
CHEMBL679 287 69 3H-dopamine -52 29 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
DB00668 287 69 3H-dopamine -52 29 Bovine 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O None
135398737 944 89 3H-dopamine -204 91 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-dopamine -204 91 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-dopamine -204 91 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-dopamine -204 91 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-dopamine -204 91 Bovine 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
125564 659 88 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
388 659 88 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
7670 659 88 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
CHEMBL178803 659 88 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
DB09223 659 88 3H-SCH23390 -5011 7 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 367 3 0 3 4.7 CCN1CCN(CC1)c1nc2CCCCCCc2c(c1)c1ccc(cc1)F None
135398737 944 89 3H-SCH233930 -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH233930 -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH233930 -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH233930 -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH233930 -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
209 3008 94 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-SCH23390 -51 23 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
135398737 944 89 UNDEFINED -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -44 91 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
134 2478 19 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 3H-dopamine -575 67 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
25058166 214181 0 UNDEFINED -144 26 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 UNDEFINED -144 26 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
None 214989 0 UNDEFINED - 1 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.9 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O None
10145 214988 0 UNDEFINED - 1 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 355 4 0 5 3.5 CN1CCC2=CC(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)OC None
None 215217 0 UNDEFINED -1 2 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 265 0 2 3 2.6 CN1CCC2=C3C1CC4=C(C3=CC(=C2)N)C(=CC=C4)N None
185 3943 54 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-SCH23390 -6606 37 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
122324 203 17 125I-SCH 23982 323 3 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 None
6077 203 17 125I-SCH 23982 323 3 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 None
CHEMBL86931 203 17 125I-SCH 23982 323 3 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1 None
37459 735 10 3H-SCH23390 -10 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -10 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -10 24 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
5281878 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -2 16 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281878 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -34 16 Bovine 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
9861622 197763 3 3H-SCH23390 1202 2 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 None
CHEMBL59139 197763 3 3H-SCH23390 1202 2 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 313 0 1 2 4.0 CN1CCc2cc(Cl)c(O)cc2C2c3ccccc3CCC21 None
62865 1248 0 3H-SCH23390 -2 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1248 0 3H-SCH23390 -2 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1248 0 3H-SCH23390 -2 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1248 0 3H-SCH23390 -2 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1248 0 3H-SCH23390 -2 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
1621 2396 16 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 3H-dopamine -97 44 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2865 4079 67 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-SCH23390 -114 53 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
11954224 214174 0 3H-dopamine -426 59 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1242 3556 23 3H-SCH23390 High -11 17 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 High -11 17 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 High -11 17 Bovine 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1427 1982 50 3H-SCH23390 -295 26 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
357 1982 50 3H-SCH23390 -295 26 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
3696 1982 50 3H-SCH23390 -295 26 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
CHEMBL11 1982 50 3H-SCH23390 -295 26 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
DB00458 1982 50 3H-SCH23390 -295 26 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C None
10333195 47922 0 UNDEFINED -10 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
CHEMBL155208 47922 0 UNDEFINED -10 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
44591099 175616 0 UNDEFINED -1122 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL459350 175616 0 UNDEFINED -1122 6 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 494 10 0 3 7.0 CN(CCC=C1c2ccccc2CCc2ccccc21)Cc1ccc(OCCCN2CCCCC2)cc1 None
135398745 2869 108 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -23 65 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 215626 0 UNDEFINED - 1 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 393 2 2 3 5.3 CCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5.Cl None
1353 1880 85 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -512 85 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 UNDEFINED -74 85 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135 2496 38 3H-SCH23390 -457 57 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-SCH23390 -457 57 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-SCH23390 -457 57 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-SCH23390 -457 57 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-SCH23390 -457 57 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
6852400 214160 0 3H-SCH23390 -14125 21 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-SCH23390 -14125 21 Bovine 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
186 1777 47 3H-SCH23390 -42 16 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1777 47 3H-SCH23390 -42 16 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1777 47 3H-SCH23390 -42 16 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
11696813 187335 12 UNDEFINED -316 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
CHEMBL496739 187335 12 UNDEFINED -316 9 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 391 7 1 4 4.1 Cc1cccc(N2CCN(CCCCNC(=O)c3cc4ccccc4o3)CC2)c1 None
6603820 95330 13 125I-SCH 23982 -4 13 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 125I-SCH 23982 -4 13 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
2865 4079 67 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 3H-SCH23390 -114 53 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2105 3005 34 3H-SCH23390 -537 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 3H-SCH23390 -537 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 3H-SCH23390 -537 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 3H-SCH23390 -537 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 3H-SCH23390 -537 33 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1212 1632 45 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-dopamine -288 65 Bovine 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
None 214827 0 UNDEFINED -549 6 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
30137 2833 0 UNDEFINED -3981 10 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2833 0 UNDEFINED -3981 10 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2833 0 UNDEFINED -3981 10 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
135398745 2869 108 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -26 65 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
6603820 95330 13 3H-SCH23390 -4 13 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 -4 13 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
10707972 168490 0 UNDEFINED 1 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
CHEMBL439639 168490 0 UNDEFINED 1 2 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cc(O)cc3c2C1Cc1ccccc1O3 None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 UNDEFINED -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -83 91 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2470 3596 46 3H-SCH23390 -51286 59 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SCH23390 -51286 59 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SCH23390 -51286 59 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SCH23390 -51286 59 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SCH23390 -51286 59 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 1880 85 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -38 85 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
73453 29403 22 3H-dopamine -51 17 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 None
CHEMBL1385840 29403 22 3H-dopamine -51 17 Bovine 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 None
2470 3596 46 3H-SCH23390 -10964 59 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SCH23390 -10964 59 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SCH23390 -10964 59 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SCH23390 -10964 59 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SCH23390 -10964 59 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25293 214187 0 3H-dopamine -724 4 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 443 6 1 3 5.4 C1CN(CCC1(C2=CC(=C(C=C2)Cl)C(F)(F)F)O)CCCC(=O)C3=CC=C(C=C3)F None
44448059 94379 0 UNDEFINED 5 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
CHEMBL253530 94379 0 UNDEFINED 5 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 251 0 2 2 2.7 Oc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
25058166 214181 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
213 3792 50 3H-SCH23390 -7 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 3H-SCH23390 -7 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 3H-SCH23390 -7 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 3H-SCH23390 -7 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 3H-SCH23390 -7 43 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
681 1437 65 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 -97 38 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
13994416 190096 1 UNDEFINED -851 2 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1C(C2)N(C)CC3 None
CHEMBL5181992 190096 1 UNDEFINED -851 2 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.5 Cc1ccc2c(c1O)-c1cccc3c1C(C2)N(C)CC3 None
5018 3493 8 3H-SCH23390 -194 9 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 3493 8 3H-SCH23390 -194 9 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 3493 8 3H-SCH23390 -194 9 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 3493 8 3H-SCH23390 -194 9 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
5770 203349 80 3H-SCH23390 -2 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
CHEMBL772 203349 80 3H-SCH23390 -2 6 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
242 467 117 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-SCH23390 -281 51 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2337 3205 72 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 UNDEFINED -134 62 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
1524 2150 89 3H-SCH23390 -288 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-SCH23390 -288 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-SCH23390 -288 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-SCH23390 -288 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-SCH23390 -288 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-SCH23390 -288 51 Bovine 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
5281878 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -2 16 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
37459 735 10 3H-SCH23390 -10 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -10 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -10 24 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
1577 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
164512405 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
2537 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5355 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5501 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
643497 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
688272 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
958 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
960 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL196677 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL26 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
CHEMBL267044 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB00391 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
DB16021 3647 104 None -50 25 Bovine 8.4 pKi = 8.4 Binding
In vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membraneIn vitro displacement of [3H]- SCH 23390 from the dopamine receptor D1 of bovine striatal membrane
Drug Central 341 6 2 5 0.6 CCN1CCCC1CNC(=O)c1cc(ccc1OC)S(=O)(=O)N None
5281878 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -11 16 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2402 3318 58 None -74 25 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3318 58 None -74 25 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3318 58 None -74 25 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3318 58 None -74 25 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3318 58 None -74 25 Human 8.4 pKi = 8.4 Binding
NoneNone
Drug Central 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
1212 1632 45 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1212 1632 45 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -8 65 Mouse 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -14 65 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
10742 3560 27 3H-SCH23390 2 7 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
1225 3560 27 3H-SCH23390 2 7 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
CHEMBL35354 3560 27 3H-SCH23390 2 7 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O None
6603820 95330 13 3H-SCH23390 1 13 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 1 13 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
2662 11279 124 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11279 124 None -3 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
441383 20133 54 None -12 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 20133 54 None -12 17 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
28417 39799 48 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
CHEMBL1479 39799 48 None -1 12 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 337 0 1 3 4.2 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=Cc5oncc5C[C@]4(C)[C@H]3CC[C@@]21C None
2105 3005 34 3H-SCH23390 -645 33 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2105 3005 34 3H-SCH23390 -645 33 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 3H-SCH23390 -645 33 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 3H-SCH23390 -645 33 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 3H-SCH23390 -645 33 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 3H-SCH23390 -645 33 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 3H-SCH23390 -645 33 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 3H-SCH23390 -645 33 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 3H-SCH23390 -645 33 Mouse 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 3H-SCH23390 -645 33 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
25058166 214181 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 -144 26 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
4011 81996 43 UNDEFINED -64 23 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81996 43 UNDEFINED -64 23 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
135398737 944 89 3H-SCH23390 -169 91 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -169 91 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -169 91 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -169 91 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -169 91 Rhesus macaque 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5018 3493 8 3H-SCH23390 2 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
943 3493 8 3H-SCH23390 2 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
946 3493 8 3H-SCH23390 2 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
CHEMBL13668 3493 8 3H-SCH23390 2 9 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O None
115237 55296 113 3H-SCH23390 -13 54 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-SCH23390 -13 54 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1242 3556 23 3H-SCH23390 1 17 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 1 17 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 1 17 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
242 467 117 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 3H-SCH23390 -74 51 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
16363 589 48 3H-dopamine -20892 6 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
312 589 48 3H-dopamine -20892 6 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
9215 589 48 3H-dopamine -20892 6 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL297302 589 48 3H-dopamine -20892 6 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB12867 589 48 3H-dopamine -20892 6 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
16362 3076 67 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-dopamine -30199 29 Bovine 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
1816 2504 99 3H-SCH23390 -323 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2504 99 3H-SCH23390 -323 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2504 99 3H-SCH23390 -323 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2504 99 3H-SCH23390 -323 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2504 99 3H-SCH23390 -323 16 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
3294 1975 106 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-SCH23390 -56 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2337 3205 72 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SCH23390 -134 62 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135 2496 38 3H-MIANSERIN -91 57 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 3H-MIANSERIN -91 57 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 3H-MIANSERIN -91 57 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 3H-MIANSERIN -91 57 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 3H-MIANSERIN -91 57 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44448070 94452 0 UNDEFINED 3 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 None
CHEMBL254147 94452 0 UNDEFINED 3 2 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 295 2 1 3 3.0 COc1cc2c3c(c1OC)Cc1ccccc1CC3NCC2 None
25186021 187441 0 UNDEFINED -1318 3 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 None
CHEMBL497574 187441 0 UNDEFINED -1318 3 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2ccc(Cl)cc2Cl)CC1 None
25058166 214181 0 3H-SCH23390 -147 26 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 -147 26 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
11712530 187307 0 UNDEFINED -41686 4 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 None
CHEMBL496531 187307 0 UNDEFINED -41686 4 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 470 6 0 4 5.0 O=C1c2cc3ccccc3n2CCN1CCCCN1CCN(c2cccc(Cl)c2Cl)CC1 None
2726 906 64 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -36 72 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
209 3008 94 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2113 3008 94 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4748 3008 94 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL567 3008 94 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00850 3008 94 3H-SCH23390 -51 23 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 6 1 5 3.9 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
None 214827 0 UNDEFINED -549 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
681 1437 65 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 -154 38 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1222 1634 44 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1634 44 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1634 44 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1634 44 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1634 44 3H-SCH23390 -741 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
None 214193 0 3H-SCH23390 -9772 14 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 473 7 0 5 3.5 COC1=CC=CC=C1N2CCN(CC2)CCCCN3C(=O)C4=CC=CC=C4C3=O.Br None
2337 3205 72 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SCH23390 -134 62 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
135398745 2869 108 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -23 65 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
None 215035 0 UNDEFINED 1 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.2 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
None 215035 0 UNDEFINED -1 4 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.2 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)O None
25186569 176408 0 UNDEFINED -45708 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 None
CHEMBL462508 176408 0 UNDEFINED -45708 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 456 7 1 4 4.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2cn1 None
None 214479 0 3H-SCH23390 -11 4 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 226 0 2 2 1.4 C1CCC(=O)NCCCCCC(=O)NCC1 None
1524 2150 89 3H-SCH23390 -75 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 3H-SCH23390 -75 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 3H-SCH23390 -75 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 3H-SCH23390 -75 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 3H-SCH23390 -75 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 3H-SCH23390 -75 51 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
219050 3321 21 3H-SCH23390 -2884 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
52 3321 21 3H-SCH23390 -2884 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
CHEMBL431367 3321 21 3H-SCH23390 -2884 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 None
5281878 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281878 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -4 16 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -11 16 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
30137 2833 0 3H-SCH23390 -1202 10 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2833 0 3H-SCH23390 -1202 10 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2833 0 3H-SCH23390 -1202 10 Mouse 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
6446379 214533 0 3H-dopamine -154 2 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 472 5 1 4 5.1 C1CN(CCN1CC/C=C/2\C3=CC=CC=C3SC4=C2C=C(C=C4)Cl)CCO.Cl.Cl None
10264969 48031 0 UNDEFINED -6 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
CHEMBL155352 48031 0 UNDEFINED -6 2 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 267 0 1 3 3.3 CN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
None 214999 0 UNDEFINED - 1 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 405 2 2 5 3.6 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)O)OC)O)Br None
2181 3079 0 3H-dopamine -776 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3079 0 3H-dopamine -776 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3079 0 3H-dopamine -776 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3079 0 3H-dopamine -776 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3079 0 3H-dopamine -776 34 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
None 214827 0 UNDEFINED -549 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
46780481 107045 18 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 3H-SCH23390 -64 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
64143 197186 57 None -1 8 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C None
CHEMBL584 197186 57 None -1 8 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 567 9 4 6 4.7 Cc1c(O)cccc1C(=O)N[C@@H](CSc1ccccc1)[C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C None
2477 734 54 None -28 28 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 734 54 None -28 28 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 734 54 None -28 28 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 734 54 None -28 28 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 734 54 None -28 28 Bovine 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatumInhibition of [3H]SCH-23390 binding to Dopamine receptor D1 of bovine striatum
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2780 110040 32 None -138 11 Bovine 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 110040 32 None -138 11 Bovine 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranesDisplacement of [3H]SCH-23390 [0.3 nM (Kd=0.35 nM)] from dopamine receptor D1 in bovine striatal membranes
Drug Central 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
176 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 394 63 None -4 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3198 203802 73 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 203802 73 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 203802 73 None -31 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
2812 4711 96 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4711 96 None -32 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1016 3690 75 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2561 3690 75 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
2733526 3690 75 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
5384 3690 75 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
CHEMBL83 3690 75 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
DB00675 3690 75 None -29 35 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 371 8 0 2 6.0 CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1 None
1816 2504 99 None -323 16 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2504 99 None -323 16 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2504 99 None -323 16 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2504 99 None -323 16 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2504 99 None -323 16 Rat 8.3 pKi = 8.3 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
1816 2504 99 None -323 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
4205 2504 99 None -323 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
7241 2504 99 None -323 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
CHEMBL654 2504 99 None -323 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
DB00370 2504 99 None -323 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 265 0 0 3 2.5 CN1CCN2C(C1)c1ccccc1Cc1c2nccc1 None
448537 159703 86 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
CHEMBL411 159703 86 None -28 25 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 None
4189 205195 91 None -25 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 205195 91 None -25 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 205195 91 None -25 34 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1042 1551 20 None -204 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1551 20 None -204 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1551 20 None -204 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1551 20 None -204 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1551 20 None -204 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
2407 3320 73 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 3320 73 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 3320 73 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 3320 73 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 3320 73 None -128 7 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
5353853 17803 41 None -19 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
9556529 17803 41 None -19 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1262 17803 41 None -19 15 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
11154555 788 57 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
5037 788 57 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
7671 788 57 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL2028019 788 57 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL3085826 788 57 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB06016 788 57 None -1445 12 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay
Drug Central 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl None
2247 502 77 None -61 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 502 77 None -61 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 502 77 None -61 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 502 77 None -61 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 502 77 None -61 41 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
12488 1627 51 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
941361 1627 51 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
CHEMBL30008 1627 51 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
DB04841 1627 51 None -19 23 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F None
2351 3234 60 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3234 60 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3234 60 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3234 60 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3234 60 None -16 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
240 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
2769 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
44279790 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
660 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL1729 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
CHEMBL560739 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
DB00604 931 39 None -19 25 Rat 8.2 pKi = 8.2 Binding
The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striataThe ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata
Drug Central 465 9 2 6 3.4 COC1CN(CCCOc2ccc(cc2)F)CCC1NC(=O)c1cc(Cl)c(cc1OC)N None
1830 2552 39 None -16 27 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
207 2552 39 None -16 27 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
23897 2552 39 None -16 27 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
CHEMBL460 2552 39 None -16 27 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
DB01618 2552 39 None -16 27 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 None
None 214633 0 3H-SCH23390 1737 2 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 340 2 1 5 2.9 CN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC4=C3OCC4)O)[N+](=O)[O-] None
11057 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
3468 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL459265 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
CHEMBL64894 175575 19 None -2 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 None
135 2496 38 None -46 57 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None -46 57 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None -46 57 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None -46 57 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None -46 57 Rat 8.2 pKi = 8.2 Binding
Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2286 3134 48 None -30 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
4927 3134 48 None -30 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
7282 3134 48 None -30 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
CHEMBL643 3134 48 None -30 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
DB01069 3134 48 None -30 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C None
2600 3720 73 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
2608 3720 73 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
5405 3720 73 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
CHEMBL17157 3720 73 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
DB00342 3720 73 None -7 13 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O None
6917970 3635 54 3H-SCH23390 -1 34 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3635 54 3H-SCH23390 -1 34 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3635 54 3H-SCH23390 -1 34 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
2284 3133 27 None -36 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3133 27 None -36 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3133 27 None -36 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3133 27 None -36 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3133 27 None -36 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
10531 1392 18 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 1392 18 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 1392 18 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 1392 18 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 1392 18 None -218 24 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
3117 206106 100 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 206106 100 None -2 16 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
2389 3279 114 UNDEFINED -331 67 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 UNDEFINED -331 67 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 UNDEFINED -331 67 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 UNDEFINED -331 67 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 UNDEFINED -331 67 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3947 214378 0 3H-SCH23390 -74 15 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 418 7 0 3 5.8 CN(CCCN1C2=CC=CC=C2CCC3=CC=CC=C31)CC(=O)C4=CC=C(C=C4)Cl None
5 139 66 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-SCH23390 -16595 54 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 214481 0 3H-SCH23390 -6 6 Mouse 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 255 2 1 2 2.4 CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl None
None 214481 0 3H-SCH23390 -6 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 255 2 1 2 2.4 CCCN1CCCC2C1CC3=C(C2)NN=C3.Cl None
11954259 214201 0 3H-SCH23390 -169 43 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
681 1437 65 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 High -23 38 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
115237 55296 113 3H-SCH23390 -457 54 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-SCH23390 -457 54 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
3153 294 24 3H-SCH23390 -3019 7 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
932 294 24 3H-SCH23390 -3019 7 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
CHEMBL26736 294 24 3H-SCH23390 -3019 7 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O None
135398745 2869 108 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
31116 214531 0 3H-dopamine -37 2 Bovine 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 609 5 3 6 2.6 CC(C)C1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
135398745 2869 108 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH233930 -26 65 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214997 0 UNDEFINED - 1 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 433 4 0 5 4.2 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)OC)Br None
2389 3279 114 3H-SCH23390 -467 67 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -467 67 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -467 67 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -467 67 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -467 67 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 215533 0 UNDEFINED - 1 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 323 2 0 4 3.4 CC(=O)OC1=CC=CC2=C1C3=CC(=CC4=C3C(C2)N(CC4)C)OC None
135398737 944 89 UNDEFINED -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
5568 195823 26 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
66069 195823 26 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
CHEMBL1201102 195823 26 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
CHEMBL570 195823 26 3H-dopamine -251 5 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 None
16362 3076 67 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-dopamine -30199 29 Bovine 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
185 3943 54 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-SCH23390 -6606 37 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
135398737 944 89 3H-SCH23390 -44 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -44 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -44 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -44 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -44 91 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1613 2316 44 3H-SCH23390 -4 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 3H-SCH23390 -4 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 3H-SCH23390 -4 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 3H-SCH23390 -4 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 3H-SCH23390 -4 44 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
11954259 214201 0 3H-dopamine -7762 43 Bovine 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
None 214827 0 UNDEFINED -549 6 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 158 7 0 2 2.6 CCCCN(CCCC)N=O None
3294 1975 106 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 3H-SCH23390 -794 44 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2995 202700 49 3H-SCH23390 -23 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202700 49 3H-SCH23390 -23 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202700 49 3H-SCH23390 -23 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995 202700 49 3H-SCH23390 -23 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202700 49 3H-SCH23390 -23 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202700 49 3H-SCH23390 -23 22 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
135398737 944 89 3H-SCH23390 -22 91 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 3H-SCH23390 -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -22 91 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -22 91 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -22 91 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -22 91 Mouse 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3279 114 3H-SCH23390 -331 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -331 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -331 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -331 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -331 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11654739 176274 0 UNDEFINED -20417 4 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 None
CHEMBL461236 176274 0 UNDEFINED -20417 4 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 422 7 1 4 4.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2)CC1)c1cc2ccccc2cn1 None
1242 3556 23 125I-SCH 23982 -5 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 125I-SCH 23982 -5 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 125I-SCH 23982 -5 17 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
24949693 181722 0 UNDEFINED -7244 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
CHEMBL478413 181722 0 UNDEFINED -7244 3 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 370 6 0 6 4.0 c1ccc(N2CCN(CCCSc3nc4ccccc4s3)CC2)nc1 None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2389 3279 114 3H-SCH233930 -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH233930 -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH233930 -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH233930 -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH233930 -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2470 3596 46 3H-SCH23390 -4168 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SCH23390 -4168 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SCH23390 -4168 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SCH23390 -4168 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SCH23390 -4168 59 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 1880 85 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -38 85 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -26 65 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
2389 3279 114 UNDEFINED -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 UNDEFINED -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 UNDEFINED -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 UNDEFINED -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 UNDEFINED -467 67 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 3745 52 3H-SCH23390 -16 55 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SCH23390 -16 55 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SCH23390 -16 55 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SCH23390 -16 55 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SCH23390 -16 55 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
1353 1880 85 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 214576 0 3H-SCH23390 16 28 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
135 2496 38 None -91 57 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2496 38 None -91 57 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2496 38 None -91 57 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2496 38 None -91 57 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2496 38 None -91 57 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
None 214994 0 UNDEFINED - 1 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 467 3 1 5 3.8 CN1CCC2=C(C(=C(C3=C2C1CC4=CC(=C(C=C43)OC)OC)OC)O)I None
11954224 214174 0 None -3467 59 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
242 467 117 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -281 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
26987 936 29 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 936 29 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 936 29 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 936 29 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 936 29 None -245 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
2585 790 100 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 790 100 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 790 100 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 790 100 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 790 100 None -112 22 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
31101 720 39 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 None -436 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
6603820 95330 13 3H-SCH23390 1 13 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 1 13 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
3191 102385 93 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102385 93 None -12 25 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
107715 199260 18 None -144 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 199260 18 None -144 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 199260 18 None -144 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
3168 9172 84 None -89 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9172 84 None -89 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
150 2473 18 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 2473 18 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 2473 18 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 2473 18 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 2473 18 None -43 15 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
2407 3320 73 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
59227 3320 73 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
941 3320 73 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
CHEMBL1303 3320 73 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
DB05271 3320 73 None -60 7 Bovine 8.2 pKi = 8.2 Binding
Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390Binding affinity of compound for Dopamine receptor D1 using [3H]-SCH- 23390
Drug Central 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 None
5440 216001 0 None -1 9 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 399 6 0 5 5.0 CCSC1=CC=C2SC3=CC=CC=C3N(CCCN3CCN(C)CC3)C2=C1 None
4011 81996 43 None -64 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
CHEMBL21731 81996 43 None -64 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 None
134 2478 19 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2478 19 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2478 19 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2478 19 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2478 19 None -263 67 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1530 2151 44 None -53 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
3827 2151 44 None -53 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
7206 2151 44 None -53 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
CHEMBL534 2151 44 None -53 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
DB00920 2151 44 None -53 20 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 None
68663 27075 17 None -5 3 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 None
CHEMBL136711 27075 17 None -5 3 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 391 5 1 3 4.0 O=C(CCCN1CCN2Cc3[nH]c4ccccc4c3CC2C1)c1ccc(F)cc1 None
135398737 944 89 None -204 91 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -204 91 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -204 91 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -204 91 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -204 91 Bovine 8.2 pKi = 8.2 Binding
Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390Binding affinity against bovine dopamine receptor D1 using radioligand [3H]-SCH- 23390
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737 944 89 None -37 91 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -37 91 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -37 91 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -37 91 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -37 91 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membraneDisplacement of [3H]SCH 23990 from dopamine receptor D1 in porcine striatal membrane
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2337 3205 72 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 None -53 62 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
7077 66625 24 None -3 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL186720 66625 24 None -3 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
CHEMBL3925724 66625 24 None -3 5 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant dopamine receptor D1Binding affinity for human recombinant dopamine receptor D1
Drug Central 255 6 0 2 3.2 CN(C)CCOc1ccccc1Cc1ccccc1 None
2105 3005 34 None -537 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3005 34 None -537 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3005 34 None -537 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3005 34 None -537 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3005 34 None -537 33 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
2470 3596 46 None -4168 59 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 None -4168 59 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 None -4168 59 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 None -4168 59 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 None -4168 59 Human 8.2 pKi = 8.2 Binding
Binding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkeyBinding affinity against dopamine receptor D1 by using [3H]-SCH- 23390 as radioligand in caudate-putamen of monkey
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3561 18886 34 None -1 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
CHEMBL1289 18886 34 None -1 11 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 360 2 0 1 4.4 Clc1cc(Cl)c(OCC#CI)cc1Cl None
4543 169982 36 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL1201156 169982 36 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
CHEMBL445 169982 36 None -5 29 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2ccccc21 None
5462328 216016 0 None 1 3 Rat 8.2 pKi = 8.2 Binding
Dopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranesDopamine receptor D1 affinity was tested in vitro against corpus striatum from rat brain membranes
Drug Central 369 2 0 6 2.0 CN1CC[C@]23[C@H]4OC5=C(OC(C)=O)C=CC(C[C@@H]1[C@@H]2C=C[C@@H]4OC(C)=O)=C35 None
2801 161325 56 None -10 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL1200710 161325 56 None -10 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
CHEMBL415 161325 56 None -10 28 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21 None
3294 1975 106 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 1975 106 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 1975 106 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 1975 106 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 1975 106 None -56 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2435 3533 78 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 None -72 48 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Dopamine receptor D1Binding affinity towards human Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
134551 355 25 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 355 25 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 355 25 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 355 25 None -28 21 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
37 766 56 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 766 56 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 766 56 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 766 56 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 766 56 None -14 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
1524 2150 89 None -75 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2150 89 None -75 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2150 89 None -75 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2150 89 None -75 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2150 89 None -75 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2150 89 None -75 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
191 399 92 None -26 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
201 399 92 None -26 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
2170 399 92 None -26 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
CHEMBL1113 399 92 None -26 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
DB00543 399 92 None -26 28 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 None
1621 2396 16 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2396 16 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2396 16 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2396 16 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2396 16 None -112 44 Mouse 8.2 pKi = 8.2 Binding
Binding affinities towards Dopamine receptor D1Binding affinities towards Dopamine receptor D1
Drug Central 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11978813 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 713 72 None -8 23 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
681 1437 65 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 None -97 38 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
33630 178379 94 None -5 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
CHEMBL47050 178379 94 None -5 27 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assayDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293T cells by radioligand binding assay
Drug Central 523 7 1 2 7.5 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 None
52919 14317 43 None -15 4 Pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL1200986 14317 43 None -15 4 Pig 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 529 15 0 4 8.1 CCCCCCCCCC(=O)OC1(c2ccc(Cl)cc2)CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
135398737 944 89 None -44 91 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -44 91 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -44 91 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -44 91 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -44 91 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
277 1274 55 None -47 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1274 55 None -47 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1274 55 None -47 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1274 55 None -47 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1274 55 None -47 45 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
1712 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
4078 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
7227 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
CHEMBL1088 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
DB00933 2456 0 None -6 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C None
2389 3279 114 3H-SCH23390 -467 67 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -467 67 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -467 67 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -467 67 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -467 67 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2448 214184 0 3H-dopamine -426 17 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
1042 1551 20 3H-dopamine -97 16 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1551 20 3H-dopamine -97 16 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1551 20 3H-dopamine -97 16 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1551 20 3H-dopamine -97 16 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1551 20 3H-dopamine -97 16 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
None 215036 0 UNDEFINED -2 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 251 0 1 2 3.1 CN1CCC2=CC=CC3=C2C1CC4=C3C(=CC=C4)O None
10265732 94408 0 UNDEFINED 2 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
CHEMBL253738 94408 0 UNDEFINED 2 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 0 2 3 2.8 CN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
2389 3279 114 3H-SCH23390 -331 67 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -331 67 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -331 67 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -331 67 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -331 67 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
185 3943 54 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 3943 54 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 3943 54 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 3943 54 3H-SCH23390 -6606 37 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
44448063 154706 0 UNDEFINED 3 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
CHEMBL402736 154706 0 UNDEFINED 3 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 1 1 2 3.0 COc1cc2c3c(c1)Cc1ccccc1CC3NCC2 None
68617 203816 60 3H-SCH23390 -912 25 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL1709 203816 60 3H-SCH23390 -912 25 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
CHEMBL809 203816 60 3H-SCH23390 -912 25 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 None
1242 3556 23 125I-SCH 23982 1 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 125I-SCH 23982 1 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 125I-SCH 23982 1 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
1588 2294 24 3H-SCH23390 -190 43 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 3H-SCH23390 -190 43 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 3H-SCH23390 -190 43 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 3H-SCH23390 -190 43 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 3H-SCH23390 -190 43 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
10355510 155121 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
CHEMBL404865 155121 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 265 0 1 2 3.1 CN1CCc2cc(O)cc3c2C1Cc1ccccc1C3 None
None 214990 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 325 3 2 4 3.6 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=C(C=C4)O)O None
1353 1880 85 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-dopamine -512 85 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44448061 94406 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
CHEMBL253736 94406 0 UNDEFINED 1 2 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 293 2 0 2 3.8 CCN1CCc2cc(OC)cc3c2C1Cc1ccccc1C3 None
None 215629 0 UNDEFINED - 1 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 407 3 2 3 5.7 CCCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5.Cl None
20840341 214423 0 3H-dopamine -75 4 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 451 5 1 3 6.2 C1CN(CCC1CCO)CCC=C2C3=C(C=C(C=C3)F)SC4=C2C=C(C=C4)C(F)(F)F None
115237 55296 113 3H-SCH23390 -457 54 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 3H-SCH23390 -457 54 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
31101 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
25058166 214181 0 3H-SCH23390 -144 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 -144 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
16362 3076 67 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-dopamine -30199 29 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
10660476 47109 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
CHEMBL154468 47109 0 UNDEFINED - 1 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 281 1 1 3 3.7 CCN1CCc2cccc3c2C1Cc1cc(O)ccc1O3 None
134551 355 25 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 355 25 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 355 25 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 355 25 3H-dopamine -53 21 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
135398745 2869 108 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 UNDEFINED -23 65 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
31101 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 720 39 3H-SCH23390 -436 35 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
127708 112029 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 112029 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
228 441 26 None -4 24 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None -4 24 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None -4 24 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None -4 24 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None -4 24 Mouse 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cellsDisplacement of [3H]SCH23390 from dopamine D1 receptor in mouse Ltk- fibroblast cells
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
2448 214184 0 None -5 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 419 6 1 3 4.5 C1CN(CCC1(C2=CC=C(C=C2)Br)O)CCCC(=O)C3=CC=C(C=C3)F None
1212 1632 45 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 3H-SCH23390 -51 65 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 1880 85 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -30 85 Pig 8.2 pKi = 8.2 Binding
Displacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenatesDisplacement of [3H]SCH23390 from D1 receptor from porcine cerebral cortex homogenates
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
180 397 50 None -109 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 None -109 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 None -109 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 None -109 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 None -109 38 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1588 2294 24 None -190 43 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2294 24 None -190 43 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2294 24 None -190 43 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2294 24 None -190 43 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2294 24 None -190 43 Human 8.2 pKi = 8.2 Binding
Affinity towards Dopamine receptor D1Affinity towards Dopamine receptor D1
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2274 3124 53 None -16 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 None -16 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 None -16 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 None -16 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 None -16 32 Human 8.2 pKi = 8.2 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
2726 906 64 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -36 72 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
25058166 214181 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1613 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2316 44 None -4 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
228 441 26 None -30 24 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None -30 24 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None -30 24 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None -30 24 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None -30 24 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
212 3746 43 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3746 43 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3746 43 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3746 43 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3746 43 None -6 25 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
135398737 944 89 None -83 91 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 None -83 91 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 None -83 91 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 None -83 91 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 None -83 91 Rat 8.1 pKi = 8.1 Binding
Affinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligandAffinity was evaluated as inhibition constant for dopamine receptor D1 using [3H]-SCH- 23390 as radioligand
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
21302490 112308 26 None -8 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3233142 112308 26 None -8 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
CHEMBL3306803 112308 26 None -8 9 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 393 5 0 4 3.9 CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12 None
115237 55296 113 None -13 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55296 113 None -13 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398745 2869 108 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -26 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
133 2460 48 None -30 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2460 48 None -30 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2460 48 None -30 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2460 48 None -30 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2460 48 None -30 42 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
2726 906 64 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 None -18 72 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
103 4089 56 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 None -28 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1212 1632 45 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1632 45 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1632 45 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1632 45 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1632 45 None -51 65 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2389 3279 114 None -331 67 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -331 67 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -331 67 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -331 67 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -331 67 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
2389 3279 114 None -467 67 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 None -467 67 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 None -467 67 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 None -467 67 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 None -467 67 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3389 215982 0 None -1 26 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
1353 1880 85 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -74 85 Rat 8.1 pKi = 8.1 Binding
Affinity for Dopamine receptor D1Affinity for Dopamine receptor D1
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2869 108 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 None -23 65 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
11976 907 54 None -12 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
667467 907 54 None -12 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
CHEMBL908 907 54 None -12 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
DB01239 907 54 None -12 23 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cellsDisplacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK cells
Drug Central 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl None
5281878 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 None -34 16 Bovine 8.1 pKi = 8.1 Binding
Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determinedBinding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
6761 67457 17 None -5 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67457 17 None -5 18 Human 8.1 pKi = 8.1 Binding
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
1353 1880 85 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 None -38 85 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
16351 102257 41 None -4 5 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL304902 102257 41 None -4 5 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against Dopamine receptor D1 in rat striatal tissueIn vitro binding affinity against Dopamine receptor D1 in rat striatal tissue
Drug Central 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 None
2435 3533 78 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3533 78 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3533 78 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3533 78 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3533 78 None -43 48 Rat 8.1 pKi = 8.1 Binding
Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
37459 735 10 3H-dopamine -53 24 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-dopamine -53 24 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-dopamine -53 24 Bovine 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
127708 112029 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
CHEMBL329904 112029 7 UNDEFINED -22 5 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 279 2 1 2 3.9 CCCN1CCc2cccc3c2C1Cc1cccc(O)c1-3 None
7153 97570 74 3H-SCH23390 -371 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 97570 74 3H-SCH23390 -371 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
103 4089 56 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-SCH23390 -28 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2284 3133 27 3H-dopamine -3019 28 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
4926 3133 27 3H-dopamine -3019 28 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
7281 3133 27 3H-dopamine -3019 28 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
CHEMBL564 3133 27 3H-dopamine -3019 28 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
DB00420 3133 27 3H-dopamine -3019 28 Bovine 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C None
2337 3205 72 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3205 72 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3205 72 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3205 72 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3205 72 3H-SCH23390 -53 62 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
25186023 187161 0 UNDEFINED -50118 4 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl None
CHEMBL495572 187161 0 UNDEFINED -50118 4 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 443 8 0 4 5.9 Clc1cccc(N2CCN(CCCCCOc3cc4ccccc4cn3)CC2)c1Cl None
25058166 214181 0 UNDEFINED -144 26 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 UNDEFINED -144 26 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
44448067 154989 0 UNDEFINED - 1 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 None
CHEMBL404240 154989 0 UNDEFINED - 1 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 309 2 0 3 3.4 COc1cc2c3c(c1OC)Cc1ccccc1CC3N(C)CC2 None
5281878 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -34 16 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2726 906 64 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -36 72 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1241 99716 19 3H-SCH23390 -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL288090 99716 19 3H-SCH23390 -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
CHEMBL552611 99716 19 3H-SCH23390 -2 7 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 295 3 2 3 3.3 C=CCN1CCc2cc(O)c(O)cc2C(c2ccccc2)C1 None
30137 2833 0 UNDEFINED -3981 10 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
8594 2833 0 UNDEFINED -3981 10 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
934 2833 0 UNDEFINED -3981 10 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O None
2726 906 64 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-SCH23390 -18 72 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
214 3799 52 3H-dopamine -891 29 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2740 3799 52 3H-dopamine -891 29 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5566 3799 52 3H-dopamine -891 29 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
66064 3799 52 3H-dopamine -891 29 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL422 3799 52 3H-dopamine -891 29 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00831 3799 52 3H-dopamine -891 29 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5567 42556 24 3H-dopamine -812 7 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
CHEMBL15023 42556 24 3H-dopamine -812 7 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 409 6 1 3 4.8 O=C(CCCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)c1ccc(F)cc1 None
2389 3279 114 3H-SCH23390 -331 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3279 114 3H-SCH23390 -331 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3279 114 3H-SCH23390 -331 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3279 114 3H-SCH23390 -331 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3279 114 3H-SCH23390 -331 67 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
100 3745 52 3H-SCH23390 -309 55 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SCH23390 -309 55 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SCH23390 -309 55 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SCH23390 -309 55 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SCH23390 -309 55 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
None 215400 0 UNDEFINED -199 2 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 359 1 3 4 4.2 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=C(C=C5)O None
1353 1880 85 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1353 1880 85 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -52 85 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214668 0 3H-SCH23390 -691 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 453 8 1 4 4.6 COC1=CC=CC=C1N2CCN(CC2)CCCCNC(=O)C3=CC4=CC=CC=C4C=C3.Cl None
16362 3076 67 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2172 3076 67 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
90 3076 67 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
CHEMBL1423 3076 67 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
DB01100 3076 67 3H-dopamine -30199 29 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 None
2470 3596 46 3H-SCH23390 -31622 59 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SCH23390 -31622 59 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SCH23390 -31622 59 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SCH23390 -31622 59 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SCH23390 -31622 59 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
681 1437 65 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 3H-SCH23390 -1548 38 Pig 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
None 215218 0 UNDEFINED 8 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 280 1 1 3 3.0 CN1CCC2=C3C1CC4=C(C3=CC(=C2)OC)C(=CC=C4)N None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2107 3006 0 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
4747 3006 0 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
9216 3006 0 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
CHEMBL251940 3006 0 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
DB01608 3006 0 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 None
25058166 214181 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
2865 4079 67 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 None -114 53 Human 8.1 pKi = 8.1 Binding
Binding affinity against dopamine receptor D1Binding affinity against dopamine receptor D1
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
681 1437 65 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 None -23 38 Bovine 8.1 pKi = 8.1 Binding
Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
228 441 26 None -35 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 441 26 None -35 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 441 26 None -35 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 441 26 None -35 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 441 26 None -35 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to dopamine D1 receptor high binding site by radioligand displacement assayBinding affinity to dopamine D1 receptor high binding site by radioligand displacement assay
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
5281878 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 None -2 16 Human 8.1 pKi = 8.1 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Drug Central 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
62865 1248 0 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
746 1248 0 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
84 1248 0 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
CHEMBL2104153 1248 0 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
DB09000 1248 0 None -2 14 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 323 4 0 4 4.4 N#Cc1ccc2c(c1)N(CC(CN(C)C)C)c1c(S2)cccc1 None
1153 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1598 53 None -1 10 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranesDisplacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
25058166 214181 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-dopamine -6 26 Bovine 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
1238 201484 21 None -5 16 Rat 8.1 pKi = 8.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL64249 201484 21 None -5 16 Rat 8.1 pKi = 8.1 Binding
Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenateHalf-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate
Drug Central 344 1 0 3 4.3 CN1CCN(C2Cc3ccccc3Sc3ccc(Cl)cc32)CC1 None
46780481 107045 18 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107045 18 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107045 18 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107045 18 None -29 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
37459 735 10 3H-dopamine -53 24 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-dopamine -53 24 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-dopamine -53 24 Bovine 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
15139 197402 48 3H-dopamine -794 4 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 356 7 0 4 3.6 COc1ccccc1N1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
CHEMBL58792 197402 48 3H-dopamine -794 4 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 356 7 0 4 3.6 COc1ccccc1N1CCN(CCCC(=O)c2ccc(F)cc2)CC1 None
16219195 214362 0 3H-dopamine 1 5 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 325 1 1 5 2.9 CN1CCC2=CC3=C(C4=C2C1CC5=C4C(=C(C=C5)OC)O)OCO3 None
None 214985 0 UNDEFINED - 1 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 325 4 0 3 3.9 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)F)C(=CC=C4)OC=O None
5281878 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-dopamine -34 16 Bovine 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
180 397 50 3H-SCH23390 -158 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 3H-SCH23390 -158 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 3H-SCH23390 -158 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 3H-SCH23390 -158 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 3H-SCH23390 -158 38 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
1353 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
484 2814 45 3H-dopamine -4 35 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2814 45 3H-dopamine -4 35 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2814 45 3H-dopamine -4 35 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
2780 110040 32 3H-SCH23390 -630 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
CHEMBL325109 110040 32 3H-SCH23390 -630 11 Mouse 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 None
1353 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -38 85 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
44448064 94433 0 UNDEFINED 1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
CHEMBL253947 94433 0 UNDEFINED 1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 295 1 2 3 3.2 CCN1CCc2cc(O)c(O)c3c2C1Cc1ccccc1C3 None
1353 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-SCH23390 -74 85 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214360 0 3H-SCH23390 -2290 7 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 401 5 1 5 2.2 C1COC(C2=CC=CC=C21)CCN3CCN(CC3)C4=CC=C(C=C4)S(=O)(=O)N None
103 4089 56 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4089 56 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4089 56 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4089 56 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4089 56 3H-SCH23390 -69 53 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2470 3596 46 3H-SCH23390 -51286 59 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3596 46 3H-SCH23390 -51286 59 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3596 46 3H-SCH23390 -51286 59 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3596 46 3H-SCH23390 -51286 59 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3596 46 3H-SCH23390 -51286 59 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135398737 944 89 3H-SCH23390 -83 91 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
279 1631 26 3H-SCH23390 -17 17 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
49381 1631 26 3H-SCH23390 -17 17 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
CHEMBL63756 1631 26 3H-SCH23390 -17 17 Mouse 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 309 0 0 3 3.1 CN1CCN(CC1)C1=Nc2cc(F)ccc2Cc2c1cccc2 None
135398745 2869 108 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2869 108 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2869 108 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2869 108 3H-SCH23390 -23 65 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
44448060 154705 0 UNDEFINED -1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 None
CHEMBL402735 154705 0 UNDEFINED -1 2 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 279 1 0 2 3.4 COc1cc2c3c(c1)Cc1ccccc1CC3N(C)CC2 None
None 215395 0 UNDEFINED -269 11 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 116 4 0 2 1.4 CCCCN(C)N=O None
25058166 214181 0 3H-SCH23390 -147 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 214181 0 3H-SCH23390 -147 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
135398737 944 89 3H-SCH23390 -83 91 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 3H-SCH23390 -83 91 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 3H-SCH23390 -83 91 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 3H-SCH23390 -83 91 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 3H-SCH23390 -83 91 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
44591012 175007 0 UNDEFINED -177 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 None
CHEMBL457957 175007 0 UNDEFINED -177 6 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 522 10 0 3 6.6 CN(CCC=C1c2ccccc2CCc2ccccc21)C(=O)Cc1ccc(OCCCN2CCCCC2)cc1 None
None 215399 0 UNDEFINED 1 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 343 1 2 3 4.5 CN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=CC=C5 None
3168 9172 84 3H-dopamine -1318 21 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
CHEMBL1108 9172 84 3H-dopamine -1318 21 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1 None
180 397 50 UNDEFINED -109 38 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 397 50 UNDEFINED -109 38 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 397 50 UNDEFINED -109 38 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 397 50 UNDEFINED -109 38 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 397 50 UNDEFINED -109 38 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
135398737 944 89 UNDEFINED -44 91 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 944 89 UNDEFINED -44 91 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 944 89 UNDEFINED -44 91 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 944 89 UNDEFINED -44 91 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 944 89 UNDEFINED -44 91 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
100 3745 52 3H-SCH23390 -47 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3745 52 3H-SCH23390 -47 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3745 52 3H-SCH23390 -47 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3745 52 3H-SCH23390 -47 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3745 52 3H-SCH23390 -47 55 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
681 1437 65 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1437 65 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1437 65 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1437 65 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1437 65 None -154 38 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
242 467 117 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 467 117 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 467 117 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 467 117 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 467 117 None -74 51 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometryDisplacement of [3H]SCH23390 from dopamine D1 receptor in CRL:CD(SD)BR-COBS rat striatum by scintillation spectrometry
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
37459 735 10 3H-SCH23390 -21 24 Rhesus macaque 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
62 735 10 3H-SCH23390 -21 24 Rhesus macaque 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
CHEMBL8514 735 10 3H-SCH23390 -21 24 Rhesus macaque 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C None
2865 4079 67 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4079 67 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4079 67 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4079 67 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4079 67 UNDEFINED -114 53 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
6603820 95330 13 3H-SCH23390 1 13 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
CHEMBL25856 95330 13 3H-SCH23390 1 13 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2 None
2726 906 64 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 3H-dopamine -186 72 Bovine 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
6852400 214160 0 3H-SCH23390 -22387 21 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
73759726 214160 0 3H-SCH23390 -22387 21 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 361 0 1 2 4.8 CC(C)(C)C1(CCN2CC3C4=CC=CC=C4CCC5=C3C(=CC=C5)C2C1)O None
None 214366 0 3H-KETANSERIN -8912 23 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
5281878 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
5281881 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
948 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
968 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL42055 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL54661 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00875 1630 33 3H-SCH23390 -11 16 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
1353 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1880 85 3H-dopamine -512 85 Bovine 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
None 214991 0 UNDEFINED - 1 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 311 2 3 4 3.3 CCCN1CCC2=C3C1CC4=C(C3=CC(=C2)O)C(=C(C=C4)O)O None
24949535 180977 0 UNDEFINED -1122 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 None
CHEMBL476722 180977 0 UNDEFINED -1122 3 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 425 10 0 6 5.3 COc1ccccc1N1CCN(CCCCCCSc2nc3ccccc3o2)CC1 None
5074 3280 75 3H-SCH23390 -1737 29 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3280 75 3H-SCH23390 -1737 29 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3280 75 3H-SCH23390 -1737 29 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3280 75 3H-SCH23390 -1737 29 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
None 215630 0 UNDEFINED - 1 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 423 3 3 4 5.4 CCCN1CCC2=CC(=CC3=C2C1CC4=C3C(=C(C=C4)O)O)C5=CC=C(C=C5)O.Cl None
2726 906 64 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 906 64 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 906 64 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 906 64 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 906 64 UNDEFINED -36 72 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
5 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 66 3H-SCH23390 -23442 54 Human 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1242 3556 23 3H-SCH23390 -5 17 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
935 3556 23 3H-SCH23390 -5 17 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
CHEMBL286080 3556 23 3H-SCH23390 -5 17 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 None
5281878 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
5281878 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
5281881 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
5281881 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
948 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
948 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
968 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
968 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
CHEMBL42055 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL42055 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
CHEMBL54661 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL54661 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
DB00875 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
DB00875 1630 33 None -2 16 Human 7.7 pKi = 7.7 Binding
Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.Note that this assay uses the <i>cis</i> form of the compound, whereas the approved drug is a racemic mixture of <i>cis</i> and <i>trans</i> molecules.
Guide to Pharmacology 434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F 7525564
681 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
681 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
940 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
940 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
947 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
947 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
CHEMBL59 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
CHEMBL59 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
DB00988 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 1826762
DB00988 1437 65 None -154 38 Human 5.0 pKi = 5.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 7525564
5 139 66 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
5202 139 66 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
CHEMBL39 139 66 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
DB08839 139 66 None -23442 54 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1826762
1153 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
12668023 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026874 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026875 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
3341 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
6603851 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
933 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
939 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
985 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1160786 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1161520 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL588 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
DB00800 1598 53 None -32 10 Human 5.7 pKi = 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
1242 3556 23 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
1242 3556 23 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
935 3556 23 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
935 3556 23 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
CHEMBL286080 3556 23 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 1826762
CHEMBL286080 3556 23 None -5 17 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1 7525564
1712 2456 0 None -6 21 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
4078 2456 0 None -6 21 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
7227 2456 0 None -6 21 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
CHEMBL1088 2456 0 None -6 21 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
DB00933 2456 0 None -6 21 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 15357957
2274 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3124 53 None -16 32 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1153 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
12668023 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
30026874 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
30026875 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
3341 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
6603851 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
933 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
939 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
985 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
CHEMBL1160786 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
CHEMBL1161520 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
CHEMBL588 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
DB00800 1598 53 None -32 10 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 7525564
1153 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
12668023 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026874 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
30026875 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
3341 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
6603851 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
933 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
939 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
985 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1160786 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL1161520 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
CHEMBL588 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
DB00800 1598 53 None -32 10 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 1826762
1353 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
1353 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
3559 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
3559 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
86 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
86 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
CHEMBL54 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
CHEMBL54 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
DB00502 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 1826762
DB00502 1880 85 None -38 85 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 18308814
5311070 1389 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
9267 1389 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
CHEMBL4280145 1389 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
DB12890 1389 0 None - 1 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 3 3 2.6 Oc1cc2CC[C@H]3[C@H](c2cc1O)c1ccccc1CN3 2572425
2107 3006 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
4747 3006 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
9216 3006 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
CHEMBL251940 3006 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
DB01608 3006 0 None - 1 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 7918347
107930 1500 20 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
3304 1500 20 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
CHEMBL298406 1500 20 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
DB12273 1500 20 None 1 6 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O 7862709
5018 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
5018 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
943 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
943 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
946 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
946 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
CHEMBL13668 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 1826762
CHEMBL13668 3493 8 None 2 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O 7525564
1218 3559 24 None 11 7 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 1973652
938 3559 24 None 11 7 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 1973652
CHEMBL353335 3559 24 None 11 7 Rat 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 1973652
6603703 206 7 None -1 5 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 17067639
9637 206 7 None -1 5 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 17067639
CHEMBL291143 206 7 None -1 5 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3 17067639
1243 3561 26 None 3 5 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
944 3561 26 None 3 5 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
CHEMBL324017 3561 26 None 3 5 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 1 1 2 3.8 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Br)O 1826762
2995 202700 49 None -23 22 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 202700 49 None -23 22 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 202700 49 None -23 22 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
5770 203349 80 None -2 6 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
CHEMBL772 203349 80 None -2 6 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 608 8 1 10 4.2 COC(=O)[C@H]1[C@H]2C[C@@H]3c4[nH]c5cc(OC)ccc5c4CCN3C[C@H]2C[C@@H](OC(=O)c2cc(OC)c(OC)c(OC)c2)[C@@H]1OC None
213 3792 50 None -7 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3792 50 None -7 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3792 50 None -7 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3792 50 None -7 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3792 50 None -7 43 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2601 3721 30 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3721 30 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3721 30 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3721 30 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3721 30 None -16 21 Human 8.1 pKi None 8.1 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
484 2814 45 None -223 35 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
951 2814 45 None -223 35 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
CHEMBL432 2814 45 None -223 35 Human 4.3 pKi None 4.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O 1826762
2407 3320 73 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
59227 3320 73 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
941 3320 73 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
CHEMBL1303 3320 73 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
DB05271 3320 73 None -128 7 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 1826762
228 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
228 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
33 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
33 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
6005 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
6005 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
CHEMBL53 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
CHEMBL53 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
DB00714 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 1826762
DB00714 441 26 None -35 24 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 7525564
3153 294 24 None -831 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 12388666
3153 294 24 None -831 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
932 294 24 None -831 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 12388666
932 294 24 None -831 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
CHEMBL26736 294 24 None -831 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 12388666
CHEMBL26736 294 24 None -831 7 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 179 0 3 3 0.9 NC1CCc2c(C1)cc(c(c2)O)O 1826762
2105 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2105 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
47811 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
48 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
CHEMBL531 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
DB01186 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 3005 34 None -537 33 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 1826762
31101 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
31101 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
35 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
403 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
CHEMBL493 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
DB01200 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 720 39 None -436 35 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 1826762
937 3558 0 None -1 2 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1826762
37 766 56 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 766 56 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 766 56 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 766 56 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 766 56 None -14 17 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
1524 2150 89 None -75 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
197 2150 89 None -75 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
3822 2150 89 None -75 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
88 2150 89 None -75 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
CHEMBL51 2150 89 None -75 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
DB12465 2150 89 None -75 51 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1826762
2470 3596 46 None -4168 59 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
3300 3596 46 None -4168 59 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
5265 3596 46 None -4168 59 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
99 3596 46 None -4168 59 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
CHEMBL267930 3596 46 None -4168 59 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1826762
135398737 944 89 None -44 91 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
38 944 89 None -44 91 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
722 944 89 None -44 91 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
CHEMBL42 944 89 None -44 91 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
DB00363 944 89 None -44 91 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 1826762
100 3745 52 None -47 55 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
2637 3745 52 None -47 55 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
5452 3745 52 None -47 55 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
CHEMBL479 3745 52 None -47 55 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
DB00679 3745 52 None -47 55 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 1826762
2726 906 64 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
621 906 64 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
83 906 64 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
CHEMBL71 906 64 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
DB00477 906 64 None -36 72 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 1826762
1588 2294 24 None -190 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 2294 24 None -190 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 2294 24 None -190 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 2294 24 None -190 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 2294 24 None -190 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
30137 2833 0 None -676 10 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
8594 2833 0 None -676 10 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
934 2833 0 None -676 10 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 2 2 3 3.6 CCCN1CCc2c3C1Cc1ccc(c(c1c3ccc2)O)O 1826762
37459 735 10 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
37459 735 10 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 7525564
62 735 10 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
62 735 10 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 7525564
CHEMBL8514 735 10 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 1826762
CHEMBL8514 735 10 None -10 24 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 361 0 1 2 4.8 O[C@]1(CCN2[C@@H](C1)c1cccc3c1[C@@H](C2)c1ccccc1CC3)C(C)(C)C 7525564
1212 1632 45 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
204 1632 45 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
3372 1632 45 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
CHEMBL726 1632 45 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
DB00623 1632 45 None -51 65 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 1826762
173871 3557 1 None 4 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 1973652
936 3557 1 None 4 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 1973652
CHEMBL1193571 3557 1 None 4 3 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O 1973652