Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL1196161 drd1_human Human Yes 9.9 EC50 = 0.1 nM Funct
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
343 3 2 3 4.2 CC1=CC(=CC=C1)C2CN(CCC3=C(C(=C(C=C23)O)O)Cl)CC=C
CHEMBL574558 drd1_human Human Yes 9.7 EC50 = 0.2 nM Funct
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
317 1 2 3 3.7 CN1CCc2c(C(C1)c1cccc(c1)C)cc(c(c2Cl)O)O
CHEMBL4465393 drd1_human Human No 9.6 EC50 = 0.2 nM Funct
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
372 3 0 6 5.4 CC1=C(C=CC(=C1)OC2=NC=CC3=C2SC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4465393 drd1_human Human No 9.6 EC50 = 0.2 nM Funct
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
372 3 0 6 5.4 CC1=C(C=CC(=C1)OC2=NC=CC3=C2SC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4277264 drd1_human Human Yes 9.6 EC50 = 0.2 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4277264 drd1_human Human Yes 9.6 EC50 = 0.3 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4472022 drd1_human Human No 9.5 EC50 = 0.3 nM Funct
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
303 1 2 3 3.4 CN1CCC2=C(C(=C(C=C2[C@H](C1)C3=CC=CC=C3)O)O)Cl
CHEMBL4453318 drd1_human Human Yes 9.5 EC50 = 0.3 nM Funct
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
363 3 1 6 3.3 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(C(=O)NC(=O)N4C)C
CHEMBL4437552 drd1_human Human No 9.4 EC50 = 0.4 nM Bind
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
379 3 0 5 3.9 CCC1=C(C(=C2C(=C1)C[C@@H]3C4=C(CCN3C)C=CC=C42)OC(=O)C)OC(=O)C
CHEMBL4437552 drd1_human Human No 9.4 EC50 = 0.4 nM Bind
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
379 3 0 5 3.9 CCC1=C(C(=C2C(=C1)C[C@@H]3C4=C(CCN3C)C=CC=C42)OC(=O)C)OC(=O)C
CHEMBL1193571 drd1_human Human Yes 9.4 EC50 = 0.5 nM Funct
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
269 1 2 3 2.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)O)O
CHEMBL1224527 drd1_human Human No 9.2 EC50 = 0.6 nM Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
295 1 3 3 3.1 Oc1ccc2c(c1O)C[C@@H](c1ccccc1)[C@@H]1CCNC[C@@H]21
CHEMBL35354 drd1_human Human Yes 9.1 EC50 = 0.7 nM Funct
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
329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O
CHEMBL4589737 drd1_human Human No 9.1 EC50 = 0.8 nM Bind
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
309 2 0 3 3.8 CC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4589737 drd1_human Human No 9.1 EC50 = 0.8 nM Bind
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
309 2 0 3 3.8 CC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4467080 drd1_human Human No 9.1 EC50 = 0.9 nM Funct
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
355 3 0 6 4.5 CC1=C(C=CC(=C1)OC2=NC=CN3C2=CC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4467080 drd1_human Human No 9.1 EC50 = 0.9 nM Funct
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
355 3 0 6 4.5 CC1=C(C=CC(=C1)OC2=NC=CN3C2=CC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL288090 drd1_human Human Yes 9.0 EC50 = 1 nM Funct
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
295 3 2 3 3.3 C=CCN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O
CHEMBL415080 drd1_human Human No 9.0 EC50 = 1.0 nM Funct
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
349 2 3 4 3.2 NC[C@@H]1OC(c2ccc(Br)cc2)Cc2c1ccc(O)c2O
CHEMBL225230 drd1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL225230 drd1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL286080 drd1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL3421729 drd1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C
CHEMBL441343 drd1_human Human Yes 9.0 EC50 = 1.1 nM Funct
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
138 1 2 2 1.1 O=C(O)c1ccc(O)cc1
CHEMBL4437012 drd1_human Human No 8.9 EC50 = 1.2 nM Funct
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
331 3 0 5 5.0 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=NC=C4C)C
CHEMBL4437012 drd1_human Human No 8.9 EC50 = 1.2 nM Funct
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
331 3 0 5 5.0 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=NC=C4C)C
CHEMBL4450338 drd1_human Human No 8.9 EC50 = 1.3 nM Funct
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
357 3 1 7 4.2 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL4450338 drd1_human Human No 8.9 EC50 = 1.3 nM Funct
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
357 3 1 7 4.2 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL315750 drd1_human Human No 8.9 EC50 = 1.3 nM Funct
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
291 3 3 4 2.9 CNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL4572614 drd1_human Human No 8.8 EC50 = 1.7 nM Funct
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
410 3 0 6 5.7 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL314459 drd1_rat Rat No 8.8 EC50 = 1.7 nM Funct
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
277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL4572614 drd1_human Human No 8.8 EC50 = 1.7 nM Funct
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
410 3 0 6 5.7 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL4593703 drd1_human Human No 8.8 EC50 = 1.7 nM Funct
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
356 3 1 6 4.1 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=NN3)C4=C(N=CC5=NC=CN54)C
CHEMBL4593703 drd1_human Human No 8.7 EC50 = 1.8 nM Funct
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
356 3 1 6 4.1 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=NN3)C4=C(N=CC5=NC=CN54)C
CHEMBL86931 drd1_human Human Yes 8.7 EC50 = 2.0 nM Funct
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
271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1
CHEMBL86931 drd1_rat Rat Yes 8.7 EC50 = 2.0 nM Funct
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
271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1
CHEMBL86931 drd1_human Human Yes 8.7 EC50 = 2.0 nM Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1
CHEMBL4548284 drd1_human Human Yes 8.0 EC50 = 10 nM Funct
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
342 3 1 6 4.5 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL4469983 drd1_human Human No 8.0 EC50 = 10 nM Funct
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
351 3 1 5 4.1 CC1=C(C(=NNC1=O)C)C2=C(C=C(C=C2)OC3=NC=CC4=C3C=CO4)F
CHEMBL2397383 drd1_human Human No 8.0 EC50 = 10.5 nM Funct
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
373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL3040217 drd1_human Human No 8.0 EC50 = 10.5 nM Funct
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
373 2 3 4 4.1 CN1CCc2ccc(Cc3ccc(O)cc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL59 drd1_human Human Yes 7.0 EC50 = 100 nM Bind
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL35426 drd1_human Human No 7.0 EC50 = 100 nM Funct
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
279 0 0 3 3.2 CN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C5=C(C=C4)OCO5
CHEMBL4457872 drd1_human Human No 7.0 EC50 = 100 nM Funct
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
397 4 0 6 5.7 CC1=C(C=CC(=C1)N(C2=NC=CC3=C2C=CO3)C(C)C)C4=C(N=CC5=NC=CN54)C
CHEMBL87172 drd1_human Human No 7.0 EC50 = 100 nM Funct
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
361 4 3 4 3.9 NC[C@@H]1OC(C(c2ccccc2)c2ccccc2)Cc2c1ccc(O)c2O
CHEMBL1180542 drd1_rat Rat No 7.0 EC50 = 100 nM Funct
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
329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1
CHEMBL129634 drd1_rat Rat No 7.0 EC50 = 100 nM Funct
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
329 3 3 4 3.1 C=CCN1CCc2c(cc(O)c(O)c2F)C(c2ccc(O)cc2)C1
CHEMBL1467585 drd1_rat Rat Yes 7.0 EC50 = 100 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL24077 drd1_rat Rat Yes 7.0 EC50 = 100 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL503958 drd1_rat Rat Yes 7.0 EC50 = 100 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL4437975 drd1_human Human No 6.0 EC50 = 1000 nM Funct
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
399 4 0 7 5.0 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CN=C5N4C=CC=C5C(=O)OC
CHEMBL101617 drd1_rat Rat No 6.0 EC50 = 1000 nM Funct
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
269 3 3 3 2.7 Oc1ccc2c(c1O)CCC(NCc1ccccc1)C2
CHEMBL43345 drd1_rat Rat No 5.0 EC50 = 10000 nM Funct
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
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL4437975 drd1_human Human No 6.0 EC50 = 1023.3 nM Funct
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
399 4 0 7 5.0 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CN=C5N4C=CC=C5C(=O)OC
CHEMBL4457872 drd1_human Human No 7.0 EC50 = 104.7 nM Funct
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
397 4 0 6 5.7 CC1=C(C=CC(=C1)N(C2=NC=CC3=C2C=CO3)C(C)C)C4=C(N=CC5=NC=CN54)C
CHEMBL4277264 drd1_human Human Yes 7.0 EC50 = 106 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4466769 drd1_human Human No 7.0 EC50 = 109.7 nM Funct
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
355 3 0 5 5.6 CC1=C(C=CC(=C1C)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL41132 drd1_carau Goldfish No 8.0 EC50 = 11 nM Funct
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
287 0 3 4 3.0 Cc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2
CHEMBL2335737 drd1_human Human No 8.0 EC50 = 11 nM Funct
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
343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2
CHEMBL4277264 drd1_human Human Yes 8.0 EC50 = 11 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4277264 drd1_human Human Yes 7.0 EC50 = 110 nM Bind
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4466769 drd1_human Human No 7.0 EC50 = 110 nM Funct
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
355 3 0 5 5.6 CC1=C(C=CC(=C1C)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL275379 drd1_human Human No 7.0 EC50 = 110 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
282 0 3 4 2.4 Cc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2
CHEMBL1203924 drd1_human Human No 6.0 EC50 = 1100 nM Funct
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
311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21
CHEMBL216945 drd1_human Human No 6.0 EC50 = 1100 nM Funct
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
311 2 2 4 3.2 CCCN1Cc2ccccc2C2c3cc(O)c(O)cc3OCC21
CHEMBL384046 drd1_human Human No 6.0 EC50 = 1100 nM Funct
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
269 0 3 4 2.1 Oc1cc2c(cc1O)[C@@H]1c3ccccc3CN[C@H]1CO2
CHEMBL4591207 drd1_human Human No 6.0 EC50 = 1100 nM Bind
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
331 3 1 5 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC(=C4)N)C
CHEMBL4556763 drd1_human Human No 6.0 EC50 = 1100 nM Funct
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
423 4 0 6 6.2 CC1=C(C=CC(=C1)N(C2CCCC2)C3=NC=CC4=C3C=CO4)C5=C(N=CC6=NC=CN65)C
CHEMBL4437012 drd1_human Human No 6.0 EC50 = 1100 nM Bind
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
331 3 0 5 5.0 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=NC=C4C)C
CHEMBL4283176 drd1_human Human No 6.0 EC50 = 1108 nM Funct
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
347 3 0 5 5.5 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C(C)(C)C
CHEMBL4449550 drd1_human Human No 7.0 EC50 = 112 nM Funct
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
413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1cc(F)ccc1Cl
CHEMBL35426 drd1_human Human No 7.0 EC50 = 112.2 nM Funct
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
279 0 0 3 3.2 CN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C5=C(C=C4)OCO5
CHEMBL4591207 drd1_human Human No 6.0 EC50 = 1122.0 nM Bind
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
331 3 1 5 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC(=C4)N)C
CHEMBL4277264 drd1_human Human Yes 6.9 EC50 = 114.8 nM Bind
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4289538 drd1_human Human No 5.9 EC50 = 1141 nM Funct
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
342 3 0 6 4.7 Cc1nc2cnccc2n1-c1ccc(Oc2nccc3occc23)cc1
CHEMBL4556763 drd1_human Human No 5.9 EC50 = 1148.2 nM Funct
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
423 4 0 6 6.2 CC1=C(C=CC(=C1)N(C2CCCC2)C3=NC=CC4=C3C=CO4)C5=C(N=CC6=NC=CN65)C
CHEMBL2397382 drd1_human Human No 6.9 EC50 = 117 nM Funct
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
297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL3040156 drd1_human Human No 6.9 EC50 = 117 nM Funct
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
297 1 3 4 2.3 CN1CCc2ccc(CO)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL4755709 drd1_human Human No 6.9 EC50 = 117 nM Funct
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)
435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL4756486 drd1_human Human Yes 5.9 EC50 = 1190 nM Bind
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)
419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21
CHEMBL4474245 drd1_human Human No 7.9 EC50 = 12 nM Funct
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
361 5 0 6 5.1 CCOC1=NC=NC(=C1C2=C(C=C(C=C2)OC3=NC=CC4=C3C=CO4)C)C
CHEMBL4474245 drd1_human Human No 7.9 EC50 = 12.3 nM Funct
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
361 5 0 6 5.1 CCOC1=NC=NC(=C1C2=C(C=C(C=C2)OC3=NC=CC4=C3C=CO4)C)C
CHEMBL420788 drd1_human Human No 7.9 EC50 = 12.5 nM Funct
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
315 4 3 4 2.9 C#CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL3421729 drd1_human Human Yes 7.9 EC50 = 12.8 nM Funct
Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 60 mins by HTRF assay
449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C
CHEMBL4591207 drd1_human Human No 7.9 EC50 = 12.9 nM Funct
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
331 3 1 5 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC(=C4)N)C
CHEMBL59 drd1_human Human Yes 6.9 EC50 = 120 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL3099225 drd1_human Human No 6.9 EC50 = 120 nM Funct
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
233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3139011 drd1_human Human No 6.9 EC50 = 120 nM Funct
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
233 1 1 3 1.6 CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4541632 drd1_human Human No 6.9 EC50 = 120 nM Funct
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
316 3 0 5 4.2 CC1=C(C=CC(=C1)OC2=CC=CC=N2)C3=C(N=CC4=NC=CN43)C
CHEMBL284959 drd1_human Human No 6.9 EC50 = 120 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
296 0 3 4 2.7 Cc1cc2c(nc1C)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL4754602 drd1_human Human No 6.9 EC50 = 122 nM Funct
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)
401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4286177 drd1_human Human No 6.9 EC50 = 123 nM Funct
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
341 3 0 5 5.2 Cc1ccc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1
CHEMBL1311333 drd1_human Human Yes 6.9 EC50 = 123 nM Funct
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)
385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21
CHEMBL4541632 drd1_human Human No 6.9 EC50 = 123.0 nM Funct
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
316 3 0 5 4.2 CC1=C(C=CC(=C1)OC2=CC=CC=N2)C3=C(N=CC4=NC=CN43)C
CHEMBL4293356 drd1_human Human No 5.9 EC50 = 1232 nM Funct
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
305 3 0 5 4.3 Cc1cc(Oc2nccc3occc23)ccc1-c1ccnn1C
CHEMBL86669 drd1_human Human No 6.9 EC50 = 124 nM Funct
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
317 4 3 4 3.4 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNC1CC1
CHEMBL287931 drd1_carau Goldfish No 6.9 EC50 = 125 nM Funct
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
355 2 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3sc(CC4CCCC4)cc3CN[C@H]1CC2
CHEMBL15564 drd1_rat Rat Yes 4.9 EC50 = 12500 nM Funct
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
237 7 2 3 2.8 CCCN(CCC)CCc1ccc(O)c(O)c1
CHEMBL4590150 drd1_human Human No 6.9 EC50 = 127 nM Funct
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
397 4 2 3 3.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1F
CHEMBL4591207 drd1_human Human No 7.9 EC50 = 13 nM Funct
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
331 3 1 5 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC(=C4)N)C
CHEMBL1160787 drd1_human Human Yes 7.9 EC50 = 13.2 nM Bind
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
289 1 3 3 3.0 C1CNC[C@@H](C2=CC(=C(C(=C21)Cl)O)O)C3=CC=CC=C3
CHEMBL4464150 drd1_human Human No 7.9 EC50 = 13.4 nM Funct
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
429 4 2 3 4.4 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL420972 drd1_human Human No 7.9 EC50 = 13.6 nM Funct
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
279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL3421730 drd1_human Human No 7.9 EC50 = 13.9 nM Funct
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
421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL286080 drd1_human Human Yes 6.9 EC50 = 130 nM Funct
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
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL4574454 drd1_human Human No 5.9 EC50 = 1300 nM Funct
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
345 4 1 5 4.1 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC(=CN=C4)C(=O)N
CHEMBL4574454 drd1_human Human No 5.9 EC50 = 1318.3 nM Funct
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
345 4 1 5 4.1 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC(=CN=C4)C(=O)N
CHEMBL4286110 drd1_human Human No 5.9 EC50 = 1333 nM Funct
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
368 4 0 5 5.8 COc1ccc2cnccc2c1-c1ccc(Oc2nccc3occc23)cc1
CHEMBL448891 drd1_human Human Yes 5.9 EC50 = 1350 nM Funct
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
341 3 1 5 3.1 COc1cc2c(cc1OC)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2
CHEMBL4755481 drd1_human Human No 6.9 EC50 = 137 nM Funct
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)
405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21
CHEMBL25856 drd1_human Human Yes 7.9 EC50 = 14 nM Bind
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
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL25856 drd1_human Human Yes 7.9 EC50 = 14 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL4523054 drd1_human Human No 7.8 EC50 = 14.5 nM Bind
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
365 2 0 5 3.6 CC1=CC2=C(C3=CC=CC4=C3[C@@H](C2)N(CC4)C)C(=C1OC(=O)C)OC(=O)C
CHEMBL4577432 drd1_human Human No 7.8 EC50 = 14.5 nM Funct
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
366 3 0 5 5.4 CC1=C(C=CC(=C1)OC2=NC=CC3=CC=CC=C32)C4=C(N=CC5=NC=CN54)C
CHEMBL289927 drd1_carau Goldfish No 6.9 EC50 = 140 nM Funct
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
357 5 3 4 4.8 CCCCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2
CHEMBL4460394 drd1_human Human No 6.9 EC50 = 140 nM Funct
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
378 3 0 6 4.9 CC1=C(N2C=CN=C2C=N1)C3=CC(=C(C(=C3)F)OC4=NC=CC5=C4C=CO5)F
CHEMBL59 drd1_human Human Yes 5.9 EC50 = 1400 nM Bind
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4740497 drd1_human Human No 5.9 EC50 = 1400 nM Bind
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)
413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4277264 drd1_human Human Yes 6.9 EC50 = 141 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4460394 drd1_human Human No 6.9 EC50 = 141.3 nM Funct
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
378 3 0 6 4.9 CC1=C(N2C=CN=C2C=N1)C3=CC(=C(C(=C3)F)OC4=NC=CC5=C4C=CO5)F
CHEMBL2115213 drd1_human Human No 6.9 EC50 = 142 nM Funct
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
223 2 3 4 1.4 CC[C@@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL4577432 drd1_human Human No 7.8 EC50 = 15 nM Funct
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
366 3 0 5 5.4 CC1=C(C=CC(=C1)OC2=NC=CC3=CC=CC=C32)C4=C(N=CC5=NC=CN54)C
CHEMBL130795 drd1_rat Rat Yes 7.8 EC50 = 15 nM Funct
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
345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1
CHEMBL368456 drd1_rat Rat Yes 7.8 EC50 = 15 nM Funct
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
345 3 3 4 3.6 C=CCN1CCc2c(cc(O)c(O)c2Cl)C(c2ccc(O)cc2)C1
CHEMBL4475848 drd1_human Human No 7.8 EC50 = 15.5 nM Funct
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
355 3 1 6 4.9 CC1=C(C=CC(=C1)NC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL3099234 drd1_human Human No 6.8 EC50 = 150 nM Funct
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
328 4 1 6 1.6 CCCN1C[C@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3099226 drd1_human Human No 6.8 EC50 = 150 nM Funct
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
247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3139040 drd1_human Human No 6.8 EC50 = 150 nM Funct
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
247 2 1 3 2.0 CCCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4754602 drd1_human Human No 6.8 EC50 = 150 nM Bind
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)
401 3 0 6 3.9 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4756163 drd1_human Human No 6.8 EC50 = 150 nM Bind
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)
389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4759339 drd1_human Human No 6.8 EC50 = 150 nM Funct
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)
385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4779641 drd1_human Human No 6.8 EC50 = 150 nM Funct
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)
393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1
CHEMBL4579687 drd1_human Human No 6.8 EC50 = 150.2 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C(C=CC3=C2[C@H]1CC4=C3C(=C(C=C4)OC)OC)Br
CHEMBL4787728 drd1_human Human No 5.8 EC50 = 1500 nM Bind
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)
433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21
CHEMBL4796761 drd1_human Human No 5.8 EC50 = 1500 nM Bind
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)
433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21
CHEMBL4579687 drd1_human Human No 6.8 EC50 = 151.4 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C(C=CC3=C2[C@H]1CC4=C3C(=C(C=C4)OC)OC)Br
CHEMBL4278861 drd1_human Human Yes 6.8 EC50 = 153 nM Funct
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
356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21
CHEMBL4437552 drd1_human Human No 5.8 EC50 = 1548 nM Funct
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
379 3 0 5 3.9 CCC1=C(C(=C2C(=C1)C[C@@H]3C4=C(CCN3C)C=CC=C42)OC(=O)C)OC(=O)C
CHEMBL4523054 drd1_human Human No 5.8 EC50 = 1548.8 nM Funct
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
365 2 0 5 3.6 CC1=CC2=C(C3=CC=CC4=C3[C@@H](C2)N(CC4)C)C(=C1OC(=O)C)OC(=O)C
CHEMBL4437552 drd1_human Human No 5.8 EC50 = 1548.8 nM Funct
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
379 3 0 5 3.9 CCC1=C(C(=C2C(=C1)C[C@@H]3C4=C(CCN3C)C=CC=C42)OC(=O)C)OC(=O)C
CHEMBL4523054 drd1_human Human No 5.8 EC50 = 1555 nM Funct
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
365 2 0 5 3.6 CC1=CC2=C(C3=CC=CC4=C3[C@@H](C2)N(CC4)C)C(=C1OC(=O)C)OC(=O)C
CHEMBL4789255 drd1_human Human No 6.8 EC50 = 158 nM Funct
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)
419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21
CHEMBL1457510 drd1_human Human Yes 4.8 EC50 = 15970 nM Funct
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
325 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCO4
CHEMBL4475848 drd1_human Human No 7.8 EC50 = 16 nM Funct
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
355 3 1 6 4.9 CC1=C(C=CC(=C1)NC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL82899 drd1_human Human No 7.8 EC50 = 16.4 nM Funct
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
251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL4468760 drd1_human Human No 7.8 EC50 = 16.4 nM Funct
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
443 4 1 4 4.4 C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL1191276 drd1_carau Goldfish No 6.8 EC50 = 160 nM Funct
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
315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL542351 drd1_carau Goldfish No 6.8 EC50 = 160 nM Funct
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
315 2 3 4 3.7 CCCc1csc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL4570859 drd1_human Human No 6.8 EC50 = 160 nM Funct
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
346 3 1 5 3.8 CC1=C(C=CC(=C1)OC2=C(C(=O)C=CN2)C)C3=C(N=CC4=NC=CN43)C
CHEMBL4744261 drd1_human Human No 6.8 EC50 = 160 nM Bind
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)
405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21
CHEMBL4754761 drd1_human Human No 5.8 EC50 = 1600 nM Bind
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)
399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21
CHEMBL3421730 drd1_rat Rat No 6.8 EC50 = 162 nM Funct
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
421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL4570859 drd1_human Human No 6.8 EC50 = 162.2 nM Funct
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
346 3 1 5 3.8 CC1=C(C=CC(=C1)OC2=C(C(=O)C=CN2)C)C3=C(N=CC4=NC=CN43)C
CHEMBL4762375 drd1_human Human No 6.8 EC50 = 163 nM Funct
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)
399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4796389 drd1_human Human No 6.8 EC50 = 163 nM Funct
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)
343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21
CHEMBL4519818 drd1_human Human No 6.8 EC50 = 165 nM Bind
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
333 2 0 1 4.7 C[C@H]1c2ccccc2CCN1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL4744261 drd1_human Human No 6.8 EC50 = 167 nM Funct
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)
405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCC3)nc21
CHEMBL4277264 drd1_human Human Yes 7.8 EC50 = 17 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL38757 drd1_carau Goldfish No 6.8 EC50 = 170 nM Funct
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
343 4 3 4 4.4 CCCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL39266 drd1_carau Goldfish No 6.8 EC50 = 170 nM Funct
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
307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3cc(Cl)sc3CN[C@H]1CC2
CHEMBL286080 drd1_human Human Yes 6.8 EC50 = 170 nM Funct
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
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL4740312 drd1_human Human No 6.8 EC50 = 170 nM Funct
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)
295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21
CHEMBL2115374 drd1_human Human No 5.8 EC50 = 1700 nM Bind
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL39230 drd1_human Human No 5.8 EC50 = 1700 nM Bind
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL544814 drd1_human Human No 5.8 EC50 = 1700 nM Bind
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4573538 drd1_human Human No 6.8 EC50 = 172 nM Funct
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
457 5 1 4 4.9 CCn1cc(-c2cccc3c2C[C@H](CO)N(C(=O)Cc2c(Cl)cccc2Cl)[C@H]3C)cn1
CHEMBL85552 drd1_human Human No 5.8 EC50 = 1740 nM Funct
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
335 6 4 5 2.6 OCCCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL2115373 drd1_carau Goldfish No 5.8 EC50 = 1750 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL290438 drd1_carau Goldfish No 5.8 EC50 = 1750 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4294397 drd1_human Human No 6.8 EC50 = 177.8 nM Bind
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL27101 drd1_human Human No 7.8 EC50 = 18 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3ccc(F)nc3CN[C@@H]1CC2
CHEMBL4536851 drd1_human Human No 7.7 EC50 = 18.3 nM Funct
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
473 6 2 5 3.9 C[C@H]1c2cccc(-c3cnn(CCO)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL84983 drd1_rat Rat No 7.7 EC50 = 18.9 nM Funct
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
299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O
CHEMBL286080 drd1_human Human Yes 6.8 EC50 = 180 nM Funct
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
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL4294397 drd1_human Human No 6.8 EC50 = 180 nM Bind
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL4546823 drd1_human Human No 6.8 EC50 = 180 nM Funct
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
395 3 0 6 4.9 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CN5C4=NC=C5)C(F)(F)F
CHEMBL4760355 drd1_human Human No 6.8 EC50 = 180 nM Bind
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)
359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1
CHEMBL283247 drd1_human Human No 6.8 EC50 = 180 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
324 3 3 4 3.4 CCCCc1cnc2c(c1)[C@@H]1c3cc(O)c(O)cc3CC[C@H]1NC2
CHEMBL4759814 drd1_human Human No 5.8 EC50 = 1800 nM Bind
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)
463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL4546823 drd1_human Human No 6.7 EC50 = 182.0 nM Funct
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
395 3 0 6 4.9 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CN5C4=NC=C5)C(F)(F)F
CHEMBL4740678 drd1_human Human No 6.7 EC50 = 185 nM Funct
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)
415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4790909 drd1_human Human No 6.7 EC50 = 185 nM Funct
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)
373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL225230 drd1_human Human Yes 5.7 EC50 = 1862.1 nM Bind
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
295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL4465320 drd1_human Human No 5.7 EC50 = 1870 nM Bind
Positive allosteric modulation of D1R (unknown origin) by HTS assayPositive allosteric modulation of D1R (unknown origin) by HTS assay
340 1 1 2 5.2 CC1c2ccsc2CCN1C(=O)Nc1c(Cl)cccc1Cl
CHEMBL225230 drd1_human Human Yes 5.7 EC50 = 1884 nM Bind
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
295 2 2 3 3.6 CCCN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL25856 drd1_human Human Yes 7.7 EC50 = 19 nM Funct
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
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL3099222 drd1_human Human No 7.7 EC50 = 19 nM Funct
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
307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3139044 drd1_human Human No 7.7 EC50 = 19 nM Funct
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
307 4 1 4 2.7 CCCN1C[C@H](CSC)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4474567 drd1_human Human No 6.7 EC50 = 190 nM Funct
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
363 3 0 5 5.2 C1=CC2=NC=CN2C(=C1)C3=CC(=C(C(=C3)F)OC4=NC=CC5=C4C=CO5)F
CHEMBL4581262 drd1_human Human No 6.7 EC50 = 194.3 nM Funct
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
385 2 0 5 3.9 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)Cl
CHEMBL4581262 drd1_human Human No 6.7 EC50 = 195.0 nM Funct
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
385 2 0 5 3.9 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)Cl
CHEMBL4474567 drd1_human Human No 6.7 EC50 = 195.0 nM Funct
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
363 3 0 5 5.2 C1=CC2=NC=CN2C(=C1)C3=CC(=C(C(=C3)F)OC4=NC=CC5=C4C=CO5)F
CHEMBL4470553 drd1_human Human Yes 5.7 EC50 = 1949 nM Bind
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
307 2 0 3 3.9 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C5=C(C=C4)OCO5
CHEMBL4470553 drd1_human Human Yes 5.7 EC50 = 1949.8 nM Bind
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
307 2 0 3 3.9 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C5=C(C=C4)OCO5
CHEMBL4754761 drd1_human Human No 6.7 EC50 = 196 nM Funct
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)
399 3 0 5 4.4 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(CC3CCCCC3)nc21
CHEMBL4764398 drd1_human Human No 6.7 EC50 = 199 nM Funct
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)
449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL35354 drd1_human Human Yes 8.7 EC50 = 2 nM Bind
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
329 3 2 3 3.9 C=CCN1CCc2c(C(C1)c1ccccc1)cc(c(c2Cl)O)O
CHEMBL1160787 drd1_human Human Yes 8.7 EC50 = 2 nM Funct
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
289 1 3 3 3.0 C1CNC[C@@H](C2=CC(=C(C(=C21)Cl)O)O)C3=CC=CC=C3
CHEMBL313304 drd1_human Human No 8.7 EC50 = 2.0 nM Funct
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
397 2 3 4 3.0 NC[C@@H]1OC(c2ccc(I)cc2)Cc2c1ccc(O)c2O
CHEMBL315468 drd1_human Human No 8.7 EC50 = 2.1 nM Funct
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
271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O
CHEMBL86931 drd1_human Human Yes 8.7 EC50 = 2.1 nM Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
271 2 3 4 2.4 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)c1ccccc1
CHEMBL4466483 drd1_human Human No 8.7 EC50 = 2.2 nM Funct
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
411 3 0 5 6.4 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4SC=C5)C(F)(F)F
CHEMBL4466483 drd1_human Human No 8.7 EC50 = 2.2 nM Funct
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
411 3 0 5 6.4 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4SC=C5)C(F)(F)F
CHEMBL4469848 drd1_human Human No 8.6 EC50 = 2.3 nM Funct
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
395 3 0 5 6.0 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL1196161 drd1_human Human Yes 8.6 EC50 = 2.3 nM Bind
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
343 3 2 3 4.2 CC1=CC(=CC=C1)C2CN(CCC3=C(C(=C(C=C23)O)O)Cl)CC=C
CHEMBL4469848 drd1_human Human No 8.6 EC50 = 2.3 nM Funct
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
395 3 0 5 6.0 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL3421729 drd1_human Human Yes 8.6 EC50 = 2.3 nM Funct
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
449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C
CHEMBL4294397 drd1_human Human No 8.6 EC50 = 2.7 nM Funct
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL4294397 drd1_human Human No 8.6 EC50 = 2.7 nM Funct
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL588 drd1_human Human Yes 8.6 EC50 = 2.8 nM Funct
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
305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O
CHEMBL59 drd1_human Human Yes 7.7 EC50 = 20 nM Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL3276140 drd1_human Human Yes 7.7 EC50 = 20.4 nM Funct
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
351 2 0 5 3.3 CC(=O)OC1=C(C2=C(C[C@@H]3C4=C(CCN3C)C=CC=C42)C=C1)OC(=O)C
CHEMBL3276140 drd1_human Human Yes 7.7 EC50 = 20.4 nM Funct
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
351 2 0 5 3.3 CC(=O)OC1=C(C2=C(C[C@@H]3C4=C(CCN3C)C=CC=C42)C=C1)OC(=O)C
CHEMBL4759339 drd1_human Human No 6.7 EC50 = 200 nM Bind
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)
385 2 0 5 4.2 Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL587 drd1_rat Rat Yes 4.7 EC50 = 20000 nM Funct
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
276 7 2 3 2.6 CCCN(CCC)CCc1ccc(O)c2c1CC(=O)N2
CHEMBL4450338 drd1_human Human No 6.7 EC50 = 208.9 nM Bind
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
357 3 1 7 4.2 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL4465393 drd1_human Human No 7.7 EC50 = 21.4 nM Bind
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
372 3 0 6 5.4 CC1=C(C=CC(=C1)OC2=NC=CC3=C2SC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4543306 drd1_human Human Yes 7.7 EC50 = 21.9 nM Funct
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
332 3 1 6 4.3 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=NC(=CN=C4C)N
CHEMBL2397380 drd1_human Human No 7.7 EC50 = 21.9 nM Funct
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
281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2
CHEMBL3040164 drd1_human Human No 7.7 EC50 = 21.9 nM Funct
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
281 0 2 3 3.2 Cc1ccc2c3c1-c1c(ccc(O)c1O)C[C@H]3N(C)CC2
CHEMBL3099231 drd1_human Human No 6.7 EC50 = 210 nM Funct
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
327 4 1 5 2.2 CCCN1C[C@@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4450338 drd1_human Human No 6.7 EC50 = 210 nM Bind
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
357 3 1 7 4.2 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL4519136 drd1_human Human No 6.7 EC50 = 210 nM Funct
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
502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1
CHEMBL2114444 drd1_carau Goldfish No 7.7 EC50 = 22 nM Funct
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
301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL2219803 drd1_carau Goldfish No 7.7 EC50 = 22 nM Funct
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
301 1 3 4 3.3 CCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL4465393 drd1_human Human No 7.7 EC50 = 22 nM Bind
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
372 3 0 6 5.4 CC1=C(C=CC(=C1)OC2=NC=CC3=C2SC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4543306 drd1_human Human Yes 7.7 EC50 = 22 nM Funct
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
332 3 1 6 4.3 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=NC(=CN=C4C)N
CHEMBL4448100 drd1_human Human No 7.7 EC50 = 22 nM Funct
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
421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12
CHEMBL4572614 drd1_human Human No 6.6 EC50 = 229.1 nM Bind
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
410 3 0 6 5.7 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL4282096 drd1_human Human No 5.6 EC50 = 2293 nM Funct
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
291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1
CHEMBL487387 drd1_human Human Yes 7.6 EC50 = 23 nM Funct
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
327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O
CHEMBL27117 drd1_human Human No 7.6 EC50 = 23 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
282 0 3 4 2.4 Cc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL420972 drd1_rat Rat No 7.6 EC50 = 23.4 nM Funct
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
279 6 3 4 3.0 CCCCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL3099235 drd1_human Human No 6.6 EC50 = 230 nM Funct
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
328 4 1 6 1.6 CCCN1C[C@@H](Cn2cncn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4572614 drd1_human Human No 6.6 EC50 = 230 nM Bind
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
410 3 0 6 5.7 CC1=C(N2C=CN=C2C=N1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL282136 drd1_human Human No 6.6 EC50 = 230 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
282 0 3 4 2.4 Cc1cncc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL59 drd1_human Human Yes 6.6 EC50 = 232 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL2114209 drd1_human Human No 6.6 EC50 = 232 nM Funct
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
223 2 3 4 1.4 CC[C@H]1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL4790277 drd1_human Human No 6.6 EC50 = 233 nM Funct
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)
423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL87897 drd1_human Human No 6.6 EC50 = 237 nM Funct
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
315 4 3 5 2.3 COc1ccc(CC2Cc3c(ccc(O)c3O)[C@H](CN)O2)cc1
CHEMBL4467483 drd1_human Human No 6.6 EC50 = 239.2 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C3[C@H]1CC4=C(C3=C(C=C2)Br)C(=C(C=C4)OC)OC
CHEMBL4467483 drd1_human Human No 6.6 EC50 = 239.9 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C3[C@H]1CC4=C(C3=C(C=C2)Br)C(=C(C=C4)OC)OC
CHEMBL2114441 drd1_carau Goldfish No 7.6 EC50 = 24 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL2219802 drd1_carau Goldfish No 7.6 EC50 = 24 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL28338 drd1_carau Goldfish Yes 7.6 EC50 = 24 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL86576 drd1_human Human No 7.6 EC50 = 24 nM Funct
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
301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O
CHEMBL1195441 drd1_carau Goldfish No 6.6 EC50 = 240 nM Funct
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
273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2
CHEMBL554571 drd1_carau Goldfish No 6.6 EC50 = 240 nM Funct
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
273 0 3 4 2.7 Oc1cc2c(cc1O)[C@H]1c3cscc3CN[C@@H]1CC2
CHEMBL4285528 drd1_human Human No 5.6 EC50 = 2411 nM Funct
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
333 3 0 5 5.2 CC(C)(C)n1nccc1-c1ccc(Oc2nccc3occc23)cc1
CHEMBL4796761 drd1_human Human No 6.6 EC50 = 245 nM Funct
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)
433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(CC3CCCCC3)nc21
CHEMBL4442011 drd1_human Human No 6.6 EC50 = 246.8 nM Bind
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
323 3 0 3 4.0 CCC1=C2CCN([C@@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL286080 drd1_human Human Yes 6.6 EC50 = 247.5 nM Bind
[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.
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL405519 drd1_human Human No 7.6 EC50 = 25 nM Funct
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
261 2 2 3 2.7 CCCN1CCC[C@@H]2Cc3c(ccc(O)c3O)C[C@H]21
CHEMBL288090 drd1_rat Rat Yes 7.6 EC50 = 25 nM Funct
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
295 3 2 3 3.3 C=CCN1CCC2=CC(=C(C=C2C(C1)C3=CC=CC=C3)O)O
CHEMBL53 drd1_human Human Yes 7.6 EC50 = 25.7 nM Funct
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL4519136 drd1_human Human No 6.6 EC50 = 250 nM Funct
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
502 4 0 4 5.5 Clc1ccc(Br)c(CN2CCN([C@@H]3CC[C@@]4(c5ccc6c(c5)OCO6)C[C@H]4C3)CC2)c1
CHEMBL4442011 drd1_human Human No 6.6 EC50 = 251.2 nM Bind
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
323 3 0 3 4.0 CCC1=C2CCN([C@@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4282096 drd1_human Human No 5.6 EC50 = 2519 nM Funct
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
291 3 0 5 4.0 Cn1nccc1-c1ccc(Oc2nccc3occc23)cc1
CHEMBL4756486 drd1_human Human Yes 6.6 EC50 = 255 nM Funct
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)
419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3cccc(Cl)c3)c(C3CCCCC3)nc21
CHEMBL4446525 drd1_human Human No 6.6 EC50 = 257.0 nM Funct
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
356 3 0 7 3.8 CC1=C(C=CC(=C1)OC2=NC=CN3C2=NC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4439333 drd1_human Human No 5.6 EC50 = 2570.4 nM Bind
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=C5N4C=CN=C5)C
CHEMBL4446525 drd1_human Human No 6.6 EC50 = 260 nM Funct
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
356 3 0 7 3.8 CC1=C(C=CC(=C1)OC2=NC=CN3C2=NC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4439333 drd1_human Human No 5.6 EC50 = 2600 nM Bind
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=C5N4C=CN=C5)C
CHEMBL4294397 drd1_human Human No 6.6 EC50 = 262 nM Funct
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=CC=CC5=NC=CN54
CHEMBL4469848 drd1_human Human No 6.6 EC50 = 269.2 nM Bind
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
395 3 0 5 6.0 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL4470740 drd1_human Human No 6.6 EC50 = 269.2 nM Funct
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
355 3 0 4 5.2 C1=CC=NC(=C1)OC2=CC(=C(C=C2)C3=CC=CC4=NC=CN43)C(F)(F)F
CHEMBL4469848 drd1_human Human No 6.6 EC50 = 270 nM Bind
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
395 3 0 5 6.0 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)C(F)(F)F
CHEMBL4470740 drd1_human Human No 6.6 EC50 = 270 nM Funct
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
355 3 0 4 5.2 C1=CC=NC(=C1)OC2=CC(=C(C=C2)C3=CC=CC4=NC=CN43)C(F)(F)F
CHEMBL2115374 drd1_carau Goldfish No 5.6 EC50 = 2700 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL39230 drd1_carau Goldfish No 5.6 EC50 = 2700 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL544814 drd1_carau Goldfish No 5.6 EC50 = 2700 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL315516 drd1_human Human No 5.6 EC50 = 2730 nM Funct
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
367 5 3 4 4.5 Oc1ccc2c(c1O)CC(C1CCCCC1)O[C@H]2CNCc1ccccc1
CHEMBL4740497 drd1_human Human No 6.6 EC50 = 276 nM Funct
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)
413 3 0 5 4.7 Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL291100 drd1_carau Goldfish No 7.6 EC50 = 28 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2
CHEMBL40667 drd1_carau Goldfish No 7.6 EC50 = 28 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2
CHEMBL1303 drd1_human Human Yes 7.6 EC50 = 28 nM Funct
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
315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1
CHEMBL4449549 drd1_human Human No 7.6 EC50 = 28 nM Funct
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
413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1c(F)cccc1Cl
CHEMBL4559891 drd1_human Human No 6.5 EC50 = 287 nM Funct
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
469 5 1 4 5.2 C[C@H]1c2cccc(-c3cnn(C4CC4)c3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL446350 drd1_carau Goldfish No 7.5 EC50 = 29 nM Funct
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
315 1 3 4 3.8 CC(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL387250 drd1_human Human No 7.5 EC50 = 29 nM Funct
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
269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CO2
CHEMBL17357 drd1_rat Rat Yes 6.5 EC50 = 295 nM Funct
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.
210 2 3 5 1.2 NCCc1ccc(O)c2nc(O)sc12
CHEMBL4759814 drd1_human Human No 6.5 EC50 = 295 nM Funct
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)
463 4 0 6 5.0 COc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL291143 drd1_human Human Yes 8.5 EC50 = 3 nM Bind
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
329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3
CHEMBL3421729 drd1_human Human Yes 8.5 EC50 = 3 nM Funct
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
449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C
CHEMBL314459 drd1_human Human No 8.5 EC50 = 3.1 nM Funct
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
277 2 3 4 2.6 NC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL87734 drd1_human Human No 8.5 EC50 = 3.5 nM Funct
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
287 2 4 5 2.1 NC[C@@H]1OC(c2cccc(O)c2)Cc2c1ccc(O)c2O
CHEMBL3421836 drd1_human Human No 8.4 EC50 = 3.7 nM Funct
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
435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL53 drd1_human Human Yes 8.4 EC50 = 3.8 nM Funct
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL1224528 drd1_human Human Yes 8.4 EC50 = 3.9 nM Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CC2
CHEMBL53 drd1_human Human Yes 8.4 EC50 = 4.0 nM Funct
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL1467585 drd1_human Human Yes 7.5 EC50 = 30 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL24077 drd1_human Human Yes 7.5 EC50 = 30 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL503958 drd1_human Human Yes 7.5 EC50 = 30 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL25856 drd1_rat Rat Yes 7.5 EC50 = 30 nM Funct
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
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL4555682 drd1_human Human Yes 7.5 EC50 = 30 nM Funct
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
421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl
CHEMBL419680 drd1_rat Rat No 7.5 EC50 = 30.3 nM Funct
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
317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL286080 drd1_human Human Yes 6.5 EC50 = 300 nM Funct
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
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL2115377 drd1_carau Goldfish No 7.5 EC50 = 31 nM Funct
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
301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL296993 drd1_carau Goldfish No 7.5 EC50 = 31 nM Funct
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
301 1 3 4 3.3 CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4555547 drd1_human Human Yes 7.5 EC50 = 31.6 nM Funct
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
379 4 0 5 4.1 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)OC(=O)C)OC(=O)C
CHEMBL4555547 drd1_human Human Yes 7.5 EC50 = 31.7 nM Funct
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
379 4 0 5 4.1 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)OC(=O)C)OC(=O)C
CHEMBL588 drd1_human Human Yes 7.5 EC50 = 31.7 nM Bind
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
305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O
CHEMBL3421730 drd1_mouse Mouse No 6.5 EC50 = 312 nM Funct
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
421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL2397385 drd1_human Human No 6.5 EC50 = 316 nM Funct
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
423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL3040059 drd1_human Human No 6.5 EC50 = 316 nM Funct
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
423 2 3 4 5.3 CN1CCc2ccc(Cc3ccc(O)c4ccccc34)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL4531083 drd1_human Human No 6.5 EC50 = 316.2 nM Funct
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
409 5 0 6 5.7 CC1=C(C=CC(=C1)N(CC2CC2)C3=NC=CC4=C3C=CO4)C5=C(N=CC6=NC=CN65)C
CHEMBL217299 drd1_human Human Yes 7.5 EC50 = 32 nM Funct
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
269 0 3 4 2.1 Oc1cc2c(cc1O)C1c3ccccc3CNC1CO2
CHEMBL4531083 drd1_human Human No 6.5 EC50 = 320 nM Funct
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
409 5 0 6 5.7 CC1=C(C=CC(=C1)N(CC2CC2)C3=NC=CC4=C3C=CO4)C5=C(N=CC6=NC=CN65)C
CHEMBL4277264 drd1_human Human Yes 6.5 EC50 = 320 nM Bind
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL1311333 drd1_human Human Yes 6.5 EC50 = 320 nM Bind
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)
385 2 0 5 4.3 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCCC3)nc21
CHEMBL4755481 drd1_human Human No 6.5 EC50 = 320 nM Bind
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)
405 2 0 5 4.5 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCC3)nc21
CHEMBL4784295 drd1_human Human No 6.5 EC50 = 320 nM Bind
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)
371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21
CHEMBL28054 drd1_human Human No 6.5 EC50 = 320 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cnccc3CN[C@@H]1CC2
CHEMBL1191487 drd1_carau Goldfish No 5.5 EC50 = 3200 nM Funct
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
273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2
CHEMBL542593 drd1_carau Goldfish No 5.5 EC50 = 3200 nM Funct
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
273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@@H]1CC2
CHEMBL2114440 drd1_carau Goldfish No 7.5 EC50 = 33 nM Funct
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
287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL2219804 drd1_carau Goldfish No 7.5 EC50 = 33 nM Funct
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
287 0 3 4 3.0 Cc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL4277264 drd1_human Human Yes 7.5 EC50 = 33 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL3099227 drd1_human Human No 6.5 EC50 = 330 nM Funct
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
245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3139043 drd1_human Human No 6.5 EC50 = 330 nM Funct
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
245 2 1 3 1.7 C=CCN1CCO[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4448100 drd1_rat Rat No 6.5 EC50 = 332 nM Funct
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
421 2 1 1 6.9 Cc1cccc(Cl)c1NC(=O)C1(C)CC2c3ccccc3C1c1cc(Cl)ccc12
CHEMBL4438800 drd1_human Human No 6.5 EC50 = 333.9 nM Funct
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
429 2 0 5 4.1 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)Br
CHEMBL87910 drd1_human Human No 7.5 EC50 = 34.4 nM Funct
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
285 3 3 4 2.3 NC[C@@H]1OC(Cc2ccccc2)Cc2c1ccc(O)c2O
CHEMBL59 drd1_human Human Yes 7.5 EC50 = 35 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4453318 drd1_human Human Yes 7.5 EC50 = 35 nM Bind
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
363 3 1 6 3.3 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(C(=O)NC(=O)N4C)C
CHEMBL4465592 drd1_human Human No 7.5 EC50 = 35.5 nM Funct
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
383 4 0 6 5.3 CCN(C1=CC(=C(C=C1)C2=C(N=CC3=NC=CN32)C)C)C4=NC=CC5=C4C=CO5
CHEMBL59 drd1_rat Rat Yes 5.5 EC50 = 3500 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4438800 drd1_human Human No 6.5 EC50 = 354.8 nM Funct
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
429 2 0 5 4.1 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)Br
CHEMBL4465592 drd1_human Human No 7.4 EC50 = 36 nM Funct
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
383 4 0 6 5.3 CCN(C1=CC(=C(C=C1)C2=C(N=CC3=NC=CN32)C)C)C4=NC=CC5=C4C=CO5
CHEMBL4439029 drd1_human Human No 7.4 EC50 = 36.9 nM Bind
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
323 3 0 3 4.0 CCC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL3099232 drd1_human Human No 6.4 EC50 = 360 nM Funct
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
403 5 1 5 3.9 CCCN1C[C@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL353335 drd1_human Human Yes 6.4 EC50 = 360 nM Bind
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
289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1
CHEMBL4475239 drd1_human Human No 6.4 EC50 = 360 nM Funct
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
388 2 1 6 3.2 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1nccc2occc12
CHEMBL59 drd1_human Human Yes 7.4 EC50 = 37 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4439029 drd1_human Human No 7.4 EC50 = 37.2 nM Bind
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
323 3 0 3 4.0 CCC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL315535 drd1_human Human No 7.4 EC50 = 37.6 nM Funct
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
329 4 2 4 3.2 C#CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL4790909 drd1_human Human No 6.4 EC50 = 370 nM Bind
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)
373 3 0 5 3.7 Cc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL284644 drd1_human Human No 7.4 EC50 = 38 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3ccncc3CN[C@@H]1CC2
CHEMBL4779641 drd1_human Human No 6.4 EC50 = 380 nM Bind
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)
393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccc(Cl)cc1
CHEMBL4513262 drd1_human Human No 6.4 EC50 = 385.9 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C(C=CC3=C2[C@@H]1CC4=C3C(=C(C=C4)OC)OC)Br
CHEMBL1467585 drd1_human Human Yes 6.4 EC50 = 386 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL24077 drd1_human Human Yes 6.4 EC50 = 386 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL503958 drd1_human Human Yes 6.4 EC50 = 386 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL286080 drd1_human Human Yes 6.4 EC50 = 386 nM Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL4513262 drd1_human Human No 6.4 EC50 = 389.1 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C(C=CC3=C2[C@@H]1CC4=C3C(=C(C=C4)OC)OC)Br
CHEMBL288536 drd1_carau Goldfish No 7.4 EC50 = 39 nM Funct
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
273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3sccc3CN[C@H]1CC2
CHEMBL59 drd1_human Human Yes 7.4 EC50 = 39 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL86576 drd1_rat Rat No 7.4 EC50 = 39.8 nM Funct
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
301 4 3 5 2.1 NC[C@@H]1OC(COc2ccccc2)Cc2c1ccc(O)c2O
CHEMBL3099233 drd1_human Human No 5.4 EC50 = 3900 nM Funct
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
403 5 1 5 3.9 CCCN1C[C@@H](Cn2ccc(-c3ccccc3)n2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL1224452 drd1_human Human No 8.4 EC50 = 4.3 nM Funct
Agonist activity at human D1 receptor assessed as cAMP accumulationAgonist activity at human D1 receptor assessed as cAMP accumulation
269 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@H]1CO2
CHEMBL353335 drd1_human Human Yes 8.3 EC50 = 4.7 nM Funct
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
289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1
CHEMBL292418 drd1_human Human Yes 7.4 EC50 = 40.4 nM Bind
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
273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1
CHEMBL540857 drd1_human Human Yes 7.4 EC50 = 40.4 nM Bind
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
273 1 2 2 3.3 Oc1cc2c(cc1Cl)CCNCC2c1ccccc1
CHEMBL3099239 drd1_human Human No 6.4 EC50 = 400 nM Funct
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
361 4 1 5 2.9 CCCN1C[C@@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL1189465 drd1_rat Rat No 6.4 EC50 = 400 nM Funct
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
325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1
CHEMBL538785 drd1_rat Rat No 6.4 EC50 = 400 nM Funct
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
325 3 3 4 3.3 C=CCN1CCc2c(cc(O)c(O)c2C)C(c2ccc(O)cc2)C1
CHEMBL1190300 drd1_rat Rat No 6.4 EC50 = 400 nM Funct
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
311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1
CHEMBL540575 drd1_rat Rat No 6.4 EC50 = 400 nM Funct
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
311 3 3 4 3.0 C=CCN1CCc2cc(O)c(O)cc2C(c2ccc(O)cc2)C1
CHEMBL4435882 drd1_human Human No 7.4 EC50 = 41.4 nM Bind
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
457 4 0 6 5.0 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)C5=CC(=CC=C5)OC
CHEMBL4435882 drd1_human Human No 7.4 EC50 = 41.7 nM Bind
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
457 4 0 6 5.0 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)C5=CC(=CC=C5)OC
CHEMBL4449782 drd1_human Human No 6.4 EC50 = 410 nM Funct
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
374 2 1 6 2.9 Cc1c(-c2ccc3c(c2)CCN3c2nccc3occc23)n(C)c(=O)[nH]c1=O
CHEMBL4740678 drd1_human Human No 6.4 EC50 = 410 nM Bind
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)
415 3 0 6 4.3 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL487387 drd1_rat Rat Yes 4.4 EC50 = 41100 nM Funct
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
327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O
CHEMBL4278861 drd1_human Human Yes 6.4 EC50 = 416 nM Funct
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
356 3 0 6 5.0 Cc1cc(Oc2nccc3occc23)ccc1-n1c(C)nc2cnccc21
CHEMBL4784143 drd1_human Human No 6.4 EC50 = 423 nM Funct
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)
393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1
CHEMBL290842 drd1_carau Goldfish No 7.4 EC50 = 43 nM Funct
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
307 0 3 4 3.4 Oc1cc2c(cc1O)[C@@H]1c3sc(Cl)cc3CN[C@H]1CC2
CHEMBL4784295 drd1_human Human No 7.4 EC50 = 43.1 nM Funct
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)
371 2 0 5 3.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CCCC3)nc21
CHEMBL4787728 drd1_human Human No 6.4 EC50 = 431 nM Funct
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)
433 3 0 5 5.0 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(CC3CCCCC3)nc21
CHEMBL1822918 drd1_human Human No 6.4 EC50 = 438 nM Funct
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
281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2
CHEMBL1852340 drd1_human Human No 6.4 EC50 = 438 nM Funct
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
281 0 3 3 2.7 Oc1cc2c(cc1O)[C@H]1c3ccccc3CC[C@@H]1NCC2
CHEMBL289867 drd1_carau Goldfish No 7.4 EC50 = 44 nM Funct
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
329 3 3 4 4.1 CCCCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2
CHEMBL59 drd1_human Human Yes 7.4 EC50 = 44 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL4514994 drd1_human Human No 6.4 EC50 = 440 nM Funct
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
448 4 1 5 3.5 CN(Cc1nc2cc(Br)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21
CHEMBL4538358 drd1_human Human No 6.4 EC50 = 450 nM Funct
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
349 3 2 7 2.3 Cc1c(-c2ccc(Nc3nccc4occc34)nc2)n(C)c(=O)[nH]c1=O
CHEMBL419680 drd1_human Human No 7.3 EC50 = 46.5 nM Funct
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
317 5 3 4 3.4 C=CCNC[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL4558647 drd1_human Human No 6.3 EC50 = 460 nM Funct
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
438 4 1 5 3.8 CN(Cc1nc2cc(C(F)(F)F)ccc2[nH]1)C(=O)Cn1c(=O)oc2ccc(Cl)cc21
CHEMBL278188 drd1_rat Rat Yes 5.3 EC50 = 4650 nM Funct
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
192 2 3 3 0.4 NCCc1ccc(O)c2c1CC(=O)N2
CHEMBL40950 drd1_carau Goldfish No 7.3 EC50 = 47 nM Funct
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
273 0 3 4 2.7 Oc1cc2c(cc1O)[C@@H]1c3ccsc3CN[C@H]1CC2
CHEMBL41809 drd1_carau Goldfish No 6.3 EC50 = 470 nM Funct
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
343 3 3 4 4.3 CC(C)CCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4469983 drd1_human Human No 6.3 EC50 = 490 nM Bind
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
351 3 1 5 4.1 CC1=C(C(=NNC1=O)C)C2=C(C=C(C=C2)OC3=NC=CC4=C3C=CO4)F
CHEMBL87958 drd1_human Human Yes 6.3 EC50 = 490 nM Funct
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
195 1 3 4 0.7 NC[C@@H]1OCCc2c1ccc(O)c2O
CHEMBL542683 drd1_human Human Yes 6.3 EC50 = 490 nM Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O
CHEMBL99361 drd1_human Human Yes 6.3 EC50 = 490 nM Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
195 1 3 4 0.7 NCC1OCCc2c1ccc(O)c2O
CHEMBL317741 drd1_rat Rat No 6.3 EC50 = 491 nM Funct
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
329 3 2 3 3.9 C=CCN1CCc2c(cc(O)c(O)c2Cl)[C@@H](c2ccccc2)C1
CHEMBL2335736 drd1_human Human No 8.3 EC50 = 5 nM Funct
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
409 3 2 5 3.9 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(OC(F)(F)F)cc3)CCN1CC2
CHEMBL313530 drd1_human Human No 8.3 EC50 = 5.1 nM Funct
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
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
CHEMBL291143 drd1_rat Rat Yes 8.3 EC50 = 5.1 nM Funct
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
329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3
CHEMBL84983 drd1_human Human No 8.3 EC50 = 5.2 nM Funct
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
299 4 3 4 2.7 NC[C@@H]1OC(CCc2ccccc2)Cc2c1ccc(O)c2O
CHEMBL3697578 drd1_human Human Yes 8.3 EC50 = 5.3 nM Funct
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
389 5 1 6 3.1 CC1=C(C=CC(=C1)OC2=C(C=CC=N2)OC(F)F)C3=C(C(=O)NC(=O)N3C)C
CHEMBL1950491 drd1_human Human Yes 8.3 EC50 = 5.6 nM Funct
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2
CHEMBL1962947 drd1_human Human Yes 8.3 EC50 = 5.6 nM Funct
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
327 2 2 5 2.8 COc1cc2c(cc1O)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2
CHEMBL4439333 drd1_human Human No 8.2 EC50 = 5.8 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=C5N4C=CN=C5)C
CHEMBL4439333 drd1_human Human No 8.2 EC50 = 5.8 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=C5N4C=CN=C5)C
CHEMBL85689 drd1_human Human No 8.2 EC50 = 5.8 nM Funct
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
305 2 3 4 3.4 NC[C@@H]1OC(C2CCCCCCC2)Cc2c1ccc(O)c2O
CHEMBL3421730 drd1_human Human No 8.2 EC50 = 5.8 nM Funct
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
421 4 2 3 4.3 C[C@H]1c2cccc(C(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL44414 drd1_carau Goldfish No 7.3 EC50 = 50 nM Funct
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
301 1 3 4 3.3 CCc1cc2c(s1)[C@H]1c3cc(O)c(O)cc3CC[C@@H]1NC2
CHEMBL1180562 drd1_rat Rat No 7.3 EC50 = 50 nM Funct
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
389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1
CHEMBL131313 drd1_rat Rat No 7.3 EC50 = 50 nM Funct
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
389 3 3 4 3.7 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccc(O)cc2)C1
CHEMBL59 drd1_rat Rat Yes 5.3 EC50 = 5000 nM Funct
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
153 2 3 3 0.6 NCCc1ccc(c(c1)O)O
CHEMBL53 drd1_human Human Yes 6.3 EC50 = 501.2 nM Bind
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL4442011 drd1_human Human No 6.3 EC50 = 501.2 nM Funct
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
323 3 0 3 4.0 CCC1=C2CCN([C@@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4555547 drd1_human Human Yes 5.3 EC50 = 5011.9 nM Bind
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
379 4 0 5 4.1 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)OC(=O)C)OC(=O)C
CHEMBL4442011 drd1_human Human No 6.3 EC50 = 505.1 nM Funct
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
323 3 0 3 4.0 CCC1=C2CCN([C@@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4762375 drd1_human Human No 6.3 EC50 = 510 nM Bind
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)
399 2 0 5 4.6 Cc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4790277 drd1_human Human No 6.3 EC50 = 510 nM Bind
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)
423 4 0 6 4.1 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL2115374 drd1_carau Goldfish No 7.3 EC50 = 52 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL39230 drd1_carau Goldfish No 7.3 EC50 = 52 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL544814 drd1_carau Goldfish No 7.3 EC50 = 52 nM Funct
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL53 drd1_human Human Yes 7.3 EC50 = 52 nM Funct
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL82899 drd1_rat Rat No 7.3 EC50 = 52.3 nM Funct
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
251 1 3 4 2.1 CC(C)(C)C1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL53 drd1_human Human Yes 6.3 EC50 = 520.8 nM Bind
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
267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O
CHEMBL4517022 drd1_human Human No 6.3 EC50 = 530 nM Funct
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)C2=CC=CC3=NC=CN32)OC4=NC=CC5=C4C=CO5
CHEMBL4517022 drd1_human Human No 6.3 EC50 = 537.0 nM Funct
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
341 3 0 5 5.2 CC1=C(C=CC(=C1)C2=CC=CC3=NC=CN32)OC4=NC=CC5=C4C=CO5
CHEMBL4574838 drd1_human Human No 7.3 EC50 = 55.0 nM Funct
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
370 3 0 6 5.3 CC1=C(C=CC(=C1C)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4465386 drd1_human Human No 6.3 EC50 = 540 nM Funct
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
413 4 2 3 3.9 C[C@H]1c2cccc(-c3cn[nH]c3)c2C[C@H](CO)N1C(=O)Cc1ccc(F)cc1Cl
CHEMBL4287192 drd1_human Human No 5.3 EC50 = 5485 nM Funct
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
343 3 0 7 4.0 Cc1cc(Oc2nccc3occc23)ccc1-c1cncc2ncnn12
CHEMBL4555547 drd1_human Human Yes 5.3 EC50 = 5496 nM Bind
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
379 4 0 5 4.1 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)OC(=O)C)OC(=O)C
CHEMBL4574838 drd1_human Human No 7.3 EC50 = 55 nM Funct
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
370 3 0 6 5.3 CC1=C(C=CC(=C1C)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4760355 drd1_human Human No 7.3 EC50 = 55.9 nM Funct
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)
359 3 0 5 3.4 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1
CHEMBL1467585 drd1_human Human Yes 7.3 EC50 = 56 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL24077 drd1_human Human Yes 7.3 EC50 = 56 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL503958 drd1_human Human Yes 7.3 EC50 = 56 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL4555682 drd1_human Human Yes 7.3 EC50 = 56 nM Funct
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
421 2 1 1 6.9 Cc1ccc(Cl)c(NC(=O)C2(C)CC3c4ccccc4C2c2ccccc23)c1Cl
CHEMBL588 drd1_rat Rat Yes 7.2 EC50 = 57 nM Funct
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
305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O
CHEMBL1822919 drd1_human Human No 6.2 EC50 = 570 nM Funct
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
283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2
CHEMBL1852625 drd1_human Human No 6.2 EC50 = 570 nM Funct
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
283 0 3 4 2.1 Oc1cc2c(cc1O)[C@H]1c3ccccc3OC[C@@H]1NCC2
CHEMBL4565185 drd1_human Human No 6.2 EC50 = 580 nM Funct
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
378 3 1 6 2.7 Cc1nc2c(c(Oc3ccc(-c4c(C)c(=O)[nH]c(=O)n4C)c(C)c3)n1)CCC2
CHEMBL4755709 drd1_human Human No 6.2 EC50 = 580 nM Bind
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)
435 3 0 6 4.6 COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL1822920 drd1_human Human No 6.2 EC50 = 584 nM Funct
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
299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2
CHEMBL1852349 drd1_human Human No 6.2 EC50 = 584 nM Funct
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
299 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3ccccc3SC[C@@H]1NCC2
CHEMBL1467585 drd1_human Human Yes 7.2 EC50 = 59 nM Bind
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL24077 drd1_human Human Yes 7.2 EC50 = 59 nM Bind
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL503958 drd1_human Human Yes 7.2 EC50 = 59 nM Bind
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL431220 drd1_human Human No 8.2 EC50 = 6.3 nM Funct
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
251 4 3 4 2.2 CCCCC1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL315005 drd1_human Human No 8.2 EC50 = 6.4 nM Funct
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
301 3 3 5 2.4 COc1cccc(C2Cc3c(ccc(O)c3O)[C@H](CN)O2)c1
CHEMBL85409 drd1_human Human No 8.2 EC50 = 6.7 nM Funct
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
277 3 3 4 2.6 NC[C@@H]1OC(CC2CCCC2)Cc2c1ccc(O)c2O
CHEMBL281932 drd1_human Human No 8.2 EC50 = 6.7 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
268 0 3 4 2.0 Oc1cc2c(cc1O)[C@H]1c3cccnc3CN[C@@H]1CC2
CHEMBL4449153 drd1_human Human No 6.2 EC50 = 602.6 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)C2=C(N=CC3=NC=CN32)C)OC4=NC=CC5=C4C=CO5
CHEMBL4443737 drd1_human Human No 7.2 EC50 = 61.7 nM Funct
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
396 4 0 6 5.8 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C(=CO3)C4CC4)C5=C(N=CC6=NC=CN65)C
CHEMBL4449153 drd1_human Human No 6.2 EC50 = 610 nM Funct
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
356 3 0 6 4.9 CC1=C(C=CC(=C1)C2=C(N=CC3=NC=CN32)C)OC4=NC=CC5=C4C=CO5
CHEMBL4470808 drd1_human Human No 6.2 EC50 = 610 nM Funct
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
380 4 2 6 2.5 CC(=O)Nc1cccnc1Oc1ccc(-c2c(C)c(=O)[nH]c(=O)n2C)c(C)c1
CHEMBL4443737 drd1_human Human No 7.2 EC50 = 62 nM Funct
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
396 4 0 6 5.8 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C(=CO3)C4CC4)C5=C(N=CC6=NC=CN65)C
CHEMBL3421729 drd1_mouse Mouse Yes 7.2 EC50 = 62.1 nM Funct
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
449 6 2 3 4.7 OC[C@H]1Cc2c(cccc2[C@@H](N1C(=O)Cc1c(Cl)cccc1Cl)C)CCC(O)(C)C
CHEMBL287513 drd1_human Human No 7.2 EC50 = 63 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
322 0 3 4 2.9 Oc1cc2c(cc1O)[C@H]1c3cc4c(nc3CN[C@@H]1CC2)CCCC4
CHEMBL4784143 drd1_human Human No 6.2 EC50 = 630 nM Bind
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)
393 3 0 5 4.1 CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1cccc(Cl)c1
CHEMBL4279267 drd1_human Human No 7.2 EC50 = 64 nM Funct
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
355 3 0 5 5.6 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ccc2nccn12
CHEMBL416435 drd1_carau Goldfish No 6.2 EC50 = 640 nM Funct
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
363 1 3 4 4.7 Cc1cccc(-c2cc3c(s2)CN[C@H]2CCc4cc(O)c(O)cc4[C@H]32)c1
CHEMBL4459395 drd1_human Human No 6.2 EC50 = 640 nM Funct
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
399 4 0 6 5.2 CC1=C(C=CC(=C1)OC2=NC=CC(=C2)N3CCCCC3)C4=C(N=CC5=NC=CN54)C
CHEMBL4459395 drd1_human Human No 6.2 EC50 = 645.7 nM Funct
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
399 4 0 6 5.2 CC1=C(C=CC(=C1)OC2=NC=CC(=C2)N3CCCCC3)C4=C(N=CC5=NC=CN54)C
CHEMBL84557 drd1_human Human No 6.2 EC50 = 650 nM Funct
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
331 5 2 4 3.8 C=CCN(C)C[C@@H]1OC(C2CCCCC2)Cc2c1ccc(O)c2O
CHEMBL4740312 drd1_human Human No 6.2 EC50 = 650 nM Bind
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)
295 1 1 4 2.4 Cn1c2ccccc2c(=O)c2c(=O)[nH]c(C3CCCC3)nc21
CHEMBL4452764 drd1_human Human No 7.2 EC50 = 66.1 nM Funct
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
405 3 0 4 6.4 C1=CC=C2C(=C1)C=CN=C2OC3=CC(=C(C=C3)C4=CC=CC5=NC=CN54)C(F)(F)F
CHEMBL4435882 drd1_human Human No 6.2 EC50 = 660.7 nM Funct
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
457 4 0 6 5.0 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)C5=CC(=CC=C5)OC
CHEMBL286080 drd1_human Human Yes 6.2 EC50 = 665.9 nM Funct
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
255 1 3 3 2.4 Oc1cc2CCNCC(c2cc1O)c1ccccc1
CHEMBL4435882 drd1_human Human No 6.2 EC50 = 669.1 nM Funct
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
457 4 0 6 5.0 CC(=O)OC1=C(C=C2C[C@@H]3C4=C(CCN3C)C=CC=C4C2=C1OC(=O)C)C5=CC(=CC=C5)OC
CHEMBL4452764 drd1_human Human No 7.2 EC50 = 67 nM Funct
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
405 3 0 4 6.4 C1=CC=C2C(=C1)C=CN=C2OC3=CC(=C(C=C3)C4=CC=CC5=NC=CN54)C(F)(F)F
CHEMBL315849 drd1_human Human No 7.2 EC50 = 67 nM Funct
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
233 2 3 4 1.1 C#CCC1Cc2c(ccc(O)c2O)[C@H](CN)O1
CHEMBL420604 drd1_human Human No 7.2 EC50 = 68.7 nM Funct
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
263 1 3 4 2.4 NC[C@@H]1OC2(CCCCC2)Cc2c1ccc(O)c2O
CHEMBL2115373 drd1_carau Goldfish No 7.2 EC50 = 69 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL290438 drd1_carau Goldfish No 7.2 EC50 = 69 nM Funct
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
329 0 3 4 4.0 CC(C)(C)c1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4467080 drd1_human Human No 6.2 EC50 = 690 nM Bind
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
355 3 0 6 4.5 CC1=C(C=CC(=C1)OC2=NC=CN3C2=CC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL4467080 drd1_human Human No 6.2 EC50 = 691.8 nM Bind
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
355 3 0 6 4.5 CC1=C(C=CC(=C1)OC2=NC=CN3C2=CC=C3)C4=C(N=CC5=NC=CN54)C
CHEMBL315468 drd1_rat Rat No 8.2 EC50 = 7.1 nM Funct
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
271 2 3 4 2.4 NC[C@@H]1OC(c2ccccc2)Cc2c1ccc(O)c2O
CHEMBL25856 drd1_human Human Yes 8.1 EC50 = 7.2 nM Funct
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
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL4589664 drd1_human Human No 8.1 EC50 = 7.8 nM Funct
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
394 3 0 5 5.5 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CN5C4=CC=C5)C(F)(F)F
CHEMBL4589664 drd1_human Human No 8.1 EC50 = 7.8 nM Funct
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
394 3 0 5 5.5 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CN5C4=CC=C5)C(F)(F)F
CHEMBL4591021 drd1_human Human Yes 8.1 EC50 = 7.9 nM Bind
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
355 6 0 5 3.4 CN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)OCOC)OCOC
CHEMBL407489 drd1_rat Rat Yes 6.2 EC50 = 700 nM Funct
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
247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O
CHEMBL4470553 drd1_human Human Yes 6.1 EC50 = 717.5 nM Funct
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
307 2 0 3 3.9 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C5=C(C=C4)OCO5
CHEMBL4470553 drd1_human Human Yes 6.1 EC50 = 724.4 nM Funct
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
307 2 0 3 3.9 CCCN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C5=C(C=C4)OCO5
CHEMBL3099236 drd1_human Human No 7.1 EC50 = 74 nM Funct
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
361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3139041 drd1_human Human No 7.1 EC50 = 74 nM Funct
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
361 4 1 5 2.9 CCCN1C[C@H](Cn2cc(Cl)cn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL3040157 drd1_human Human No 6.1 EC50 = 741 nM Funct
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
400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1
CHEMBL3216146 drd1_human Human No 6.1 EC50 = 741 nM Funct
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
400 3 2 4 4.5 CN(C)c1ccc(Cc2ccc3c4c2-c2c(ccc(O)c2O)C[C@H]4N(C)CC3)cc1
CHEMBL4457399 drd1_human Human No 7.1 EC50 = 75.9 nM Funct
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
346 4 0 5 5.3 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=C(C=C4)OC)C
CHEMBL2331599 drd1_human Human No 6.1 EC50 = 750 nM Funct
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
343 1 2 3 3.9 Cc1cc2c(cc1O)[C@H]1C[C@](O)(c3ccc(Cl)cc3)CCN1CC2
CHEMBL3421836 drd1_human Human No 7.1 EC50 = 76 nM Funct
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
435 5 2 3 4.4 C[C@H]1c2cccc(CC(C)(C)O)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl
CHEMBL417164 drd1_carau Goldfish No 7.1 EC50 = 77 nM Funct
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
329 3 3 4 4.1 CCCCc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4457399 drd1_human Human No 7.1 EC50 = 77 nM Funct
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
346 4 0 5 5.3 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=C(C=C4)OC)C
CHEMBL4464545 drd1_human Human No 6.1 EC50 = 770 nM Funct
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
435 4 0 5 6.8 C1CC1C2=COC3=C2C(=NC=C3)OC4=CC(=C(C=C4)C5=CC=CC6=NC=CN65)C(F)(F)F
CHEMBL4464545 drd1_human Human No 6.1 EC50 = 776.3 nM Funct
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
435 4 0 5 6.8 C1CC1C2=COC3=C2C(=NC=C3)OC4=CC(=C(C=C4)C5=CC=CC6=NC=CN65)C(F)(F)F
CHEMBL2397381 drd1_human Human No 7.1 EC50 = 78 nM Funct
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
357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL3040115 drd1_human Human No 7.1 EC50 = 78 nM Funct
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
357 2 2 3 4.4 CN1CCc2ccc(Cc3ccccc3)c3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL41196 drd1_carau Goldfish No 7.1 EC50 = 79 nM Funct
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
355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3sc(C4CCCCC4)cc3CN[C@H]1CC2
CHEMBL4518891 drd1_human Human No 7.1 EC50 = 79 nM Funct
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
355 3 0 5 5.6 CC1=C(C=CC(=C1)OC2=CC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4518891 drd1_human Human No 7.1 EC50 = 79.4 nM Funct
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
355 3 0 5 5.6 CC1=C(C=CC(=C1)OC2=CC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4548284 drd1_human Human Yes 6.1 EC50 = 790 nM Bind
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
342 3 1 6 4.5 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL4548284 drd1_human Human Yes 6.1 EC50 = 794.3 nM Bind
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
342 3 1 6 4.5 C1=CC2=NC=CN2C(=C1)C3=C(C=C(C=C3)OC4=NC=CC5=C4C=CO5)N
CHEMBL2335740 drd1_human Human No 8.1 EC50 = 8 nM Funct
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
359 2 2 4 3.6 COc1cc2c(cc1O)[C@H]1C[C@@](O)(c3ccc(Cl)cc3)CCN1CC2
CHEMBL291143 drd1_carau Goldfish Yes 8.1 EC50 = 8.2 nM Funct
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
329 2 3 4 3.3 NC[C@@H]1O[C@@H](Cc2c1ccc(c2O)O)C12CC3CC(C2)CC(C1)C3
CHEMBL313530 drd1_rat Rat No 8.1 EC50 = 8.3 nM Funct
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
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
CHEMBL4591021 drd1_human Human Yes 8.1 EC50 = 8.5 nM Bind
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
355 6 0 5 3.4 CN1CCC2=C3[C@H]1CC4=C(C3=CC=C2)C(=C(C=C4)OCOC)OCOC
CHEMBL26965 drd1_human Human No 8.1 EC50 = 8.6 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
310 2 3 4 3.0 CCCc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL285924 drd1_human Human No 8.1 EC50 = 8.8 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
298 1 3 5 2.1 COc1ccc2c(n1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL43514 drd1_carau Goldfish No 7.1 EC50 = 80 nM Funct
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
349 1 3 4 4.4 Oc1cc2c(cc1O)[C@@H]1c3cc(-c4ccccc4)sc3CN[C@H]1CC2
CHEMBL4789255 drd1_human Human No 6.1 EC50 = 800 nM Bind
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)
419 2 0 5 4.9 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccc(Cl)cc3)c(C3CCCCC3)nc21
CHEMBL26365 drd1_human Human No 6.1 EC50 = 800 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
286 0 3 4 2.2 Oc1cc2c(cc1O)[C@H]1c3cncc(F)c3CN[C@@H]1CC2
CHEMBL4437012 drd1_human Human No 7.1 EC50 = 81 nM Funct
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
331 3 0 5 5.0 CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=NC=C4C)C
CHEMBL4464215 drd1_human Human No 7.1 EC50 = 81.2 nM Funct
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
409 4 1 4 3.8 C[C@H]1c2cccc(-c3cnn(C)c3)c2C[C@H](CO)N1C(=O)Cc1ccccc1Cl
CHEMBL1178784 drd1_carau Goldfish No 7.1 EC50 = 82 nM Funct
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
315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL41238 drd1_carau Goldfish No 7.1 EC50 = 82 nM Funct
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
315 2 3 4 3.7 CCCc1scc2c1CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL4294009 drd1_human Human No 6.1 EC50 = 821 nM Funct
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
327 3 0 5 4.9 c1cc(-c2ccc(Oc3nccc4occc34)cc2)n2ccnc2c1
CHEMBL3098131 drd1_human Human Yes 7.1 EC50 = 83 nM Funct
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
245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL455497 drd1_human Human Yes 7.1 EC50 = 83 nM Funct
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
245 2 1 2 3.0 CCCN1CCC[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL4756163 drd1_human Human No 7.1 EC50 = 83 nM Funct
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)
389 4 0 6 3.4 COc1ccc(-n2c(CC(C)C)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1
CHEMBL4764398 drd1_human Human No 6.1 EC50 = 830 nM Bind
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)
449 3 0 6 4.9 COc1ccc(-n2c(C3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1Cl
CHEMBL4796389 drd1_human Human No 6.1 EC50 = 840 nM Bind
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)
343 2 0 5 3.1 Cn1c2ccccc2c(=O)c2c(=O)n(-c3ccccc3)c(C3CC3)nc21
CHEMBL83080 drd1_human Human Yes 5.1 EC50 = 8577 nM Funct
Formation of cAMP on Dopamine receptor D1 in vitro in carp retinaFormation of cAMP on Dopamine receptor D1 in vitro in carp retina
271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O
CHEMBL83080 drd1_human Human Yes 5.1 EC50 = 8580 nM Funct
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
271 2 3 4 2.4 NC[C@H]1O[C@@H](c2ccccc2)Cc2c1ccc(O)c2O
CHEMBL2115372 drd1_carau Goldfish No 7.1 EC50 = 87 nM Funct
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
287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL289283 drd1_carau Goldfish No 7.1 EC50 = 87 nM Funct
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
287 0 3 4 3.0 Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4589737 drd1_human Human No 7.1 EC50 = 87.1 nM Funct
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
309 2 0 3 3.8 CC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4589737 drd1_human Human No 7.1 EC50 = 87.4 nM Funct
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
309 2 0 3 3.8 CC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL25856 drd1_carau Goldfish Yes 7.1 EC50 = 88 nM Funct
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
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL288846 drd1_carau Goldfish No 7.1 EC50 = 88 nM Funct
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
329 2 3 4 3.9 CC(C)Cc1cc2c(s1)CN[C@H]1CCc3cc(O)c(O)cc3[C@H]21
CHEMBL4450916 drd1_human Human No 7.1 EC50 = 88 nM Funct
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
369 3 0 6 4.9 CC1=C(C=CC(=C1)N(C)C2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL3099230 drd1_human Human No 7.1 EC50 = 89 nM Funct
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
327 4 1 5 2.2 CCCN1C[C@H](Cn2cccn2)O[C@@H]2Cc3c(O)cccc3C[C@H]21
CHEMBL86325 drd1_human Human No 7.1 EC50 = 89 nM Funct
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
315 5 3 5 2.3 NC[C@@H]1OC(COCc2ccccc2)Cc2c1ccc(O)c2O
CHEMBL4450916 drd1_human Human No 7.1 EC50 = 89.1 nM Funct
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
369 3 0 6 4.9 CC1=C(C=CC(=C1)N(C)C2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C
CHEMBL4293757 drd1_human Human Yes 6.1 EC50 = 895 nM Funct
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
361 3 0 5 5.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)cnn1C(C)(C)C
CHEMBL28338 drd1_human Human Yes 8.1 EC50 = 9 nM Bind
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
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL28338 drd1_human Human Yes 8.1 EC50 = 9 nM Funct
Potency in adenylate cyclase functional assay against Dopamine receptor D1Potency in adenylate cyclase functional assay against Dopamine receptor D1
315 2 3 4 3.7 CCCc1cc2c(s1)CN[C@@H]1CCc3cc(O)c(O)cc3[C@@H]21
CHEMBL290149 drd1_carau Goldfish No 7.0 EC50 = 94 nM Funct
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
355 1 3 4 4.8 Oc1cc2c(cc1O)[C@@H]1c3cc(C4CCCCC4)sc3CN[C@H]1CC2
CHEMBL1467585 drd1_carau Goldfish Yes 6.0 EC50 = 950 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL24077 drd1_carau Goldfish Yes 6.0 EC50 = 950 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL503958 drd1_carau Goldfish Yes 6.0 EC50 = 950 nM Funct
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2
CHEMBL4559240 drd1_human Human No 6.0 EC50 = 950 nM Funct
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
414 4 1 6 3.0 Cc1c(-c2c(C)c(=O)[nH]c(=O)n2C)ccc2c1CCN2c1ncccc1OC(F)F
CHEMBL353335 drd1_human Human Yes 5.0 EC50 = 9500 nM Bind
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
289 1 3 3 3.0 Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1
CHEMBL4537900 drd1_human Human No 6.0 EC50 = 951.4 nM Funct
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
393 3 0 5 4.4 CC(C)C1=C(C(=C2C(=C1)C[C@@H]3C4=C(CCN3C)C=CC=C42)OC(=O)C)OC(=O)C
CHEMBL4537900 drd1_human Human No 6.0 EC50 = 955.0 nM Funct
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
393 3 0 5 4.4 CC(C)C1=C(C(=C2C(=C1)C[C@@H]3C4=C(CCN3C)C=CC=C42)OC(=O)C)OC(=O)C
CHEMBL4128926 drd1_human Human No 9.7 IC50 = 0.2 nM Bind
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
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
CHEMBL1256645 drd1_human Human Yes 9.7 IC50 = 0.2 nM Bind
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 9.7 IC50 = 0.2 nM Bind
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 9.7 IC50 = 0.2 nM Bind
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1256645 drd1_human Human Yes 9.6 IC50 = 0.3 nM Bind
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 9.6 IC50 = 0.3 nM Bind
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 9.6 IC50 = 0.3 nM Bind
Binding affinity to human dopamine D1 receptor by radioligand displacement assayBinding affinity to human dopamine D1 receptor by radioligand displacement assay
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL54661 drd1_rat Rat Yes 9.5 IC50 = 0.3 nM Bind
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
434 5 1 4 4.6 OCCN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)C(F)(F)F
CHEMBL13668 drd1_human Human Yes 9.5 IC50 = 0.3 nM Bind
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
287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O
CHEMBL13668 drd1_human Human Yes 9.5 IC50 = 0.3 nM Bind
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
287 1 1 2 3.7 CN1CCc2c(C(C1)c1ccccc1)cc(c(c2)Cl)O
CHEMBL136190 drd1_rat Rat No 9.4 IC50 = 0.4 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
315 1 1 2 4.2 C[C@H]1N(C)CCc2cc(Cl)c(O)cc2[C@@]1(C)c1ccccc1
CHEMBL1256645 drd1_rat Rat Yes 9.2 IC50 = 0.6 nM Bind
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_rat Rat Yes 9.2 IC50 = 0.6 nM Bind
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_rat Rat Yes 9.2 IC50 = 0.6 nM Bind
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL136260 drd1_rat Rat No 9.2 IC50 = 0.7 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL1256645 drd1_human Human Yes 9.2 IC50 = 0.7 nM Bind
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 9.2 IC50 = 0.7 nM Bind
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 9.2 IC50 = 0.7 nM Bind
Percent inhibition against Dopamine receptor D1 at 1 uMPercent inhibition against Dopamine receptor D1 at 1 uM
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL136630 drd1_rat Rat No 9.2 IC50 = 0.7 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL136235 drd1_rat Rat No 9.2 IC50 = 0.7 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C
CHEMBL1256645 drd1_human Human Yes 9.1 IC50 = 0.7 nM Bind
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 9.1 IC50 = 0.7 nM Bind
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 9.1 IC50 = 0.7 nM Bind
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL136226 drd1_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
360 2 0 3 5.0 CN1CCN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL136260 drd1_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
400 3 0 2 5.9 CC(C)N1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL1256645 drd1_human Human Yes 9.1 IC50 = 0.8 nM Bind
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 9.1 IC50 = 0.8 nM Bind
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 9.1 IC50 = 0.8 nM Bind
Inhibition of human dopamine D1 receptorInhibition of human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL343282 drd1_rat Rat No 9.1 IC50 = 0.8 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1
CHEMBL343922 drd1_rat Rat No 9.1 IC50 = 0.9 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2
CHEMBL136235 drd1_rat Rat No 9.1 IC50 = 0.9 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
356 2 0 2 4.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1(C)C
CHEMBL344206 drd1_rat Rat No 9.1 IC50 = 0.9 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
384 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCC2
CHEMBL343922 drd1_rat Rat No 9.0 IC50 = 1.0 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
398 2 0 2 5.6 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2
CHEMBL1256645 drd1_human Human Yes 9.0 IC50 = 1.0 nM Bind
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 9.0 IC50 = 1.0 nM Bind
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 9.0 IC50 = 1.0 nM Bind
Displacement of radiolabeled SCH 23390 from human dopamine D1 receptorDisplacement of radiolabeled SCH 23390 from human dopamine D1 receptor
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL136340 drd1_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
402 4 1 3 4.4 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCO
CHEMBL136822 drd1_rat Rat No 9.0 IC50 = 1 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2
CHEMBL1256645 drd1_rat Rat Yes 9.0 IC50 = 1 nM Bind
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_rat Rat Yes 9.0 IC50 = 1 nM Bind
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_rat Rat Yes 9.0 IC50 = 1 nM Bind
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1256645 drd1_rat Rat Yes 9.0 IC50 = 1.0 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_rat Rat Yes 9.0 IC50 = 1.0 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_rat Rat Yes 9.0 IC50 = 1.0 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL136683 drd1_rat Rat No 9.0 IC50 = 1.1 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1
CHEMBL136932 drd1_rat Rat No 9.0 IC50 = 1.1 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
416 5 1 3 4.8 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1CCCO
CHEMBL137960 drd1_rat Rat Yes 9.0 IC50 = 1.1 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL64875 drd1_rat Rat Yes 8.9 IC50 = 1.2 nM Bind
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
344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1
CHEMBL64875 drd1_rat Rat Yes 8.9 IC50 = 1.2 nM Bind
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
344 1 0 3 4.3 CN1CCN([C@@H]2Cc3ccccc3Sc3ccc(Cl)cc32)CC1
CHEMBL267723 drd1_rat Rat Yes 8.9 IC50 = 1.2 nM Bind
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
404 5 2 4 2.2 CCN1CCC[C@H]1CNC(=O)c1c(OC)ccc(I)c1O
CHEMBL136630 drd1_rat Rat No 8.9 IC50 = 1.3 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
372 2 0 2 5.1 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL1256645 drd1_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
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.
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
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.
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_rat Rat Yes 8.9 IC50 = 1.3 nM Bind
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.
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL343282 drd1_rat Rat No 8.9 IC50 = 1.4 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
346 2 1 3 4.7 CC1(C)CN(C2CC(c3ccsc3)c3ccc(Cl)cc32)CCN1
CHEMBL1256645 drd1_human Human Yes 8.9 IC50 = 1.4 nM Bind
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 8.9 IC50 = 1.4 nM Bind
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 8.9 IC50 = 1.4 nM Bind
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL298406 drd1_human Human Yes 8.8 IC50 = 1.5 nM Funct
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
313 0 1 2 4.0 CN1CCc2c([C@@H]3[C@@H]1CCc1c3cccc1)cc(c(c2)Cl)O
CHEMBL343078 drd1_rat Rat No 8.8 IC50 = 1.5 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
406 2 0 2 5.4 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(C(F)(F)F)cc32)CC1(C)C
CHEMBL137960 drd1_rat Rat Yes 8.8 IC50 = 1.6 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL1256645 drd1_human Human Yes 8.8 IC50 = 1.7 nM Funct
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL1814790 drd1_human Human Yes 8.8 IC50 = 1.7 nM Funct
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL62 drd1_human Human Yes 8.8 IC50 = 1.7 nM Funct
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
287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1
CHEMBL136776 drd1_rat Rat No 8.7 IC50 = 1.8 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
416 2 0 2 5.2 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Br)cc32)CC1(C)C
CHEMBL136822 drd1_rat Rat No 8.7 IC50 = 1.9 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
428 4 1 3 5.0 OCCN1CCN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC12CCCC2
CHEMBL32145 drd1_rat Rat Yes 8.0 IC50 = 10.1 nM Bind
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
373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1
CHEMBL544114 drd1_rat Rat Yes 8.0 IC50 = 10.1 nM Bind
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
373 3 2 3 4.0 C=CCN1CCc2c(cc(O)c(O)c2Br)C(c2ccccc2)C1
CHEMBL4564103 drd1_human Human No 7.0 IC50 = 100 nM Bind
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
373 2 0 3 4.2 CN1CCC2=C3[C@@H]1CC4=C(C3=C(C=C2)Br)C(=C(C=C4)OC)OC
CHEMBL73589 drd1_rat Rat No 7.0 IC50 = 100 nM Bind
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
457 2 0 7 3.7 CN1CCN(C2=Nc3ccccc3Sc3ccc(OS(=O)(=O)C(F)(F)F)cc32)CC1
CHEMBL452510 drd1_rat Rat Yes 7.0 IC50 = 100 nM Bind
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 3.0 COc1cc2c(cc1O)C[C@H]1c3c(ccc(O)c3O2)CCN1C
CHEMBL452512 drd1_rat Rat Yes 6.0 IC50 = 1000 nM Bind
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 1 2 5 3.0 COc1ccc2c(c1O)Oc1c(O)ccc3c1[C@H](C2)N(C)CC3
CHEMBL1189682 drd1_rat Rat No 5.0 IC50 = 10000 nM Bind
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.
303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1
CHEMBL539274 drd1_rat Rat No 5.0 IC50 = 10000 nM Bind
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.
303 6 0 1 4.8 C=CCN(CC=C)C1Cc2ccccc2C(c2ccccc2)C1
CHEMBL1191339 drd1_rat Rat No 5.0 IC50 = 10000 nM Bind
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.
263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1
CHEMBL542419 drd1_rat Rat No 5.0 IC50 = 10000 nM Bind
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.
263 4 1 1 3.9 C=CCNC1Cc2ccccc2C(c2ccccc2)C1
CHEMBL27650 drd1_bovin Bovine No 5.0 IC50 = 10000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL50188 drd1_bovin Bovine No 5.0 IC50 = 10000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL329444 drd1_rat Rat No 5.0 IC50 = 10000 nM Bind
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
249 2 1 4 2.5 CCCN1CCC2=C(CCc3sc(N)nc32)C1
CHEMBL93428 drd1_rat Rat Yes 5.0 IC50 = 10000 nM Bind
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
223 3 1 4 2.2 CCCN1CCC=C(c2csc(N)n2)C1
CHEMBL1178971 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL51985 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
457 9 0 4 4.3 CCC[N+](C)(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1
CHEMBL27763 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1
CHEMBL27995 drd1_bovin Bovine Yes 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
249 5 1 3 2.8 CCCN(CCC)C1COc2cccc(O)c2C1
CHEMBL280608 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL51888 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
418 9 1 5 3.0 CCCN(CCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1
CHEMBL283606 drd1_bovin Bovine Yes 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL284912 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
362 9 0 5 2.8 CCCN(CCCCN1CCOCC1)C1COc2cccc(OC)c2C1
CHEMBL416747 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1
CHEMBL137478 drd1_bovin Bovine No 4.0 IC50 = 100000 nM Bind
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2
CHEMBL283606 drd1_bovin Bovine Yes 4.0 IC50 = 100000 nM Bind
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1
CHEMBL3912178 drd1_human Human Yes 6.0 IC50 = 1008.2 nM Bind
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.
327 2 2 5 2.8 COc1cc2c(cc1OC)C1Cc3cc(O)c(O)cc3CN1CC2
CHEMBL3982119 drd1_human Human No 7.0 IC50 = 101.4 nM Bind
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.
355 4 0 5 3.4 COc1cc2c(cc1OC)[C@@H]1Cc3c(OC)ccc(OC)c3CN1CC2
CHEMBL113477 drd1_rat Rat No 7.0 IC50 = 102 nM Bind
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
251 0 2 2 2.9 Oc1ccc2c(c1)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL4582377 drd1_human Human No 6.0 IC50 = 1030 nM Funct
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
295 0 1 4 2.8 Oc1cccc2c1CC1c3cc4c(cc3CCN1C2)OCO4
CHEMBL1187468 drd1_rat Rat Yes 6.0 IC50 = 1040 nM Bind
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
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
CHEMBL503882 drd1_rat Rat Yes 6.0 IC50 = 1040 nM Bind
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
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
CHEMBL3912606 drd1_human Human Yes 6.0 IC50 = 1057.1 nM Bind
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.
357 3 2 6 2.8 COc1cc2c(c(OC)c1OC)CN1CCc3cc(O)c(O)cc3C1C2
CHEMBL42 drd1_human Human Yes 7.0 IC50 = 107 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL119455 drd1_rat Rat No 7.0 IC50 = 107 nM Bind
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.
251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3
CHEMBL284746 drd1_rat Rat Yes 5.0 IC50 = 10700 nM Bind
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
255 1 3 3 2.4 Oc1cc2c(cc1O)[C@H](c1ccccc1)CNCC2
CHEMBL1201356 drd1_human Human Yes 6.0 IC50 = 1077 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
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
CHEMBL2314734 drd1_human Human No 6.0 IC50 = 1080 nM Funct
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
367 2 0 6 3.0 COc1ccc2c(c1OC(C)=O)CN1CCc3cc4c(cc3C1C2)OCO4
CHEMBL1192581 drd1_rat Rat No 5.0 IC50 = 10900 nM Bind
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
301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1
CHEMBL543838 drd1_rat Rat No 5.0 IC50 = 10900 nM Bind
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
301 8 1 2 4.0 CCCN(CCc1ccccc1)CCc1ccc(F)c(O)c1
CHEMBL1108 drd1_human Human Yes 6.0 IC50 = 1092 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
379 6 1 4 3.7 O=C(CCCN1CC=C(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1
CHEMBL415300 drd1_rat Rat Yes 8.0 IC50 = 11 nM Bind
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
326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1
CHEMBL415300 drd1_rat Rat Yes 8.0 IC50 = 11 nM Bind
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
326 0 1 4 3.7 CN1CCN(C2=Nc3ccccc3Nc3ccc(Cl)cc32)CC1
CHEMBL25856 drd1_rat Rat Yes 7.9 IC50 = 11.6 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL54 drd1_human Human Yes 7.0 IC50 = 110 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL119455 drd1_rat Rat No 7.0 IC50 = 110 nM Bind
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
251 0 1 2 3.1 CN1CCc2cccc3c2[C@H]1Cc1cccc(O)c1-3
CHEMBL4564103 drd1_human Human No 7.0 IC50 = 110.7 nM Bind
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
373 2 0 3 4.2 CN1CCC2=C3[C@@H]1CC4=C(C3=C(C=C2)Br)C(=C(C=C4)OC)OC
CHEMBL2203622 drd1_human Human No 6.0 IC50 = 1100 nM Funct
Antagonist activity at dopamine D1 receptorAntagonist activity at dopamine D1 receptor
298 0 0 4 4.0 Cn1c2cnc1OCC/C=C\CCCCOc1ccccc1-2
CHEMBL136683 drd1_rat Rat No 6.0 IC50 = 1100 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
358 2 1 2 4.7 CC1(C)CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CCN1
CHEMBL1190039 drd1_rat Rat No 5.0 IC50 = 11100 nM Bind
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
225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1
CHEMBL540036 drd1_rat Rat No 5.0 IC50 = 11100 nM Bind
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
225 6 1 2 2.8 CCCN(CC)CCc1ccc(F)c(O)c1
CHEMBL1186001 drd1_rat Rat No 5.0 IC50 = 11100 nM Bind
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
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
CHEMBL445011 drd1_rat Rat No 5.0 IC50 = 11100 nM Bind
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
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
CHEMBL1200710 drd1_human Human Yes 6.0 IC50 = 1113 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL415 drd1_human Human Yes 6.0 IC50 = 1113 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
314 4 0 2 4.5 CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21
CHEMBL82706 drd1_rat Rat No 6.0 IC50 = 1120 nM Bind
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.
243 4 3 3 2.4 NCC(Cc1ccccc1)c1ccc(O)c(O)c1
CHEMBL326263 drd1_human Human No 6.0 IC50 = 1120 nM Bind
Inhibition of human dopamine receptor D1Inhibition of human dopamine receptor D1
503 9 0 4 5.7 N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1
CHEMBL1190552 drd1_rat Rat Yes 5.0 IC50 = 11200 nM Bind
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1
CHEMBL541096 drd1_rat Rat Yes 5.0 IC50 = 11200 nM Bind
Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membraneInhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane
333 8 2 3 4.2 CCCN(CCc1cccc(O)c1)CCc1ccc(Cl)c(O)c1
CHEMBL2057442 drd1_human Human No 6.9 IC50 = 113.8 nM Bind
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
385 5 1 6 2.9 COc1cc2c(cc1OC)[C@@H]1Cc3c(CO)c(OC)cc(OC)c3CN1CC2
CHEMBL2057441 drd1_human Human No 6.9 IC50 = 113.8 nM Bind
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.
355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)cc3[C@@H]1C2
CHEMBL133615 drd1_rat Rat No 6.0 IC50 = 1130 nM Bind
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
369 2 1 2 3.8 Oc1cccc2c1CC[C@@H]1[C@@H]2CCCN1C/C=C/I
CHEMBL1190633 drd1_rat Rat No 4.9 IC50 = 11400 nM Bind
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
239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1
CHEMBL541304 drd1_rat Rat No 4.9 IC50 = 11400 nM Bind
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
239 7 1 2 3.2 CCCN(CCC)CCc1ccc(F)c(O)c1
CHEMBL111348 drd1_rat Rat No 6.9 IC50 = 115 nM Bind
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
265 0 1 2 3.3 CN1Cc2ccccc2[C@@H]2c3cc(O)ccc3CC[C@H]21
CHEMBL1255837 drd1_human Human Yes 5.9 IC50 = 1179 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
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
CHEMBL601773 drd1_human Human Yes 5.9 IC50 = 1179 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
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
CHEMBL2057446 drd1_human Human No 4.9 IC50 = 11840 nM Funct
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
385 5 0 6 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(OC)c(OC)c3[C@@H]1C2
CHEMBL508112 drd1_human Human Yes 5.9 IC50 = 1189 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
332 3 0 6 5.7 c1ccc2sc(SSc3nc4ccccc4s3)nc2c1
CHEMBL305660 drd1_human Human Yes 5.9 IC50 = 1192.9 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1
CHEMBL307717 drd1_rat Rat No 7.9 IC50 = 12 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
328 2 0 2 3.8 CN1CCN(C2CC(c3ccc(F)cc3)c3ccc(F)cc32)CC1
CHEMBL317982 drd1_rat Rat No 7.9 IC50 = 12 nM Bind
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
341 2 0 1 5.4 CN1CCC(C2=CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC1
CHEMBL25856 drd1_rat Rat Yes 7.9 IC50 = 12 nM Bind
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL487387 drd1_human Human Yes 7.9 IC50 = 12.3 nM Bind
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
327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O
CHEMBL407489 drd1_rat Rat Yes 6.9 IC50 = 120 nM Bind
Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatumDisplacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum
247 1 3 4 2.4 Oc1ccc([C@@H]2CNCc3sccc32)cc1O
CHEMBL132304 drd1_rat Rat No 6.9 IC50 = 120 nM Bind
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
369 2 1 2 3.5 Oc1cccc2c1CC1CCCN(C/C=C/I)C1C2
CHEMBL170974 drd1_rat Rat Yes 5.9 IC50 = 1200 nM Bind
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
277 2 0 1 4.1 c1ccc(CN2CCCC3Cc4ccccc4CC32)cc1
CHEMBL8412 drd1_bovin Bovine Yes 4.9 IC50 = 12000 nM Bind
Binding affinity towards dopamine receptor D1 in calf striatumBinding affinity towards dopamine receptor D1 in calf striatum
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL8412 drd1_bovin Bovine Yes 4.9 IC50 = 12000 nM Bind
Displacement of [3H]raclopride from Dopamine receptor D1 of calf striatumDisplacement of [3H]raclopride from Dopamine receptor D1 of calf striatum
401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1
CHEMBL155246 drd1_rat Rat No 4.9 IC50 = 12100 nM Bind
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.
265 1 0 2 3.4 COc1cccc2c1-c1cccc3c1[C@H](C2)N(C)CC3
CHEMBL14239 drd1_rat Rat No 5.9 IC50 = 1230 nM Bind
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
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
CHEMBL257958 drd1_rat Rat No 4.9 IC50 = 12500 nM Bind
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
337 2 2 5 4.0 COc1c(O)c2c3c(nccc3c1OC)C(C)(C)c1cc(O)ccc1-2
CHEMBL608530 drd1_human Human No 5.9 IC50 = 1251 nM Funct
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
386 4 0 4 4.9 CN1CCCC[C@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21
CHEMBL584 drd1_human Human Yes 4.9 IC50 = 12935 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
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
CHEMBL138745 drd1_rat Rat No 7.9 IC50 = 13 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
372 2 0 2 5.1 CC1CN(C2CC(c3ccc(F)cc3)c3ccc(Cl)cc32)CC(C)N1C
CHEMBL344680 drd1_rat Rat No 7.9 IC50 = 13 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
320 2 0 2 4.3 CN1CCN(C2CC(c3ccccc3)c3ccccc32)CC1(C)C
CHEMBL3917753 drd1_human Human No 7.9 IC50 = 13.3 nM Bind
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.
327 2 2 5 2.8 COc1ccc(OC)c2c1C[C@H]1c3cc(O)c(O)cc3CCN1C2
CHEMBL42 drd1_rat Rat Yes 6.9 IC50 = 130 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL1788129 drd1_rat Rat No 6.9 IC50 = 130 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1
CHEMBL96618 drd1_rat Rat No 6.9 IC50 = 130 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
374 4 1 3 3.7 OCCN1CCN(C2CC(c3ccc(F)cc3)c3cccc(Cl)c32)CC1
CHEMBL42 drd1_rat Rat Yes 6.9 IC50 = 130 nM Bind
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
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL42 drd1_rat Rat Yes 6.9 IC50 = 130 nM Bind
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
326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2
CHEMBL479 drd1_rat Rat Yes 5.9 IC50 = 1300 nM Bind
Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1Affinity for displacement of [3H]clonidine labeled Dopamine receptor D1
370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1
CHEMBL106622 drd1_rat Rat Yes 5.9 IC50 = 1300 nM Bind
Binding affinity against Dopamine receptor D1 from rat brain corpus striatum membraneBinding affinity against Dopamine receptor D1 from rat brain corpus striatum membrane
313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL106622 drd1_rat Rat Yes 5.9 IC50 = 1300 nM Bind
Displacement of [3H]SCH-23390 from rat dopamine D1 receptorDisplacement of [3H]SCH-23390 from rat dopamine D1 receptor
313 2 2 3 3.8 CCCN1CCc2cc(F)cc3c2[C@H]1Cc1ccc(O)c(O)c1-3
CHEMBL73082 drd1_rat Rat No 6.9 IC50 = 133 nM Bind
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
364 1 0 2 5.2 CC(C)=C1c2ccccc2C=C(N2CCN(C)CC2)c2cc(Cl)ccc21
CHEMBL38848 drd1_rat Rat No 5.9 IC50 = 1330 nM Bind
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.
255 4 0 1 4.4 CC(C)=CCN1CCCC(/C=C/c2ccccc2)C1
CHEMBL154709 drd1_rat Rat Yes 4.9 IC50 = 13300 nM Bind
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.
281 1 1 3 3.2 COc1ccc2c(c1O)-c1cccc3c1[C@@H](C2)N(C)CC3
CHEMBL1573438 drd1_human Human Yes 6.9 IC50 = 137 nM Funct
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
386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21
CHEMBL611207 drd1_human Human Yes 6.9 IC50 = 137 nM Funct
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
386 4 0 4 4.9 CN1CCCC[C@@H]1CCN1c2ccccc2Sc2ccc([S+](C)[O-])cc21
CHEMBL150550 drd1_rat Rat Yes 6.9 IC50 = 138.4 nM Bind
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
249 2 1 4 2.5 CCCN1CCC=C2c3nc(N)sc3CC[C@@H]21
CHEMBL2057455 drd1_human Human No 5.9 IC50 = 1380 nM Funct
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
341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2
CHEMBL417608 drd1_human Human No 4.9 IC50 = 13803.8 nM Bind
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
456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1
CHEMBL2057445 drd1_human Human No 7.8 IC50 = 14.3 nM Bind
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
355 4 0 5 3.4 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)cc(OC)c3[C@@H]1C2
CHEMBL2334881 drd1_human Human No 7.8 IC50 = 14.7 nM Bind
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.
339 1 1 5 2.8 COc1c(O)ccc2c1CN1CCc3cc4c(cc3[C@@H]1C2)OCCO4
CHEMBL2057455 drd1_human Human No 5.9 IC50 = 1400 nM Bind
[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.
341 3 1 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc(OC)c(O)cc3[C@@H]1C2
CHEMBL2057443 drd1_human Human No 6.9 IC50 = 141.6 nM Bind
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
339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4
CHEMBL2057443 drd1_human Human No 6.9 IC50 = 141.6 nM Bind
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.
339 2 0 5 3.1 COc1cc2c(c(OC)c1)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4
CHEMBL4589737 drd1_human Human No 5.9 IC50 = 1412.5 nM Bind
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
309 2 0 3 3.8 CC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4476383 drd1_human Human No 5.9 IC50 = 1420 nM Funct
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
295 0 1 4 2.8 Oc1ccc2c(c1)CN1CCc3cc4c(cc3C1C2)OCO4
CHEMBL13816 drd1_rat Rat No 5.9 IC50 = 1420 nM Bind
Displacement of [3H]SCH-23390 from D1 receptor in rat striatumDisplacement of [3H]SCH-23390 from D1 receptor in rat striatum
389 4 2 3 4.1 CN1C[C@H](CNC(=O)OCc2ccccc2)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21
CHEMBL4589737 drd1_human Human No 5.9 IC50 = 1427 nM Bind
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
309 2 0 3 3.8 CC1=C2CCN([C@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL192037 drd1_rat Rat No 4.8 IC50 = 14500 nM Bind
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
220 5 0 2 2.9 CCCN(CCC)[C@H]1CCn2cccc2C1
CHEMBL4579687 drd1_human Human No 5.8 IC50 = 1479.1 nM Bind
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
373 2 0 3 4.2 CN1CCC2=C(C=CC3=C2[C@H]1CC4=C3C(=C(C=C4)OC)OC)Br
CHEMBL4467483 drd1_human Human No 4.8 IC50 = 14791.1 nM Funct
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
373 2 0 3 4.2 CN1CCC2=C3[C@H]1CC4=C(C3=C(C=C2)Br)C(=C(C=C4)OC)OC
CHEMBL25856 drd1_rat Rat Yes 6.8 IC50 = 149 nM Bind
Tested for its affinity towards Dopamine receptor D1 in rat striatal membraneTested for its affinity towards Dopamine receptor D1 in rat striatal membrane
267 0 3 3 2.6 Oc1cc2c(cc1O)[C@H]1c3ccccc3CN[C@@H]1CC2
CHEMBL723 drd1_human Human Yes 5.8 IC50 = 1498 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O
CHEMBL3906676 drd1_human Human No 5.8 IC50 = 1499.9 nM Bind
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.
327 2 2 5 2.8 COc1cc2c(cc1OC)CN1CCc3cc(O)c(O)cc3C1C2
CHEMBL137960 drd1_rat Rat Yes 7.8 IC50 = 15 nM Bind
Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.Binding affinity for dopamine receptor D1, activity is expressed as IC50 values.
354 2 0 2 4.9 CN1CCN(C2CC(c3ccccc3)c3ccc(Cl)cc32)CC1(C)C
CHEMBL54 drd1_rat Rat Yes 5.8 IC50 = 1500 nM Funct
Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activityInhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl
CHEMBL4442011 drd1_human Human No 5.8 IC50 = 1513.6 nM Bind
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
323 3 0 3 4.0 CCC1=C2CCN([C@@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL4442011 drd1_human Human No 5.8 IC50 = 1522 nM Bind
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
323 3 0 3 4.0 CCC1=C2CCN([C@@H]3C2=C(C=C1)C4=C(C3)C=CC(=C4OC)OC)C
CHEMBL461571 drd1_human Human No 5.8 IC50 = 1530 nM Bind
Displacement of radioligand from dopamine D1 receptorDisplacement of radioligand from dopamine D1 receptor
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
CHEMBL1626 drd1_human Human Yes 5.8 IC50 = 1535 nM Bind
DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390)
343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C
CHEMBL1185978 drd1_rat Rat No 4.8 IC50 = 15400 nM Bind
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
608 3 1 8 6.9