Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 1218 | 3616 | None | 23 | Human | Functional | pEC50 | = | 8.9 | 8.9 | 295 | 4 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 289 | 1 | 3 | 3 | 3.0 | Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 | 10.1021/acsmedchemlett.9b00050 | ||
| 938 | 3616 | None | 23 | Human | Functional | pEC50 | = | 8.9 | 8.9 | 295 | 4 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 289 | 1 | 3 | 3 | 3.0 | Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 | 10.1021/acsmedchemlett.9b00050 | ||
| CHEMBL353335 | 3616 | None | 23 | Human | Functional | pEC50 | = | 8.9 | 8.9 | 295 | 4 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 289 | 1 | 3 | 3 | 3.0 | Oc1c(O)cc2c(c1Cl)CCNCC2c1ccccc1 | 10.1021/acsmedchemlett.9b00050 | ||
| 86764103 | 132505 | None | 15 | Human | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 2 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 389 | 5 | 1 | 6 | 3.1 | Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C | 10.1021/acsmedchemlett.9b00050 | ||
| CHEMBL3697578 | 132505 | None | 15 | Human | Functional | pEC50 | = | 7.9 | 7.9 | -2 | 2 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 389 | 5 | 1 | 6 | 3.1 | Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C | 10.1021/acsmedchemlett.9b00050 | ||
| 11938 | 2412 | None | 8 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -69 | 4 | Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay |
ChEMBL | 443 | 4 | 1 | 4 | 4.4 | C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl | 10.1021/acs.jmedchem.1c01887 | ||
| 146192952 | 2412 | None | 8 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -69 | 4 | Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay |
ChEMBL | 443 | 4 | 1 | 4 | 4.4 | C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl | 10.1021/acs.jmedchem.1c01887 | ||
| CHEMBL4468760 | 2412 | None | 8 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -69 | 4 | Agonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assayAgonist activity at mouse D5 receptor expressed in HEK293 cells assessed as increase in cyclic AMP production measured after 60 mins by HTRF assay |
ChEMBL | 443 | 4 | 1 | 4 | 4.4 | C[C@H]1c2cccc(c3cn(C)nc3)c2C[C@H](CO)N1C(=O)Cc1c(Cl)cccc1Cl | 10.1021/acs.jmedchem.1c01887 | ||
| 681 | 1465 | None | 47 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 1 | 15 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 153 | 2 | 3 | 3 | 0.6 | NCCc1ccc(c(c1)O)O | 10.1021/acsmedchemlett.9b00050 | ||
| 681.0 | 1465 | None | 47 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 1 | 15 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 153 | 2 | 3 | 3 | 0.6 | NCCc1ccc(c(c1)O)O | 10.1021/acsmedchemlett.9b00050 | ||
| 940 | 1465 | None | 47 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 1 | 15 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 153 | 2 | 3 | 3 | 0.6 | NCCc1ccc(c(c1)O)O | 10.1021/acsmedchemlett.9b00050 | ||
| 947 | 1465 | None | 47 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 1 | 15 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 153 | 2 | 3 | 3 | 0.6 | NCCc1ccc(c(c1)O)O | 10.1021/acsmedchemlett.9b00050 | ||
| CHEMBL59 | 1465 | None | 47 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 1 | 15 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 153 | 2 | 3 | 3 | 0.6 | NCCc1ccc(c(c1)O)O | 10.1021/acsmedchemlett.9b00050 | ||
| DB00988 | 1465 | None | 47 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 1 | 15 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 153 | 2 | 3 | 3 | 0.6 | NCCc1ccc(c(c1)O)O | 10.1021/acsmedchemlett.9b00050 | ||
| 75202022 | 170913 | None | 5 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 2 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 363 | 3 | 1 | 6 | 3.3 | Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C | 10.1021/acsmedchemlett.9b00050 | ||
| CHEMBL4453318 | 170913 | None | 5 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -1 | 2 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assayAgonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay |
ChEMBL | 363 | 3 | 1 | 6 | 3.3 | Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)c(=O)[nH]c(=O)n1C | 10.1021/acsmedchemlett.9b00050 | ||
| 11681599 | 75199 | None | 0 | Human | Functional | pKi | = | 10.3 | 10.3 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 301 | 0 | 1 | 2 | 3.7 | CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 | 10.1021/jm051237e | ||
| CHEMBL203637 | 75199 | None | 0 | Human | Functional | pKi | = | 10.3 | 10.3 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 301 | 0 | 1 | 2 | 3.7 | CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 | 10.1021/jm051237e | ||
| 11623343 | 140929 | None | 0 | Human | Functional | pKi | = | 9.3 | 9.3 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 283 | 0 | 2 | 3 | 2.7 | CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 | 10.1021/jm051237e | ||
| CHEMBL381936 | 140929 | None | 0 | Human | Functional | pKi | = | 9.3 | 9.3 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 283 | 0 | 2 | 3 | 2.7 | CN1CCc2cc(O)ccc2Cc2ccc(O)cc2CC1 | 10.1021/jm051237e | ||
| 11493746 | 141410 | None | 0 | Human | Functional | pKi | = | 8.9 | 8.9 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 335 | 0 | 1 | 2 | 4.3 | CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 | 10.1021/jm051237e | ||
| CHEMBL383451 | 141410 | None | 0 | Human | Functional | pKi | = | 8.9 | 8.9 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 335 | 0 | 1 | 2 | 4.3 | CN1CCc2ccccc2Cc2cc(Cl)c(O)c(Cl)c2CC1 | 10.1021/jm051237e | ||
| 11595240 | 140275 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 301 | 0 | 1 | 2 | 3.7 | CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 | 10.1021/jm051237e | ||
| CHEMBL380464 | 140275 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 301 | 0 | 1 | 2 | 3.7 | CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 | 10.1021/jm051237e | ||
| 11558055 | 73177 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | 10.1021/jm051237e | ||
| CHEMBL1204122 | 73177 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | 10.1021/jm051237e | ||
| CHEMBL201170 | 73177 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | 10.1021/jm051237e | ||
| 11558055 | 73177 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | 10.1021/jm050846j | ||
| CHEMBL1204122 | 73177 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | 10.1021/jm050846j | ||
| CHEMBL201170 | 73177 | None | 0 | Human | Functional | pKi | = | 8.8 | 8.8 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | 10.1021/jm050846j | ||
| 11522339 | 75278 | None | 0 | Human | Functional | pKi | = | 8.0 | 8.0 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2c(O)cccc2CC1 | 10.1021/jm051237e | ||
| CHEMBL203689 | 75278 | None | 0 | Human | Functional | pKi | = | 8.0 | 8.0 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 267 | 0 | 1 | 2 | 3.0 | CN1CCc2ccccc2Cc2c(O)cccc2CC1 | 10.1021/jm051237e | ||
| 11500677 | 140935 | None | 0 | Human | Functional | pKi | = | 6.0 | 6.0 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 281 | 1 | 0 | 2 | 3.3 | COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 | 10.1021/jm051237e | ||
| CHEMBL381946 | 140935 | None | 0 | Human | Functional | pKi | = | 6.0 | 6.0 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 281 | 1 | 0 | 2 | 3.3 | COc1ccc2c(c1)Cc1ccccc1CCN(C)CC2 | 10.1021/jm051237e | ||
| 11573806 | 75443 | None | 0 | Human | Functional | pKi | = | 7.9 | 7.9 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 311 | 2 | 0 | 3 | 3.3 | COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 | 10.1021/jm051237e | ||
| CHEMBL204065 | 75443 | None | 0 | Human | Functional | pKi | = | 7.9 | 7.9 | - | 0 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 311 | 2 | 0 | 3 | 3.3 | COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 | 10.1021/jm051237e | ||
| 5249952 | 73433 | None | 5 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 304 | 1 | 1 | 1 | 4.4 | CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 | 10.1021/jm050846j | ||
| CHEMBL201584 | 73433 | None | 5 | Human | Functional | pKi | = | 7.0 | 7.0 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 304 | 1 | 1 | 1 | 4.4 | CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 | 10.1021/jm050846j | ||
| 4350931 | 169416 | None | 30 | Human | Functional | pKi | = | 7.9 | 7.9 | - | 1 | Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay |
ChEMBL | 290 | 0 | 1 | 1 | 3.8 | CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm060213k | ||
| CHEMBL441618 | 169416 | None | 30 | Human | Functional | pKi | = | 7.9 | 7.9 | - | 1 | Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay |
ChEMBL | 290 | 0 | 1 | 1 | 3.8 | CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm060213k | ||
| 4350931 | 169416 | None | 30 | Human | Functional | pKi | = | 7.9 | 7.9 | - | 1 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 290 | 0 | 1 | 1 | 3.8 | CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm051237e | ||
| CHEMBL441618 | 169416 | None | 30 | Human | Functional | pKi | = | 7.9 | 7.9 | - | 1 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assayInhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay |
ChEMBL | 290 | 0 | 1 | 1 | 3.8 | CN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm051237e | ||
| 42626289 | 148167 | None | 0 | Human | Functional | pKi | = | 6.9 | 6.9 | - | 0 | Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response |
ChEMBL | 379 | 7 | 0 | 4 | 3.3 | COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 | 10.1016/j.bmc.2007.06.002 | ||
| CHEMBL393492 | 148167 | None | 0 | Human | Functional | pKi | = | 6.9 | 6.9 | - | 0 | Antagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium responseAntagonist activity at human Dopamine D5 receptor in HEK293 cells assessed as change in SKF 38393-induced intracellular calcium response |
ChEMBL | 379 | 7 | 0 | 4 | 3.3 | COc1ccccc1N1CCN(CCCCN2Cc3ccccc3C2=O)CC1 | 10.1016/j.bmc.2007.06.002 | ||
| 11566745 | 74720 | None | 0 | Human | Functional | pKi | = | 8.6 | 8.6 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 283 | 0 | 2 | 3 | 2.7 | CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 | 10.1021/jm050846j | ||
| CHEMBL1202298 | 74720 | None | 0 | Human | Functional | pKi | = | 8.6 | 8.6 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 283 | 0 | 2 | 3 | 2.7 | CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 | 10.1021/jm050846j | ||
| CHEMBL203029 | 74720 | None | 0 | Human | Functional | pKi | = | 8.6 | 8.6 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 283 | 0 | 2 | 3 | 2.7 | CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 | 10.1021/jm050846j | ||
| 16090814 | 81612 | None | 0 | Human | Functional | pKi | = | 8.6 | 8.6 | - | 0 | Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay |
ChEMBL | 304 | 0 | 1 | 1 | 4.2 | CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm060213k | ||
| CHEMBL216258 | 81612 | None | 0 | Human | Functional | pKi | = | 8.6 | 8.6 | - | 0 | Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assayActivity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay |
ChEMBL | 304 | 0 | 1 | 1 | 4.2 | CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm060213k | ||
| 11716449 | 141302 | None | 0 | Human | Functional | pKi | = | 7.7 | 7.7 | - | 0 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assayInhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay |
ChEMBL | 304 | 1 | 1 | 1 | 4.2 | CCN1CCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | 10.1021/jm050846j | ||
Showing 1 to 50 of 78 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 3158 | 56283 | None | 21 | Human | Binding | pAC50 | = | 5.8 | 5.8 | - | 20 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 279 | 3 | 0 | 2 | 4.0 | CN(C)CCC=C1c2ccccc2COc2ccccc21 | 10.1038/s41467-023-40064-9 | ||
| 3158.0 | 56283 | None | 21 | Human | Binding | pAC50 | = | 5.8 | 5.8 | - | 20 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 279 | 3 | 0 | 2 | 4.0 | CN(C)CCC=C1c2ccccc2COc2ccccc21 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL1628227 | 56283 | None | 21 | Human | Binding | pAC50 | = | 5.8 | 5.8 | - | 20 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 279 | 3 | 0 | 2 | 4.0 | CN(C)CCC=C1c2ccccc2COc2ccccc21 | 10.1038/s41467-023-40064-9 | ||
| DB01142 | 56283 | None | 21 | Human | Binding | pAC50 | = | 5.8 | 5.8 | - | 20 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 279 | 3 | 0 | 2 | 4.0 | CN(C)CCC=C1c2ccccc2COc2ccccc21 | 10.1038/s41467-023-40064-9 | ||
| 1353 | 1911 | None | 63 | Human | Binding | pAC50 | = | 6.7 | 6.7 | -54 | 85 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 375 | 6 | 1 | 3 | 4.4 | Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl | 10.1038/s41467-023-40064-9 | ||
| 3559 | 1911 | None | 63 | Human | Binding | pAC50 | = | 6.7 | 6.7 | -54 | 85 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 375 | 6 | 1 | 3 | 4.4 | Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl | 10.1038/s41467-023-40064-9 | ||
| 3559.0 | 1911 | None | 63 | Human | Binding | pAC50 | = | 6.7 | 6.7 | -54 | 85 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 375 | 6 | 1 | 3 | 4.4 | Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl | 10.1038/s41467-023-40064-9 | ||
| 86 | 1911 | None | 63 | Human | Binding | pAC50 | = | 6.7 | 6.7 | -54 | 85 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 375 | 6 | 1 | 3 | 4.4 | Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl | 10.1038/s41467-023-40064-9 | ||
| CHEMBL54 | 1911 | None | 63 | Human | Binding | pAC50 | = | 6.7 | 6.7 | -54 | 85 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 375 | 6 | 1 | 3 | 4.4 | Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl | 10.1038/s41467-023-40064-9 | ||
| DB00502 | 1911 | None | 63 | Human | Binding | pAC50 | = | 6.7 | 6.7 | -54 | 85 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 375 | 6 | 1 | 3 | 4.4 | Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl | 10.1038/s41467-023-40064-9 | ||
| 1613 | 2348 | None | 42 | Human | Binding | pAC50 | = | 6.6 | 6.6 | -5 | 44 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 327 | 0 | 0 | 4 | 3.8 | CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 | 10.1038/s41467-023-40064-9 | ||
| 205 | 2348 | None | 42 | Human | Binding | pAC50 | = | 6.6 | 6.6 | -5 | 44 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 327 | 0 | 0 | 4 | 3.8 | CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 | 10.1038/s41467-023-40064-9 | ||
| 3964 | 2348 | None | 42 | Human | Binding | pAC50 | = | 6.6 | 6.6 | -5 | 44 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 327 | 0 | 0 | 4 | 3.8 | CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 | 10.1038/s41467-023-40064-9 | ||
| 3964.0 | 2348 | None | 42 | Human | Binding | pAC50 | = | 6.6 | 6.6 | -5 | 44 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 327 | 0 | 0 | 4 | 3.8 | CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL831 | 2348 | None | 42 | Human | Binding | pAC50 | = | 6.6 | 6.6 | -5 | 44 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 327 | 0 | 0 | 4 | 3.8 | CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 | 10.1038/s41467-023-40064-9 | ||
| DB00408 | 2348 | None | 42 | Human | Binding | pAC50 | = | 6.6 | 6.6 | -5 | 44 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 327 | 0 | 0 | 4 | 3.8 | CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 | 10.1038/s41467-023-40064-9 | ||
| 135398745 | 2914 | None | 65 | Human | Binding | pAC50 | = | 6.4 | 6.4 | -26 | 65 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 312 | 1 | 1 | 5 | 1.7 | CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 135398745.0 | 2914 | None | 65 | Human | Binding | pAC50 | = | 6.4 | 6.4 | -26 | 65 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 312 | 1 | 1 | 5 | 1.7 | CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 47 | 2914 | None | 65 | Human | Binding | pAC50 | = | 6.4 | 6.4 | -26 | 65 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 312 | 1 | 1 | 5 | 1.7 | CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C | 10.1038/s41467-023-40064-9 | ||
| CHEMBL715 | 2914 | None | 65 | Human | Binding | pAC50 | = | 6.4 | 6.4 | -26 | 65 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 312 | 1 | 1 | 5 | 1.7 | CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C | 10.1038/s41467-023-40064-9 | ||
| DB00334 | 2914 | None | 65 | Human | Binding | pAC50 | = | 6.4 | 6.4 | -26 | 65 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 312 | 1 | 1 | 5 | 1.7 | CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 191 | 403 | None | 60 | Human | Binding | pAC50 | = | 6.3 | 6.3 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 313 | 0 | 1 | 4 | 3.4 | Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 | 10.1038/s41467-023-40064-9 | ||
| 201 | 403 | None | 60 | Human | Binding | pAC50 | = | 6.3 | 6.3 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 313 | 0 | 1 | 4 | 3.4 | Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 | 10.1038/s41467-023-40064-9 | ||
| 2170 | 403 | None | 60 | Human | Binding | pAC50 | = | 6.3 | 6.3 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 313 | 0 | 1 | 4 | 3.4 | Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 | 10.1038/s41467-023-40064-9 | ||
| 2170.0 | 403 | None | 60 | Human | Binding | pAC50 | = | 6.3 | 6.3 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 313 | 0 | 1 | 4 | 3.4 | Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 | 10.1038/s41467-023-40064-9 | ||
| CHEMBL1113 | 403 | None | 60 | Human | Binding | pAC50 | = | 6.3 | 6.3 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 313 | 0 | 1 | 4 | 3.4 | Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 | 10.1038/s41467-023-40064-9 | ||
| DB00543 | 403 | None | 60 | Human | Binding | pAC50 | = | 6.3 | 6.3 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 313 | 0 | 1 | 4 | 3.4 | Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 | 10.1038/s41467-023-40064-9 | ||
| 2284 | 3182 | None | 26 | Human | Binding | pAC50 | = | 5.2 | 5.2 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 284 | 4 | 0 | 3 | 4.2 | CN(CCCN1c2ccccc2Sc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 4926 | 3182 | None | 26 | Human | Binding | pAC50 | = | 5.2 | 5.2 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 284 | 4 | 0 | 3 | 4.2 | CN(CCCN1c2ccccc2Sc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 7281 | 3182 | None | 26 | Human | Binding | pAC50 | = | 5.2 | 5.2 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 284 | 4 | 0 | 3 | 4.2 | CN(CCCN1c2ccccc2Sc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| CHEMBL564 | 3182 | None | 26 | Human | Binding | pAC50 | = | 5.2 | 5.2 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 284 | 4 | 0 | 3 | 4.2 | CN(CCCN1c2ccccc2Sc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| DB00420 | 3182 | None | 26 | Human | Binding | pAC50 | = | 5.2 | 5.2 | - | 28 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 284 | 4 | 0 | 3 | 4.2 | CN(CCCN1c2ccccc2Sc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 1427 | 2013 | None | 42 | Human | Binding | pAC50 | = | 5.1 | 5.1 | - | 26 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 280 | 4 | 0 | 2 | 3.9 | CN(CCCN1c2ccccc2CCc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 357 | 2013 | None | 42 | Human | Binding | pAC50 | = | 5.1 | 5.1 | - | 26 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 280 | 4 | 0 | 2 | 3.9 | CN(CCCN1c2ccccc2CCc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 3696 | 2013 | None | 42 | Human | Binding | pAC50 | = | 5.1 | 5.1 | - | 26 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 280 | 4 | 0 | 2 | 3.9 | CN(CCCN1c2ccccc2CCc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| CHEMBL11 | 2013 | None | 42 | Human | Binding | pAC50 | = | 5.1 | 5.1 | - | 26 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 280 | 4 | 0 | 2 | 3.9 | CN(CCCN1c2ccccc2CCc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| DB00458 | 2013 | None | 42 | Human | Binding | pAC50 | = | 5.1 | 5.1 | - | 26 | Binding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human DRD5 in an in vitro assay with cellular components measured by membrane filtration |
ChEMBL | 280 | 4 | 0 | 2 | 3.9 | CN(CCCN1c2ccccc2CCc2c1cccc2)C | 10.1038/s41467-023-40064-9 | ||
| 85090335 | 181220 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 359 | 3 | 0 | 5 | 3.4 | CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 | 10.1016/j.bmcl.2020.127696 | ||
| CHEMBL4760355 | 181220 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 359 | 3 | 0 | 5 | 3.4 | CC(C)Cc1nc2c(c(=O)c3ccccc3n2C)c(=O)n1-c1ccccc1 | 10.1016/j.bmcl.2020.127696 | ||
| 168295528 | 193140 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | -4 | 20 | Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis |
ChEMBL | 333 | 6 | 4 | 5 | 0.9 | N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 | 10.1021/acs.jmedchem.1c00692 | ||
| CHEMBL5206565 | 193140 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | -4 | 20 | Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis |
ChEMBL | 333 | 6 | 4 | 5 | 0.9 | N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 | 10.1021/acs.jmedchem.1c00692 | ||
| CHEMBL5222872 | 193140 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | -4 | 20 | Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis |
ChEMBL | 333 | 6 | 4 | 5 | 0.9 | N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 | 10.1021/acs.jmedchem.1c00692 | ||
| 85090318 | 179551 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 413 | 3 | 0 | 5 | 4.7 | Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 | 10.1016/j.bmcl.2020.127696 | ||
| CHEMBL4740497 | 179551 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 413 | 3 | 0 | 5 | 4.7 | Cc1ccc(-n2c(CC3CCCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 | 10.1016/j.bmcl.2020.127696 | ||
| 168290235 | 193077 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | -16 | 20 | Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis |
ChEMBL | 315 | 6 | 4 | 3 | 1.1 | C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 | 10.1021/acs.jmedchem.1c00692 | ||
| CHEMBL5201074 | 193077 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | -16 | 20 | Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis |
ChEMBL | 315 | 6 | 4 | 3 | 1.1 | C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 | 10.1021/acs.jmedchem.1c00692 | ||
| CHEMBL5222491 | 193077 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | -16 | 20 | Displacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysisDisplacement of [3H]SCH23390 from human D5 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 60 mins by scintillation counting analysis |
ChEMBL | 315 | 6 | 4 | 3 | 1.1 | C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1 | 10.1021/acs.jmedchem.1c00692 | ||
| 85090319 | 180716 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 401 | 3 | 0 | 6 | 3.9 | COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 | 10.1016/j.bmcl.2020.127696 | ||
| CHEMBL4754602 | 180716 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 401 | 3 | 0 | 6 | 3.9 | COc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 | 10.1016/j.bmcl.2020.127696 | ||
| 85090328 | 181141 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM)Positive allosteric modulator activity at human dopamine D5 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 = 81.7 nM) |
ChEMBL | 385 | 2 | 0 | 5 | 4.2 | Cc1ccc(-n2c(C3CCCC3)nc3c(c(=O)c4ccccc4n3C)c2=O)cc1 | 10.1016/j.bmcl.2020.127696 | ||
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