Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10456166 119128 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL346692 119128 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL4285942 119128 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
52937876 60846 0 None 489 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
CHEMBL1765633 60846 0 None 489 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation countingAgonist activity at human dopamine D3 receptor expressed in HEK293 cells co-expressing Galphao1 assessed as incorporation of [35S]GTPgammaS into Galphao1 after 30 mins by scintillation counting
ChEMBL 430 10 1 4 4.8 CCCN(CCCCNC(=O)c1ccc(-c2ccccc2)cc1)[C@H]1CCn2nccc2C1 10.1021/jm101639t
24866114 178111 0 None 223 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
CHEMBL468017 178111 0 None 223 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 7 1 6 4.4 CCCN(CCN1CCN(c2cccc(Cl)c2Cl)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
24754400 154063 0 None 19 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL399164 154063 0 None 19 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 423 8 1 5 3.8 CCCN(CCN1CCN(c2ccccc2OC)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
24936081 178061 0 None 234 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
CHEMBL467540 178061 0 None 234 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2nc(N)sc2C1 10.1021/jm701524h
24866612 189029 0 None 72 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL514885 189029 0 None 72 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
2 3210 19 None 2 7 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1039/C8MD00237A
54562 3210 19 None 2 7 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1039/C8MD00237A
CHEMBL240773 3210 19 None 2 7 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1039/C8MD00237A
56941366 105219 0 None 158 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
CHEMBL3125990 105219 0 None 158 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 491 8 2 7 4.5 CCCN(CCN1CCN(c2ccc(-c3cccc(O)c3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm401883v
681 1437 65 None -2 12 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
940 1437 65 None -2 12 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
947 1437 65 None -2 12 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
CHEMBL59 1437 65 None -2 12 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
DB00988 1437 65 None -2 12 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.9b01835
24742011 93878 0 None 18 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
CHEMBL250552 93878 0 None 18 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2c(O)cccc2C1 10.1021/jm070860r
128 149 9 None 9 3 Human 9.9 pEC50 = 9.9 Functional
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
172267 149 9 None 9 3 Human 9.9 pEC50 = 9.9 Functional
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
CHEMBL273273 149 9 None 9 3 Human 9.9 pEC50 = 9.9 Functional
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1016/j.bmc.2009.04.031
119570 3110 90 None 1 7 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
2233 3110 90 None 1 7 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
953 3110 90 None 1 7 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
CHEMBL301265 3110 90 None 1 7 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
DB00413 3110 90 None 1 7 Rat 9.7 pEC50 = 9.7 Functional
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assayEffective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm000087z
17449900 139012 12 None 1 3 Human 9.7 pEC50 = 9.7 Functional
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
CHEMBL379602 139012 12 None 1 3 Human 9.7 pEC50 = 9.7 Functional
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 348 5 0 5 3.2 COc1ccccc1N1CCN(Cc2cnn(-c3ccccc3)c2)CC1 10.1016/j.bmcl.2006.02.075
52941006 16918 0 None 208 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2c(O)cccc2C1 10.1016/j.bmc.2010.06.025
CHEMBL1254947 16918 0 None 208 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2c(O)cccc2C1 10.1016/j.bmc.2010.06.025
60148494 80448 0 None 446 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152747 80448 0 None 446 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
60165801 80447 0 None 446 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
CHEMBL2152746 80447 0 None 446 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2cc3ccccc3[nH]2)CC1)C1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
85470564 156281 0 None 37 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4071240 156281 0 None 37 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
137633863 156084 0 None 12 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156084 0 None 12 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
137633863 156084 0 None 12 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4069145 156084 0 None 12 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(/C=N/O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
132578416 173234 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4538230 173234 0 None -1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 383 9 3 4 4.8 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2016.08.021
25256816 181026 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477206 181026 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 407 7 0 4 3.7 COc1ccccc1N1CCN(CCCCN2CCCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
5311346 202453 22 None 467 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL1256778 202453 22 None 467 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
CHEMBL70565 202453 22 None 467 5 Rat 9.4 pEC50 = 9.4 Functional
Agonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]-thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 249 2 1 4 1.9 CCCN1CCO[C@@H]2c3cc(O)ccc3OC[C@H]21 10.1021/jm0000113
9888555 165052 11 None - 1 Human 9.4 pEC50 = 9.4 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
CHEMBL424294 165052 11 None - 1 Human 9.4 pEC50 = 9.4 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 423 8 1 5 4.2 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3s2)CC1 10.1021/jm025558r
2 3210 19 None 2 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01835
54562 3210 19 None 2 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01835
CHEMBL240773 3210 19 None 2 7 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b01835
137651936 156850 0 None 5 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156850 0 None 5 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137651936 156850 0 None 5 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4078348 156850 0 None 5 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccn2nccc2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 158534 0 None 4 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158534 0 None 4 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
137660837 158534 0 None 4 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
CHEMBL4097330 158534 0 None 4 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 393 9 1 5 4.5 CCCN(CCCCOc1ccc2ccnn2c1)[C@H]1CCc2c(O)cccc2C1 10.1021/acs.jmedchem.6b01857
45486325 196743 0 None 158 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2ccnc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL577073 196743 0 None 158 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2ccnc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
45486330 196115 0 None 173 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL571992 196115 0 None 173 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
45486328 195686 0 None 25 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
CHEMBL569107 195686 0 None 25 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2cccc3ncccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm901184n
71459659 83421 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206264 83421 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 534 16 2 4 7.7 CCCN(CCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
11957566 183 20 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
1219 183 20 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
3296 183 20 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
950 183 20 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
CHEMBL285755 183 20 None 1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1021/jm701524h
60148495 80456 0 None 125 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152755 80456 0 None 125 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
11299620 96835 2 None 64 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL269004 96835 2 None 64 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 247 5 1 2 3.4 CCCN(CCC)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
10178704 49391 1 None 17 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm070860r
CHEMBL156639 49391 1 None 17 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm070860r
14465382 156440 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
CHEMBL4073068 156440 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 386 7 2 3 6.2 CCCCCCC(C)(C)c1cc(O)c2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
45140376 198974 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
CHEMBL599635 198974 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2ccc(O)cc2C1 10.1021/jm901618d
155522454 170148 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4452046 170148 0 None 2 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 403 10 2 6 4.4 CCCN(CCCCCc1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
119570 3110 90 None -1 7 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
2233 3110 90 None -1 7 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
953 3110 90 None -1 7 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
CHEMBL301265 3110 90 None -1 7 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
DB00413 3110 90 None -1 7 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/acs.jmedchem.1c00692
45486330 196115 0 None 173 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL571992 196115 0 None 173 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
45486330 196115 0 None 173 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
CHEMBL571992 196115 0 None 173 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 450 7 1 7 3.7 CCCN(CCN1CCN(c2nccc3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2013.03.059
127038171 136400 0 None 46 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742140 136400 0 None 46 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742430 136400 0 None 46 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
137460109 190789 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS bindingAgonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS binding
ChEMBL 482 7 2 4 5.4 CCCN(CCN1CCN(c2ccc3c(c2)[nH]c2ccccc23)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5192367 190789 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS bindingAgonist activity at dopamine D3 receptor (unknown origin) assessed as increase in GTPgammaS binding
ChEMBL 482 7 2 4 5.4 CCCN(CCN1CCN(c2ccc3c(c2)[nH]c2ccccc23)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.ejmech.2022.114378
60148496 80453 0 None 100 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2c[nH]c3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152752 80453 0 None 100 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 466 7 2 6 3.2 CCCN(CCN1CCN(C(=O)c2c[nH]c3ccccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
681 1437 65 None -2 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
940 1437 65 None -2 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
947 1437 65 None -2 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
CHEMBL59 1437 65 None -2 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
DB00988 1437 65 None -2 12 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.1c00611
85470564 156281 0 None 37 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4071240 156281 0 None 37 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466573 157990 0 None 16 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4091498 157990 0 None 16 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466716 160456 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099236 160456 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116199 160456 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
85469680 156174 0 None 5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156174 0 None 5 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
71459660 83422 0 None -2 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
CHEMBL2206265 83422 0 None -2 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay
ChEMBL 548 17 2 4 8.1 CCCN(CCCCCCCCCCN(CCC)[C@H]1CCc2c(O)cccc2C1)[C@H]1CCc2c(O)cccc2C1 10.1021/ml3002117
11957566 183 20 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
1219 183 20 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
3296 183 20 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
950 183 20 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
CHEMBL285755 183 20 None 1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assayAgonist activity at dopamine D3 receptor in human U2OS-D3 cells assessed as EA-tagged beta-arrestin translocation after 1.5 hrs by luminescence based beta-galactosidase assay
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cc(cc2)O)CCC 10.1016/j.bmc.2012.08.058
44427827 92843 0 None 15 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
CHEMBL244990 92843 0 None 15 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 498 8 2 5 4.4 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(-c2ccccn2)cc1 10.1021/jm0704200
119570 3110 90 None -1 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
2233 3110 90 None -1 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
953 3110 90 None -1 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
CHEMBL301265 3110 90 None -1 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
DB00413 3110 90 None -1 7 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/j.bmcl.2007.10.059
57242 3208 16 None 9 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
954 3208 16 None 9 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
CHEMBL155731 3208 16 None 9 4 Human 9.0 pEC50 = 9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 246 2 1 4 1.6 CCCN1CCC[C@H]2[C@H]1Cc1cnc(nc1C2)N 10.1016/j.bmcl.2007.10.059
85469680 156174 0 None 5 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156174 0 None 5 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466574 158048 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158048 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466574 158048 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
CHEMBL4092052 158048 0 None 3 2 Human 9.0 pEC50 = 9 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1016/j.ejmech.2019.111975
16038360 16788 0 None 104 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1 10.1016/j.bmc.2010.06.025
CHEMBL1253770 16788 0 None 104 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 469 8 1 4 5.5 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)C1CCc2ccc(O)cc2C1 10.1016/j.bmc.2010.06.025
10411237 116979 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL339960 116979 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
CHEMBL4287055 116979 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assayAgonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 444 7 2 3 4.8 O=C(NCCCCN1CCN(c2ccc(Cl)cc2Cl)CC1)c1cc2ccccc2[nH]1 10.1039/C8MD00237A
137660062 158839 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 370 7 1 2 6.5 CCCCCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
CHEMBL4100634 158839 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 370 7 1 2 6.5 CCCCCCC(C)(C)c1ccc2c(c1)OC(C)(C)[C@@H]1CCC(CO)=C[C@@H]21 10.1021/acs.jmedchem.6b01578
10368423 97478 0 None - 1 Green monkey 8.9 pEC50 = 8.9 Functional
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 493 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)cc2)CC1 10.1021/jm030836n
CHEMBL27254 97478 0 None - 1 Green monkey 8.9 pEC50 = 8.9 Functional
Effective concentration for Dopamine receptor D3 was determinedEffective concentration for Dopamine receptor D3 was determined
ChEMBL 493 8 1 4 3.6 COc1ccccc1N1CCN(CCCCNC(=O)c2ccc(I)cc2)CC1 10.1021/jm030836n
155531663 171103 0 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1cc(O)ccc1O)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4466245 171103 0 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1cc(O)ccc1O)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
45273211 193954 0 None 33 2 Human 8.9 pEC50 = 8.9 Functional
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2009.04.031
CHEMBL556269 193954 0 None 33 2 Human 8.9 pEC50 = 8.9 Functional
Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS bindingActivity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 460 7 2 4 3.9 CCCN(CCN1CCN(C(=O)c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2c(O)cccc2C1 10.1016/j.bmc.2009.04.031
128 149 9 None 9 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
172267 149 9 None 9 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
CHEMBL273273 149 9 None 9 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 10.1021/jm901184n
60148497 80440 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL2152633 80440 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 438 7 2 6 3.6 CCCN(CCN1CCN(c2ccc3[nH]ccc3c2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
2 3210 19 None 2 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2010.12.083
54562 3210 19 None 2 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2010.12.083
CHEMBL240773 3210 19 None 2 7 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmcl.2010.12.083
90467024 157147 0 None 10 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157147 0 None 10 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
2 3210 19 None 2 7 Human 8.9 pEC50 = 8.9 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
54562 3210 19 None 2 7 Human 8.9 pEC50 = 8.9 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
CHEMBL240773 3210 19 None 2 7 Human 8.9 pEC50 = 8.9 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050170s
10476504 33268 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
CHEMBL142020 33268 1 None - 1 Human 8.9 pEC50 = 8.9 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 6 2.7 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccn3n2)CC1 10.1021/jm025558r
127037825 136396 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740041 136396 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742426 136396 0 None 2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 472 7 2 6 4.3 CCCN(CCN1CCN(c2ccc3cc[nH]c3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
24759792 183826 0 None 190 2 Human 8.9 pEC50 = 8.9 Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O 10.1016/j.bmcl.2009.03.015
CHEMBL484598 183826 0 None 190 2 Human 8.9 pEC50 = 8.9 Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 286 2 1 3 2.0 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)CNC4=O 10.1016/j.bmcl.2009.03.015
90467024 157147 0 None 10 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157147 0 None 10 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
60194424 80026 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assay
ChEMBL 511 9 2 7 4.3 CCCN(CC[C@H]1CC[C@H](NS(=O)(=O)c2cccnc2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmcl.2012.07.003
CHEMBL2146499 80026 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by mitogenesis assay
ChEMBL 511 9 2 7 4.3 CCCN(CC[C@H]1CC[C@H](NS(=O)(=O)c2cccnc2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmcl.2012.07.003
119570 3110 90 None -1 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
2233 3110 90 None -1 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
953 3110 90 None -1 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
CHEMBL301265 3110 90 None -1 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
DB00413 3110 90 None -1 7 Human 8.8 pEC50 = 8.8 Functional
Effective concentration required for agonistic activity against human D3 receptorEffective concentration required for agonistic activity against human D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1016/s0960-894x(02)00390-6
10092819 16594 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
CHEMBL124444 16594 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 407 8 1 5 3.8 COc1ccccc1N1CCN(CCCCNC(=O)c2cc3ccccc3o2)CC1 10.1021/jm025558r
24866612 189029 0 None 72 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
CHEMBL514885 189029 0 None 72 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 475 8 1 6 4.8 CCCN(CCN1CCN(c2ccc(-c3ccccc3)cc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/jm300268s
53361666 190027 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 466 7 2 8 3.4 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5181007 190027 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting methodAgonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting method
ChEMBL 466 7 2 8 3.4 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
45140377 198975 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2c(O)cccc2C1 10.1021/jm901618d
CHEMBL599636 198975 0 None 2 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 460 7 2 6 4.0 CCCN(CCN1CCN(c2ccnc3c(O)cccc23)CC1)C1CCc2c(O)cccc2C1 10.1021/jm901618d
137660417 158609 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4098174 158609 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
53475319 83102 7 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrsAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs
ChEMBL 478 8 3 6 4.2 CCCN(CC[C@]1(O)C[C@H](NC(=O)c2ccc3ccccc3c2)C1)[C@H]1CCc2nc(N)sc2C1 10.1021/ml200100t
CHEMBL2203406 83102 7 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrsAgonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirole-induced mitogenesis after 24 hrs
ChEMBL 478 8 3 6 4.2 CCCN(CC[C@]1(O)C[C@H](NC(=O)c2ccc3ccccc3c2)C1)[C@H]1CCc2nc(N)sc2C1 10.1021/ml200100t
2 3210 19 None -4 7 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
54562 3210 19 None -4 7 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
CHEMBL240773 3210 19 None -4 7 Rat 8.8 pEC50 = 8.8 Functional
Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from ratAgonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0000113
2 3210 19 None 2 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
54562 3210 19 None 2 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
CHEMBL240773 3210 19 None 2 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00692
2 3210 19 None 2 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
54562 3210 19 None 2 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
CHEMBL240773 3210 19 None 2 7 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2021.113190
3038495 700 30 None -8 7 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
7625 700 30 None -8 7 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
CHEMBL25236 700 30 None -8 7 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm060138d
3038495 700 30 None -8 7 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
7625 700 30 None -8 7 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
CHEMBL25236 700 30 None -8 7 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm025558r
25071384 111289 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111289 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
25071384 111289 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287397 111289 0 None 251 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
2 3210 19 None 2 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3210 19 None 2 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3210 19 None 2 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3210 19 None 2 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3210 19 None 2 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3210 19 None 2 7 Human 8.7 pEC50 = 8.7 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3210 19 None 2 7 Human 8.0 pEC50 = 8 Functional
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
54562 3210 19 None 2 7 Human 8.0 pEC50 = 8 Functional
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
CHEMBL240773 3210 19 None 2 7 Human 8.0 pEC50 = 8 Functional
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
16078 1335 19 None -1 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
2424 1335 19 None -1 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
4109 1335 19 None -1 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
CHEMBL465 1335 19 None -1 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
DB00470 1335 19 None -1 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 314 4 1 2 5.7 CCCCCc1cc(O)c2c(c1)OC([C@H]1[C@H]2C=C(C)CC1)(C)C 10.1021/acs.jmedchem.6b01578
2402 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
5095 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
7295 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
CHEMBL589 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
DB00268 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1016/j.bmc.2010.06.025
2402 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
5095 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
7295 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
CHEMBL589 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
DB00268 3318 58 None 3 7 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901618d
127047458 139205 0 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 419 7 1 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3798334 139205 0 None 1 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 419 7 1 5 4.1 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
681 1437 65 None -2 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
940 1437 65 None -2 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
947 1437 65 None -2 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
CHEMBL59 1437 65 None -2 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
DB00988 1437 65 None -2 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm401883v
127037828 136399 0 None 30 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3740778 136399 0 None 30 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
CHEMBL3742429 136399 0 None 30 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 469 6 2 7 3.4 N#CCN(CCN1CCN(c2ccc3[nH]ccc3c2Cl)CC1)[C@H]1CCc2nc(N)sc2C1 10.1021/acs.jmedchem.5b01031
77461254 190630 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 477 8 1 8 3.6 CCCN(CCN1CCN(c2ccc(-c3ccccn3)nc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
CHEMBL5189785 190630 0 None -1 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 477 8 1 8 3.6 CCCN(CCN1CCN(c2ccc(-c3ccccn3)nc2)CC1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.ejmech.2022.114378
164609493 183854 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
CHEMBL4846380 183854 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 350 6 4 5 1.9 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1 10.1016/j.ejmech.2021.113190
168292954 192395 0 None -7 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5202592 192395 0 None -7 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222660 192395 0 None -7 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 388 8 4 4 2.5 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1 10.1021/acs.jmedchem.1c00692
168295541 192438 0 None -14 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5208845 192438 0 None -14 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
CHEMBL5222926 192438 0 None -14 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 347 6 4 5 1.4 C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1 10.1021/acs.jmedchem.1c00692
90467323 159011 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4102620 159011 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
122181332 121359 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 121359 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
90467022 155379 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4060896 155379 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 540 9 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4ccccc4C(F)(F)F)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
127045794 139578 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12 10.1039/C5MD00590F
CHEMBL3797771 139578 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800680 139578 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 487 7 2 5 5.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(O)c2ccccc12 10.1039/C5MD00590F
127046015 139582 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12 10.1039/C5MD00590F
CHEMBL3799465 139582 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12 10.1039/C5MD00590F
CHEMBL3800684 139582 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 477 7 1 5 5.9 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2sccc12 10.1039/C5MD00590F
25072635 111291 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111291 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
90467323 159011 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4102620 159011 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 532 11 2 7 4.2 COc1cc(OC(=O)NCCCCN2CCN(c3ccccc3OC)CC2)ccc1-c1cccc(C(N)=O)c1 10.1021/acs.jmedchem.6b01578
11706497 77812 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
CHEMBL210461 77812 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 535 7 1 3 6.2 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccc1CCc1ccc(cc1)CC2 10.1021/jm060138d
25072635 111291 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
CHEMBL3287399 111291 0 None 3 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 446 8 0 6 4.4 O=Cc1cnn2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccc12 10.1021/jm5004039
122181332 121359 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590083 121359 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 432 9 1 3 5.6 CCCN(CCCCNC(=O)/N=N/c1cc(F)c(F)c(F)c1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
164619170 185019 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185019 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164619170 185019 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4863832 185019 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 396 9 2 4 3.8 COc1ccc(F)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
25071692 111297 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111297 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
90467322 156268 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156268 0 None -6 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
25071692 111297 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
CHEMBL3287405 111297 0 None 9 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 7 0 6 4.5 N#Cc1cnn2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc12 10.1021/jm5004039
155516042 175719 0 None 794 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4443039 175719 0 None 794 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4595150 175719 0 None 794 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
164628178 185765 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 185765 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164628178 185765 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 185765 0 None -10 3 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
90467172 156353 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4072140 156353 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 510 7 2 4 6.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
90467317 155250 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.1 O=C(NCCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4059573 155250 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.1 O=C(NCCCCN1CCN(c2ccccc2C(F)(F)F)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
168295528 192429 0 None -56 9 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5206565 192429 0 None -56 9 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222872 192429 0 None -56 9 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 333 6 4 5 0.9 N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
164628178 185765 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 185765 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
164628178 185765 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
CHEMBL4875081 185765 0 None -10 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 412 9 2 4 4.4 COc1ccc(Cl)cc1[C@H]1C[C@@H]1CNCCCOc1ccc2ccc(=O)[nH]c2c1 10.1021/acs.jmedchem.1c01327
9828632 99608 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL287198 99608 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 535 6 1 4 5.5 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
90467173 157653 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 443 8 1 4 5.4 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4087889 157653 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 443 8 1 4 5.4 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
44443903 153544 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 219 3 1 3 2.0 C=CCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL398480 153544 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 219 3 1 3 2.0 C=CCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
168294449 192416 0 None -50 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5204599 192416 0 None -50 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
CHEMBL5222793 192416 0 None -50 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 367 7 4 5 1.9 CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1 10.1021/acs.jmedchem.1c00692
85469680 156174 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4070196 156174 0 None 5 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 526 8 2 5 5.1 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4cccc(Cl)c4Cl)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
90466574 158048 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158048 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
90466425 158767 0 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 158767 0 None 10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
90467319 160489 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4095588 160489 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4116454 160489 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 445 8 1 5 4.7 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3ccccc3)cc2)CC1 10.1021/acs.jmedchem.6b01578
127045797 139581 0 None 21 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2 10.1039/C5MD00590F
CHEMBL3798372 139581 0 None 21 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2 10.1039/C5MD00590F
CHEMBL3800683 139581 0 None 21 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 479 7 1 6 4.5 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc2c1OCCO2 10.1039/C5MD00590F
90466574 158048 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4092052 158048 0 None 3 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 540 9 2 5 5.5 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
127047310 139545 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 433 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3800489 139545 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 433 8 1 5 4.5 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
145988474 166598 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 379 7 2 5 2.8 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(C#N)cc1)CC2 10.1021/acsmedchemlett.8b00229
CHEMBL4290759 166598 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Antagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assayAntagonist activity at human dopamine D3 receptor assessed as inhibition of beta-arrestin recruitment by Tango assay
ChEMBL 379 7 2 5 2.8 COc1cc2c(cc1O)CN(CCCCNC(=O)c1ccc(C#N)cc1)CC2 10.1021/acsmedchemlett.8b00229
154703875 175874 1 None 6 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4586582 175874 1 None 6 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596341 175874 1 None 6 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 471 11 2 2 6.5 CCCN(CCCCNC(=O)c1cc2ccccc2[nH]1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL5077114 212711 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None CCOC(=O)/C=C1\[C@@H]2CCC[C@@]1(c1cccc(O)c1)CCN2C[C@H]1C[C@@H]1CCNC(=O)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.1c00611
136056636 111296 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111296 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
90467021 156129 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156129 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
136056636 111296 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
CHEMBL3287404 111296 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 461 8 1 7 4.4 O/N=C/c1cc2cc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)ccn2n1 10.1021/jm5004039
90467021 156129 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156129 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
164609729 184515 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4856059 184515 0 None 2 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
164612037 184795 0 None 6 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4860528 184795 0 None 6 11 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 326 8 4 4 1.8 CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
90466864 158124 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
CHEMBL4092900 158124 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 496 6 2 4 5.9 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc2c(c1)[nH]c1ccccc12 10.1021/acs.jmedchem.6b01578
90467171 160601 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 160601 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 160601 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
90467171 160601 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 160601 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 160601 0 None -1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
11581443 95954 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1021/jm050729o
CHEMBL26188 95954 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 367 8 1 4 3.0 COc1ccccc1N1CCN(CCCCNC(=O)c2ccccc2)CC1 10.1021/jm050729o
CHEMBL5089655 213446 0 None 63 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None N#CC(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
164616851 184367 0 None 2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4853772 184367 0 None 2 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 376 6 4 4 2.5 Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
137658100 159069 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4103339 159069 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 483 7 1 4 6.0 O=C(NCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
44309775 102205 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
CHEMBL304605 102205 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assayAgonist activity at human dopamine D3 receptor expressed in HEK293 cells by mitogenesis assay
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1021/jm0704200
44309775 102205 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/s0960-894x(03)00389-5
CHEMBL304605 102205 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cellsAgonistic activity of quinpirole stimulation of mitogenesis in human Dopamine receptor D3 transfected CHO cells
ChEMBL 491 6 1 3 5.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc2c(c1)Cc1ccccc1-2 10.1016/s0960-894x(03)00389-5
154705015 175940 1 None 91 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4454380 175940 1 None 91 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4596929 175940 1 None 91 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 482 11 1 2 7.2 CCCN(CCCCNC(=O)c1ccc2ccccc2c1)C[C@@H]1C[C@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
25093832 155339 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155339 0 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
90467171 160601 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4079093 160601 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
CHEMBL4117318 160601 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.6b01578
11678172 77678 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
CHEMBL209876 77678 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 531 8 1 4 5.6 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cc3ccc2CCc2ccc(cc2)CC3)CC1 10.1021/jm060138d
90467171 160601 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
CHEMBL4079093 160601 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
CHEMBL4117318 160601 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
25093832 155339 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4060461 155339 0 None -2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 423 9 1 8 3.1 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(/C=N/O)c3c2)CC1 10.1021/acs.jmedchem.6b01857
90467021 156129 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4069565 156129 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 558 9 2 5 5.6 NC(=O)c1cccc(-c2ccc(OC(=O)NCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2F)c1 10.1021/acs.jmedchem.6b01578
25072941 155933 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 155933 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
11510684 98201 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@@H](c3ccccc3)CC2)CC1 10.1021/jm050729o
CHEMBL277301 98201 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 449 9 1 4 4.7 COc1ccccc1N1CCN(CCCCNC(=O)[C@H]2CC[C@@H](c3ccccc3)CC2)CC1 10.1021/jm050729o
2 3210 19 None 2 7 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assayAgonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2016.07.038
54562 3210 19 None 2 7 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assayAgonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2016.07.038
CHEMBL240773 3210 19 None 2 7 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assayAgonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.ejmech.2016.07.038
25072002 155573 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 155573 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
25072941 155933 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4067439 155933 0 None -1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 408 9 0 7 3.1 COc1ccccc1N1CCN(CCCCOc2ccc3c(C=O)cnn3c2)CC1 10.1021/acs.jmedchem.6b01857
90467024 157147 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4081780 157147 0 None 10 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
25072002 155573 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4063235 155573 0 None 3 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 405 8 0 7 3.2 COc1ccccc1N1CCN(CCCCOc2ccn3ncc(C#N)c3c2)CC1 10.1021/acs.jmedchem.6b01857
127046755 139575 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3798943 139575 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3800677 139575 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 403 6 1 4 4.4 Cc1ccccc1N1CCN(CCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
2402 3318 58 None 3 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
5095 3318 58 None 3 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
7295 3318 58 None 3 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
CHEMBL589 3318 58 None 3 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
DB00268 3318 58 None 3 7 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma bindingAgonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1021/jm901184n
242 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
90466867 155770 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4065510 155770 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
168281746 192280 0 None -77 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5184911 192280 0 None -77 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
CHEMBL5221974 192280 0 None -77 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 365 6 4 5 1.6 CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1 10.1021/acs.jmedchem.1c00692
44436605 148531 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL394292 148531 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 429 7 1 3 4.3 C#Cc1ccc(C(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)cc1 10.1016/j.bmc.2007.08.038
44400674 124669 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
CHEMBL364516 124669 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL None None None None 10.1021/jm050170s
681 1437 65 None -2 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
940 1437 65 None -2 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
947 1437 65 None -2 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
CHEMBL59 1437 65 None -2 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
DB00988 1437 65 None -2 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.8b01096
44436600 91370 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
CHEMBL241212 91370 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrsAgonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs
ChEMBL 391 8 1 4 3.0 C#Cc1ccc(C(=O)NCCCCN2CCN(c3ccccc3OC)CC2)cc1 10.1016/j.bmc.2007.08.038
90466571 158850 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 458 8 2 5 3.8 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4ccccc4)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4100735 158850 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 458 8 2 5 3.8 NC(=O)c1cccc(-c2cccc(OC(=O)NCCCN3CCN(c4ccccc4)CC3)c2)c1 10.1021/acs.jmedchem.6b01578
25139181 183760 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 183760 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
11316847 70004 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm049465g
CHEMBL194493 70004 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 448 7 1 5 4.0 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc([N+](=O)[O-])cc1 10.1021/jm049465g
15389743 183827 0 None 1 3 Human 8.6 pEC50 = 8.6 Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.03.015
CHEMBL484599 183827 0 None 1 3 Human 8.6 pEC50 = 8.6 Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 274 3 1 3 1.9 CCCN1CCO[C@@H]2c3cc(C(N)=O)ccc3CC[C@H]21 10.1016/j.bmcl.2009.03.015
24805287 184191 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 2 0 4 2.5 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)COC4=O 10.1016/j.bmcl.2009.03.015
CHEMBL485128 184191 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assayActivation of human dopamine D3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 287 2 0 4 2.5 CCCN1CCO[C@@H]2c3cc4c(cc3CC[C@H]21)COC4=O 10.1016/j.bmcl.2009.03.015
90466425 158767 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 158767 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
54580906 61276 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771109 61276 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 459 8 0 5 4.6 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccco4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
90466425 158767 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4099798 158767 0 None 10 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 502 10 2 6 4.2 COc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc(-c3cccc(C(N)=O)c3)c2)CC1 10.1021/acs.jmedchem.6b01578
2 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00611
54562 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00611
CHEMBL240773 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c00611
2 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
54562 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
CHEMBL240773 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1016/j.bmc.2014.12.012
122181330 121357 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
CHEMBL3590081 121357 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assayActivation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay
ChEMBL 396 9 1 3 5.3 CCCN(CCCCNC(=O)/N=N/c1ccc(F)cc1)C1Cc2ccccc2C1 10.1016/j.bmc.2014.12.012
90466717 156368 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4072282 156368 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
2 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060138d
54562 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060138d
CHEMBL240773 3210 19 None 2 7 Human 8.6 pEC50 = 8.6 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm060138d
155525527 170501 0 None 8 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4457171 170501 0 None 8 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 389 9 3 6 4.1 CCCN(CCCCCc1ccc(O)c(O)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
90466717 156368 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4072282 156368 0 None 5 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 488 9 2 6 3.8 COc1ccccc1N1CCN(CCCNC(=O)Oc2ccc(-c3cccc(C(N)=O)c3)cc2)CC1 10.1021/acs.jmedchem.6b01578
3038495 700 30 None -8 7 Human 8.6 pEC50 = 8.6 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
7625 700 30 None -8 7 Human 8.6 pEC50 = 8.6 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
CHEMBL25236 700 30 None -8 7 Human 8.6 pEC50 = 8.6 Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptorEffective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm050170s
46893146 61278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771110 61278 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 475 8 0 5 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4cccs4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
10084583 104299 3 None 9 3 Human 8.6 pEC50 = 8.6 Functional
Effective concentration required for agonistic activity against human Dopamine receptor D3Effective concentration required for agonistic activity against human Dopamine receptor D3
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
CHEMBL310867 104299 3 None 9 3 Human 8.6 pEC50 = 8.6 Functional
Effective concentration required for agonistic activity against human Dopamine receptor D3Effective concentration required for agonistic activity against human Dopamine receptor D3
ChEMBL 271 5 0 3 3.3 CCCN(CCC)[C@H]1CCc2nn3ccccc3c2C1 10.1016/s0960-894x(02)00390-6
2 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
54562 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
CHEMBL240773 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
44588497 175062 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)[C@H]1CCc2ccc(O)cc2C1 10.1016/j.ejmech.2022.114378
CHEMBL458088 175062 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at dopamine D3 receptor (unknown origin)Agonist activity at dopamine D3 receptor (unknown origin)
ChEMBL 393 7 1 4 3.8 CCCN(CCN1CCN(c2ccccc2)CC1)[C@H]1CCc2ccc(O)cc2C1 10.1016/j.ejmech.2022.114378
242 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
34 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
60795 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
CHEMBL1112 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
DB01238 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/acs.jmedchem.6b01857
242 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
34 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
60795 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
CHEMBL1112 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
DB01238 467 117 None -5 11 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1021/jm5004039
90466867 155770 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4065510 155770 0 None 5 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 538 8 2 5 5.2 NC(=O)c1cccc(-c2ccc(OC(=O)NC/C=C/CN3CCN(c4cccc(Cl)c4Cl)CC3)cc2)c1 10.1021/acs.jmedchem.6b01578
44438230 93124 3 None -9 2 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246439 93124 3 None -9 2 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 3 2 2 4.6 Cc1[nH]c2ccccc2c1CN1CCC(O)(c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2006.10.076
155563589 174746 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
CHEMBL4573578 174746 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 401 9 2 6 4.5 CCCN(CCC/C=C/c1ccc(O)c(OC)c1)[C@H]1CCc2nc(N)sc2C1 10.1016/j.bmc.2016.08.021
127046238 139157 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 475 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)OC1CCCc2ccccc21 10.1039/C5MD00590F
CHEMBL3798010 139157 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 475 7 1 4 5.7 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)OC1CCCc2ccccc21 10.1039/C5MD00590F
11596603 9841 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm050729o
CHEMBL114541 9841 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 405 7 1 3 4.3 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccccc1 10.1021/jm050729o
127046753 139574 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3799147 139574 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
CHEMBL3800675 139574 0 None 15 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 417 7 1 4 4.8 Cc1ccccc1N1CCN(CCCCNC(=O)Oc2cccc3ccccc23)CC1 10.1039/C5MD00590F
137660417 158609 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4098174 158609 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
42625290 55953 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesisAgonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
ChEMBL 461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
CHEMBL1627316 55953 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesisAgonist activity at human D3 receptor expressed in HEK293 cells assessed as stimulation of mitogenesis
ChEMBL 461 7 2 5 4.0 O=C(NCCC(O)CN1CCN(c2cccc(Cl)c2Cl)CC1)c1cc2ccccc2o1 10.1021/jm900095y
137660417 158609 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
CHEMBL4098174 158609 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 527 9 1 5 6.4 COc1cc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)ccc1-c1ccccc1 10.1021/acs.jmedchem.6b01578
164622330 185280 0 None 11 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
CHEMBL4867962 185280 0 None 11 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 360 6 4 4 2.3 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1 10.1016/j.ejmech.2021.113190
162665657 181794 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 427 7 1 4 4.8 O=C(NC/C=C/CN1CCN(c2ccccc2)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
CHEMBL4785109 181794 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assayPartial agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation by flourescence assay
ChEMBL 427 7 1 4 4.8 O=C(NC/C=C/CN1CCN(c2ccccc2)CC1)Oc1ccc(-c2ccccc2)cc1 10.1016/j.ejmech.2019.111975
164614549 184360 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
CHEMBL4853668 184360 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 340 9 4 4 2.2 CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C 10.1016/j.ejmech.2021.113190
90467322 156268 0 None -6 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156268 0 None -6 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
44438197 152738 2 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL397770 152738 2 None -6 2 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 374 3 2 2 5.0 OC1(c2cccc(Cl)c2Cl)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
90467322 156268 0 None -6 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
CHEMBL4071121 156268 0 None -6 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at recombinant human CB1 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 472 8 2 5 5.0 COc1ccccc1N1CCN(CCCCNC(=O)Oc2ccc3c(c2)[nH]c2ccccc23)CC1 10.1021/acs.jmedchem.6b01578
11307083 63224 0 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm049465g
CHEMBL180060 63224 0 None 6 2 Human 7.6 pEC50 = 7.6 Functional
Inhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cellsInhibition of quinpirole stimulation of mitogenesis at human dopamine D3 receptors expressed in Chinese hamster ovary cells
ChEMBL 529 6 1 3 4.7 O=C(NC/C=C/CN1CCN(c2cccc(Cl)c2Cl)CC1)c1ccc(I)cc1 10.1021/jm049465g
90467170 160607 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4063681 160607 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.6b01578
CHEMBL4117347 160607 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assayAgonist activity at recombinant human dopamine D3 receptor expressed in CHO-K1 cells assessed as increase in cAMP accumulation after 30 mins by HTRF assay
ChEMBL 497 8 1 4 6.4 O=C(NCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)Oc1cccc(-c2ccccc2)c1 10.1021/acs.jmedchem.6b01578
44438228 93123 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
CHEMBL246438 93123 0 None -7 2 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesisAntagonist activity at human dopamine D3 receptor expressed in CHO cells assessed as inhibition of quinpirole stimulated mitogenesis
ChEMBL 354 4 1 2 5.0 COC1(c2ccc(Cl)cc2)CCN(Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2006.10.076
2 3210 19 None 2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050729o
54562 3210 19 None 2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050729o
CHEMBL240773 3210 19 None 2 7 Human 7.6 pEC50 = 7.6 Functional
Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assayIntrinsic activity against dopamine receptor D3 by Eu-GTP binding assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm050729o
127045793 139577 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL3798841 139577 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL3800679 139577 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assayAgonist activity at human dopamine D3 receptor expressed in CHOK1 cells assessed as cAMP levels preincubated for 10 mins followed by addition of adenylyl cyclase activator NKH 477 measured after 45 mins by HTRF functional assay
ChEMBL 501 8 1 5 5.8 COc1ccc(OC(=O)NCCCCN2CCN(c3cccc(Cl)c3Cl)CC2)c2ccccc12 10.1039/C5MD00590F
CHEMBL5073754 212534 0 None 41 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assayAgonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay
ChEMBL None None None CN(C)C(=O)C(CCNCCCCN1CCN(c2cccc(Cl)c2Cl)CC1)(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.1c00611
137659303 158757 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 158757 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
164608815 183872 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
CHEMBL4846638 183872 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 380 7 4 4 2.8 Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1 10.1016/j.ejmech.2021.113190
137659303 158757 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4099711 158757 0 None 9 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 410 9 1 7 2.8 COc1ccccc1N1CCN(CCCCOc2ccn3nc(CO)cc3c2)CC1 10.1021/acs.jmedchem.6b01857
15006491 4492 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 221 3 1 3 2.2 CCCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
CHEMBL102463 4492 2 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulationAgonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
ChEMBL 221 3 1 3 2.2 CCCN1CCOC(c2cccc(O)c2)C1 10.1016/j.bmcl.2007.10.059
15232477 168864 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
CHEMBL442535 168864 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Stimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cellsStimulation of mitogenesis in Dopamine receptor D3 transfected CHO p-5 cells
ChEMBL 501 6 1 4 4.8 COc1c(C(=O)NCCN2CCN(c3cccc(Cl)c3)CC2)cc(Br)c2ccccc12 10.1016/0960-894X(96)00231-4
25072633 158675 0 None -7 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 158675 0 None -7 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
164611757 184320 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
CHEMBL4853107 184320 0 None -3 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay
ChEMBL 402 8 4 4 2.8 Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1 10.1016/j.ejmech.2021.113190
168294767 192417 0 None -87 10 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5207281 192417 0 None -87 10 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5222802 192417 0 None -87 10 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 313 8 4 5 0.9 CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
25072633 158675 0 None -7 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
CHEMBL4098803 158675 0 None -7 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assayAgonist activity at human Dopamine D3 receptor expressed in HEK293T cell membranes coexpressing GalphaoA incubated for 30 mins measured after 75 mins by [35S]GTPgammaS binding assay
ChEMBL 380 8 0 6 3.3 COc1ccccc1N1CCN(CCCCOc2ccc3ccnn3c2)CC1 10.1021/acs.jmedchem.6b01857
154726381 175953 1 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4522558 175953 1 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
CHEMBL4597048 175953 1 None 1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assayAgonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay
ChEMBL 509 12 1 3 7.1 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@H]1C[C@@H]1c1cccc(Cl)c1Cl 10.1021/acs.jmedchem.9b01835
168273640 192203 0 None -4 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5176229 192203 0 None -4 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
CHEMBL5221444 192203 0 None -4 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assayAgonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay
ChEMBL 568 15 8 10 -0.1 N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1 10.1021/acs.jmedchem.1c00692
3038495 700 30 None -5 7 Green monkey 8.5 pEC50 = 8.5 Functional
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm030836n
7625 700 30 None -5 7 Green monkey 8.5 pEC50 = 8.5 Functional
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm030836n
CHEMBL25236 700 30 None -5 7 Green monkey 8.5 pEC50 = 8.5 Functional
Effective concentration for Dopamine receptor D3 was determined in monkeysEffective concentration for Dopamine receptor D3 was determined in monkeys
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm030836n
3038495 700 30 None -8 7 Human 8.5 pEC50 = 8.5 Functional
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
7625 700 30 None -8 7 Human 8.5 pEC50 = 8.5 Functional
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
CHEMBL25236 700 30 None -8 7 Human 8.5 pEC50 = 8.5 Functional
Mitogenic stimulation in NG 108-15 cells expressing human D3 receptorMitogenic stimulation in NG 108-15 cells expressing human D3 receptor
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.1021/jm040190e
25139479 183735 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 183735 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP releaseIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
2 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm025558r
54562 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm025558r
CHEMBL240773 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cellsIntrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm025558r
54580905 61274 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL1771107 61274 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 469 8 0 4 5.0 COc1ccccc1N1CCN(CCCCN2CCc3cc(-c4ccccc4)ccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
25256814 181030 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
CHEMBL477250 181030 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporationAgonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation
ChEMBL 393 7 0 4 3.3 COc1ccccc1N1CCN(CCCCN2CCc3ccccc3C2=O)CC1 10.1016/j.bmcl.2010.12.083
11983282 138414 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
CHEMBL378455 138414 0 None 2 3 Human 8.5 pEC50 = 8.5 Functional
Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assayIntrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay
ChEMBL 315 4 0 3 4.2 C1=C(c2ccccc2)CCN(Cc2cnn(-c3ccccc3)c2)C1 10.1016/j.bmcl.2006.02.075
2 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
2 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
54562 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.1c01327
CHEMBL240773 3210 19 None 2 7 Human 8.5 pEC50 = 8.5 Functional
Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assayPartial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay
ChEMBL 219 2 1