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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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57383420 109204 0 DRD3 D3 receptor Human 5.0 pAC50 = 5.0 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
CHEMBL3234540 109204 0 DRD3 D3 receptor Human 5.0 pAC50 = 5.0 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 424 3 1 3 4.0 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Cl)cc3)cc21 10.1021/jm500126s
57377246 2415 0 DRD3 D3 receptor Human 4.9 pAC50 = 4.9 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
8368 2415 0 DRD3 D3 receptor Human 4.9 pAC50 = 4.9 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
CHEMBL3234544 2415 0 DRD3 D3 receptor Human 4.9 pAC50 = 4.9 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 O=C(c1ccc2c(c1)N(C)C(=O)c1c([S@@]2=O)cccc1)NCCc1cccs1 10.1021/jm500126s
57383436 109206 0 DRD3 D3 receptor Human 4.8 pAC50 = 4.8 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
CHEMBL3234542 109206 0 DRD3 D3 receptor Human 4.8 pAC50 = 4.8 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 391 3 1 4 2.8 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3cccnc3)cc21 10.1021/jm500126s
57383414 109200 0 DRD3 D3 receptor Human 5.8 pAC50 = 5.8 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
CHEMBL3234537 109200 0 DRD3 D3 receptor Human 5.8 pAC50 = 5.8 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 429 4 1 4 3.6 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(C#N)cc3)cc21 10.1021/jm500126s
57383431 109190 0 DRD3 D3 receptor Human 4.7 pAC50 = 4.7 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
CHEMBL3234522 109190 0 DRD3 D3 receptor Human 4.7 pAC50 = 4.7 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 410 4 1 4 3.5 CN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCCc3cccs3)cc21 10.1021/jm500126s
57383403 109195 1 DRD3 D3 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL3234527 109195 1 DRD3 D3 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383430 109199 0 DRD3 D3 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
CHEMBL3234536 109199 0 DRD3 D3 receptor Human 5.5 pAC50 = 5.5 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 422 4 1 3 3.9 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(F)cc3)cc21 10.1021/jm500126s
57383434 109202 0 DRD3 D3 receptor Human 4.5 pAC50 = 4.5 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
CHEMBL3234539 109202 0 DRD3 D3 receptor Human 4.5 pAC50 = 4.5 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 4 1 3 5.5 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc4ccccc4c3)cc21 10.1021/jm500126s
57383405 109205 0 DRD3 D3 receptor Human 5.3 pAC50 = 5.3 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234541 109205 0 DRD3 D3 receptor Human 5.3 pAC50 = 5.3 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 468 3 1 3 4.1 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCc3ccc(Br)cc3)cc21 10.1021/jm500126s
57383401 109207 0 DRD3 D3 receptor Human 5.3 pAC50 = 5.3 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
CHEMBL3234543 109207 0 DRD3 D3 receptor Human 5.3 pAC50 = 5.3 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 397 4 1 4 2.3 CN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)NCCN3CCCC3)cc21 10.1021/jm500126s
16007814 42454 4 DRD3 D3 receptor Human 5.2 pAC50 = 5.2 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
CHEMBL1503220 42454 4 DRD3 D3 receptor Human 5.2 pAC50 = 5.2 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 434 5 1 4 3.8 CCN1C(=O)c2ccccc2[S+]([O-])c2ccc(C(=O)NCc3ccc(OC)cc3)cc21 10.1021/jm500126s
57383397 109201 0 DRD3 D3 receptor Human 5.0 pAC50 = 5.0 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21 10.1021/jm500126s
CHEMBL3234538 109201 0 DRD3 D3 receptor Human 5.0 pAC50 = 5.0 Binding
Antagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assayAntagonist activity at ProLink-tagged D3 receptor (unknown origin) expressed in CHO cells assessed as inhibition of dopamine-stimulated beta-arrestin binding treated for 90 mins prior to dopamine challenge by PathHunter DiscoveRx assay
ChEMBL 496 4 1 3 5.1 CCN1C(=O)c2ccccc2[S@+]([O-])c2ccc(C(=O)N[C@H](C)c3ccc(Br)cc3)cc21 10.1021/jm500126s
10456166 118877 0 DRD3 D3 receptor 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 118877 0 DRD3 D3 receptor 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 118877 0 DRD3 D3 receptor 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 60625 0 DRD3 D3 receptor 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 60625 0 DRD3 D3 receptor 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 177829 0 DRD3 D3 receptor 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 177829 0 DRD3 D3 receptor 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 153795 0 DRD3 D3 receptor 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 153795 0 DRD3 D3 receptor 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 177780 0 DRD3 D3 receptor 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 177780 0 DRD3 D3 receptor 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 186772 0 DRD3 D3 receptor 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 186772 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 104981 0 DRD3 D3 receptor 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 104981 0 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 93638 0 DRD3 D3 receptor 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 93638 0 DRD3 D3 receptor 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
128 144 6 DRD3 D3 receptor 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 144 6 DRD3 D3 receptor 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 144 6 DRD3 D3 receptor 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
27842480 171575 15 DRD3 D3 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4476784 171575 15 DRD3 D3 receptor Human 9.7 pEC50 = 9.7 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
119570 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 138747 8 DRD3 D3 receptor 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 138747 8 DRD3 D3 receptor 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 16732 0 DRD3 D3 receptor 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 16732 0 DRD3 D3 receptor 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 80212 0 DRD3 D3 receptor 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 80212 0 DRD3 D3 receptor 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 80211 0 DRD3 D3 receptor 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 80211 0 DRD3 D3 receptor 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 156009 0 DRD3 D3 receptor 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 156009 0 DRD3 D3 receptor 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 155813 0 DRD3 D3 receptor 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 155813 0 DRD3 D3 receptor 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 155813 0 DRD3 D3 receptor 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 155813 0 DRD3 D3 receptor 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 172961 0 DRD3 D3 receptor 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 172961 0 DRD3 D3 receptor 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 180733 0 DRD3 D3 receptor 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 180733 0 DRD3 D3 receptor 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 197724 18 DRD3 D3 receptor 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 197724 18 DRD3 D3 receptor 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 197724 18 DRD3 D3 receptor 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 164779 7 DRD3 D3 receptor 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 164779 7 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 156575 0 DRD3 D3 receptor 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 156575 0 DRD3 D3 receptor 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 156575 0 DRD3 D3 receptor 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 156575 0 DRD3 D3 receptor 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 158256 0 DRD3 D3 receptor 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 158256 0 DRD3 D3 receptor 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 158256 0 DRD3 D3 receptor 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 158256 0 DRD3 D3 receptor 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 192010 0 DRD3 D3 receptor 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 192010 0 DRD3 D3 receptor 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 191382 0 DRD3 D3 receptor 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 191382 0 DRD3 D3 receptor 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 190953 0 DRD3 D3 receptor 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 190953 0 DRD3 D3 receptor 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 83185 0 DRD3 D3 receptor 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 83185 0 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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
950 178 18 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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 80220 0 DRD3 D3 receptor 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 80220 0 DRD3 D3 receptor 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 96595 2 DRD3 D3 receptor 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 96595 2 DRD3 D3 receptor 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 49187 1 DRD3 D3 receptor 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 49187 1 DRD3 D3 receptor 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 156168 0 DRD3 D3 receptor 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 156168 0 DRD3 D3 receptor 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 194243 0 DRD3 D3 receptor 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 194243 0 DRD3 D3 receptor 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 169876 0 DRD3 D3 receptor 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 169876 0 DRD3 D3 receptor 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
132955 167557 7 DRD3 D3 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 231 3 2 4 1.7 CCCN[C@@H]1Cc2cccc3nc(O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL434665 167557 7 DRD3 D3 receptor Human 9.1 pEC50 = 9.1 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 231 3 2 4 1.7 CCCN[C@@H]1Cc2cccc3nc(O)n(c23)C1 10.1021/acs.jmedchem.5b01612
45486330 191382 0 DRD3 D3 receptor 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 191382 0 DRD3 D3 receptor 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 191382 0 DRD3 D3 receptor 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 191382 0 DRD3 D3 receptor 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 136137 0 DRD3 D3 receptor 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 136137 0 DRD3 D3 receptor 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 136137 0 DRD3 D3 receptor 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
60148496 80217 0 DRD3 D3 receptor 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 80217 0 DRD3 D3 receptor 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
85470564 156009 0 DRD3 D3 receptor 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 156009 0 DRD3 D3 receptor 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 157713 0 DRD3 D3 receptor 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 157713 0 DRD3 D3 receptor 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 160178 0 DRD3 D3 receptor 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 160178 0 DRD3 D3 receptor 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 160178 0 DRD3 D3 receptor 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 155902 0 DRD3 D3 receptor 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 155902 0 DRD3 D3 receptor 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 83186 0 DRD3 D3 receptor 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 83186 0 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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
950 178 18 DRD3 D3 receptor 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 178 18 DRD3 D3 receptor 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
122183778 121473 0 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 434 8 2 6 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
CHEMBL3597649 121473 0 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 434 8 2 6 2.5 COc1ccccc1N1CCN(CC(O)CCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
44427827 92604 0 DRD3 D3 receptor 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 92604 0 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 3061 11 DRD3 D3 receptor 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 3061 11 DRD3 D3 receptor 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 3061 11 DRD3 D3 receptor 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 155902 0 DRD3 D3 receptor 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 155902 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 16602 0 DRD3 D3 receptor 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 16602 0 DRD3 D3 receptor 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
681 1368 56 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
940 1368 56 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
947 1368 56 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
CHEMBL59 1368 56 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
DB00988 1368 56 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
10411237 116734 0 DRD3 D3 receptor 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 116734 0 DRD3 D3 receptor 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 116734 0 DRD3 D3 receptor 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
10014924 106549 0 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
CHEMBL316983 106549 0 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm0503805
10014924 106549 0 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
CHEMBL316983 106549 0 DRD3 D3 receptor Human 9.0 pEC50 = 9.0 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 248 6 0 3 2.7 CCCN(CCC)[C@H]1CCn2c(C=O)ccc2C1 10.1021/jm049269+
27842480 171575 15 DRD3 D3 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4476784 171575 15 DRD3 D3 receptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
137660062 158561 0 DRD3 D3 receptor 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 158561 0 DRD3 D3 receptor 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 97238 0 DRD3 D3 receptor 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 97238 0 DRD3 D3 receptor 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 170830 0 DRD3 D3 receptor 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 170830 0 DRD3 D3 receptor 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 189222 0 DRD3 D3 receptor 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 189222 0 DRD3 D3 receptor 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
128 144 6 DRD3 D3 receptor 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 144 6 DRD3 D3 receptor 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 144 6 DRD3 D3 receptor 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 80204 0 DRD3 D3 receptor 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 80204 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 156871 0 DRD3 D3 receptor 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 156871 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 33075 0 DRD3 D3 receptor 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 33075 0 DRD3 D3 receptor 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 136133 0 DRD3 D3 receptor 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 136133 0 DRD3 D3 receptor 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 136133 0 DRD3 D3 receptor 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 183508 0 DRD3 D3 receptor 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 183508 0 DRD3 D3 receptor 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 156871 0 DRD3 D3 receptor 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 156871 0 DRD3 D3 receptor 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
CHEMBL2146499 79790 0 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
2233 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
953 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
CHEMBL301265 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
DB00413 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm0503805
119570 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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 2967 79 DRD3 D3 receptor 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
119570 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
2233 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
953 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
CHEMBL301265 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
DB00413 2967 79 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1021/jm049269+
10092819 16408 0 DRD3 D3 receptor 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 16408 0 DRD3 D3 receptor 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 186772 0 DRD3 D3 receptor 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 186772 0 DRD3 D3 receptor 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
45140377 194244 0 DRD3 D3 receptor 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 194244 0 DRD3 D3 receptor 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
25139181 183466 0 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
CHEMBL484358 183466 0 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 414 10 1 2 5.7 C#CC1=CCC(N(CCC)CCCCNC(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1021/jm800895v
137660417 158331 0 DRD3 D3 receptor 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 158331 0 DRD3 D3 receptor 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
CHEMBL2203406 82866 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm000087z
54562 3062 14 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm000087z
CHEMBL240773 3062 14 DRD3 D3 receptor Human 8.8 pEC50 = 8.8 Binding
Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity)
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm000087z
681 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm400408r
940 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm400408r
947 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm400408r
CHEMBL59 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm400408r
DB00988 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assayAgonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/jm400408r
681 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
940 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
947 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
CHEMBL59 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
DB00988 1368 56 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
3038495 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 111050 0 DRD3 D3 receptor 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 111050 0 DRD3 D3 receptor 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 111050 0 DRD3 D3 receptor 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 111050 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 1271 16 DRD3 D3 receptor 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 1271 16 DRD3 D3 receptor 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 1271 16 DRD3 D3 receptor 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 1271 16 DRD3 D3 receptor 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 1271 16 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 138941 0 DRD3 D3 receptor 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 138941 0 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 136136 0 DRD3 D3 receptor 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 136136 0 DRD3 D3 receptor 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 136136 0 DRD3 D3 receptor 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
27847327 110314 0 DRD3 D3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 374 6 0 4 3.2 COc1ccc(C(=O)N2CCN(CCOc3ccc(Cl)cc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL3262809 110314 0 DRD3 D3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 374 6 0 4 3.2 COc1ccc(C(=O)N2CCN(CCOc3ccc(Cl)cc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
154703875 175597 1 DRD3 D3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango 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 175597 1 DRD3 D3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango 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 175597 1 DRD3 D3 receptor Human 6.0 pEC50 = 6 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango 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
56360144 174838 1 DRD3 D3 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 427 5 1 3 3.8 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4581907 174838 1 DRD3 D3 receptor Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 427 5 1 3 3.8 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(Br)cc2)CC1 10.1021/acs.jmedchem.0c00424
90467323 158732 0 DRD3 D3 receptor 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 158732 0 DRD3 D3 receptor 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
CHEMBL3590083 121101 0 DRD3 D3 receptor 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 155111 0 DRD3 D3 receptor 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 155111 0 DRD3 D3 receptor 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 139314 0 DRD3 D3 receptor 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 139314 0 DRD3 D3 receptor 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 139314 0 DRD3 D3 receptor 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 139318 0 DRD3 D3 receptor 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 139318 0 DRD3 D3 receptor 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 139318 0 DRD3 D3 receptor 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
127048020 139140 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 466 7 2 4 4.0 CN(CCCCNC(=O)c1ccc2c(c1)Cc1ccccc1-2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3799626 139140 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 466 7 2 4 4.0 CN(CCCCNC(=O)c1ccc2c(c1)Cc1ccccc1-2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
25072635 111052 0 DRD3 D3 receptor 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 111052 0 DRD3 D3 receptor 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 158732 0 DRD3 D3 receptor 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 158732 0 DRD3 D3 receptor 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 77576 0 DRD3 D3 receptor 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 77576 0 DRD3 D3 receptor 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
154726381 175676 1 DRD3 D3 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango 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 175676 1 DRD3 D3 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango 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 175676 1 DRD3 D3 receptor Human 5.0 pEC50 = 5.0 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango 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
25072635 111052 0 DRD3 D3 receptor 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 111052 0 DRD3 D3 receptor 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
CHEMBL3590083 121101 0 DRD3 D3 receptor 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
71725049 170546 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 397 5 1 3 4.0 Cc1cc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)ccc1Cl 10.1021/acs.jmedchem.0c00424
CHEMBL4462053 170546 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 397 5 1 3 4.0 Cc1cc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)ccc1Cl 10.1021/acs.jmedchem.0c00424
9475051 174513 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 383 5 1 3 3.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4574586 174513 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 383 5 1 3 3.7 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.0c00424
127047230 139306 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 418 7 2 5 3.1 CN(CCCCNC(=O)c1cc2ccccc2o1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3800633 139306 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 418 7 2 5 3.1 CN(CCCCNC(=O)c1cc2ccccc2o1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
71604376 110313 3 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 340 6 0 4 2.5 COc1ccc(C(=O)N2CCN(CCOc3ccccc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL3262808 110313 3 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 340 6 0 4 2.5 COc1ccc(C(=O)N2CCN(CCOc3ccccc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
71724960 171994 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 355 6 0 5 2.2 COc1ccc(C(=O)N2CCN(CCOc3cccnc3)CC2)c(C)c1 10.1021/acs.jmedchem.0c00424
CHEMBL4514438 171994 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 355 6 0 5 2.2 COc1ccc(C(=O)N2CCN(CCOc3cccnc3)CC2)c(C)c1 10.1021/acs.jmedchem.0c00424
71724974 172440 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 300 5 1 4 1.2 O=C(c1ccc[nH]1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4525545 172440 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 300 5 1 4 1.2 O=C(c1ccc[nH]1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
25071692 111058 0 DRD3 D3 receptor 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 111058 0 DRD3 D3 receptor 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 155996 0 DRD3 D3 receptor 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 155996 0 DRD3 D3 receptor 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 111058 0 DRD3 D3 receptor 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 111058 0 DRD3 D3 receptor 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 175443 0 DRD3 D3 receptor 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 175443 0 DRD3 D3 receptor 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 175443 0 DRD3 D3 receptor 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
90467172 156081 0 DRD3 D3 receptor 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 156081 0 DRD3 D3 receptor 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 154982 0 DRD3 D3 receptor 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 154982 0 DRD3 D3 receptor 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
127048020 139140 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 466 7 2 4 4.0 CN(CCCCNC(=O)c1ccc2c(c1)Cc1ccccc1-2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3799626 139140 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 466 7 2 4 4.0 CN(CCCCNC(=O)c1ccc2c(c1)Cc1ccccc1-2)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
71725020 170194 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 367 5 1 3 3.1 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4456795 170194 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 367 5 1 3 3.1 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc(F)cc2)CC1 10.1021/acs.jmedchem.0c00424
154726792 175733 1 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4475406 175733 1 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
CHEMBL4597530 175733 1 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assayAgonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay
ChEMBL 489 13 1 4 5.9 CCCN(CCCCNC(=O)c1ccc(-c2ccccn2)cc1)C[C@@H]1C[C@H]1c1cc(F)ccc1OC 10.1021/acs.jmedchem.9b01835
71724985 173516 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 364 5 1 4 2.7 Cc1ccc2[nH]c(C(=O)N3CCN(CCOc4cccnc4)CC3)cc2c1 10.1021/acs.jmedchem.0c00424
CHEMBL4551448 173516 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 364 5 1 4 2.7 Cc1ccc2[nH]c(C(=O)N3CCN(CCOc4cccnc4)CC3)cc2c1 10.1021/acs.jmedchem.0c00424
122183764 121460 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
CHEMBL3597636 121460 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 454 7 2 5 3.7 O=C(NCCC(O)CN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
9828632 99367 0 DRD3 D3 receptor 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 99367 0 DRD3 D3 receptor 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
71724943 171145 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 367 5 0 5 3.1 O=C(c1cc2ccccc2s1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4470996 171145 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 367 5 0 5 3.1 O=C(c1cc2ccccc2s1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
71724971 169494 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 351 5 1 5 1.8 O=C(c1cc2cccnc2[nH]1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4447103 169494 0 DRD3 D3 receptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 351 5 1 5 1.8 O=C(c1cc2cccnc2[nH]1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
71724957 171090 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(C)cc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4470213 171090 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(C)cc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
90467173 157376 0 DRD3 D3 receptor 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 157376 0 DRD3 D3 receptor 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
71725040 172153 0 DRD3 D3 receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 394 6 1 5 2.9 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4518079 172153 0 DRD3 D3 receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 394 6 1 5 2.9 O=C(c1cc2ccccc2[nH]1)N1CCN(CCOc2ccc([N+](=O)[O-])cc2)CC1 10.1021/acs.jmedchem.0c00424
44443903 153276 0 DRD3 D3 receptor 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 153276 0 DRD3 D3 receptor 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
85469680 155902 0 DRD3 D3 receptor 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 155902 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 158489 0 DRD3 D3 receptor 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 158489 0 DRD3 D3 receptor 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 160211 0 DRD3 D3 receptor 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 160211 0 DRD3 D3 receptor 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 160211 0 DRD3 D3 receptor 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 139317 0 DRD3 D3 receptor 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 139317 0 DRD3 D3 receptor 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 139317 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 157771 0 DRD3 D3 receptor 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 139281 0 DRD3 D3 receptor 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 139281 0 DRD3 D3 receptor 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
122183771 121467 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.5b00776
CHEMBL3597643 121467 0 DRD3 D3 receptor Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 426 7 2 3 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cc2ccccc2[nH]1 10.1021/acs.jmedchem.5b00776
145988474 166326 0 DRD3 D3 receptor 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 166326 0 DRD3 D3 receptor 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 175597 1 DRD3 D3 receptor 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 175597 1 DRD3 D3 receptor 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 175597 1 DRD3 D3 receptor 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
127046255 139232 0 DRD3 D3 receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 273 5 1 4 2.1 CCCN[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3800165 139232 0 DRD3 D3 receptor Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 273 5 1 4 2.1 CCCN[C@@H]1Cc2cccc3c2n(c(=O)n3CCC)C1 10.1021/acs.jmedchem.5b01612
127047870 138847 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 245 3 1 3 1.6 CCCN(C)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3797740 138847 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 245 3 1 3 1.6 CCCN(C)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
136056636 111057 0 DRD3 D3 receptor 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 111057 0 DRD3 D3 receptor 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 155858 0 DRD3 D3 receptor 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 155858 0 DRD3 D3 receptor 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 111057 0 DRD3 D3 receptor 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 111057 0 DRD3 D3 receptor 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 155858 0 DRD3 D3 receptor 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 155858 0 DRD3 D3 receptor 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
90466864 157846 0 DRD3 D3 receptor 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 157846 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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
56361674 170491 2 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 363 5 1 3 3.3 Cc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4461237 170491 2 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 363 5 1 3 3.3 Cc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
90467171 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 95714 0 DRD3 D3 receptor 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 95714 0 DRD3 D3 receptor 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
38417721 173076 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(OC)cc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4540693 173076 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 409 7 1 5 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccc(OC)cc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
122183765 121461 0 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 452 8 1 5 4.2 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
CHEMBL3597637 121461 0 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 452 8 1 5 4.2 COc1c(Cl)cccc1N1CCN(CCCCNC(=O)c2cnc3ccccc3c2)CC1 10.1021/acs.jmedchem.5b00776
71724941 171395 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4c(Cl)cccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4474192 171395 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 413 6 1 4 3.7 COc1ccc(OCCN2CCN(C(=O)c3cc4c(Cl)cccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
72187663 174992 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 384 7 0 5 2.9 COc1ccc(OC(C)CN2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4585248 174992 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 384 7 0 5 2.9 COc1ccc(OC(C)CN2CCN(C(=O)c3ccc(OC)cc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
71725026 168689 0 DRD3 D3 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 377 6 1 3 3.6 CCc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4435184 168689 0 DRD3 D3 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 377 6 1 3 3.6 CCc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
109030343 170021 1 DRD3 D3 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
CHEMBL4454068 170021 1 DRD3 D3 receptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assayAgonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
ChEMBL 324 5 1 4 2.5 Cc1cccc(NC(=O)CCN2CCN(c3ccccn3)CC2)c1 10.1021/acs.jmedchem.9b00231
137646281 156988 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 156988 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
71724989 171187 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3cc4cccnc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4471655 171187 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3cc4cccnc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
27842480 171575 15 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4476784 171575 15 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
71604368 174031 0 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 341 6 0 5 1.9 COc1ccc(C(=O)N2CCN(CCOc3cccnc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4563661 174031 0 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 341 6 0 5 1.9 COc1ccc(C(=O)N2CCN(CCOc3cccnc3)CC2)cc1 10.1021/acs.jmedchem.0c00424
137658100 158790 0 DRD3 D3 receptor 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 158790 0 DRD3 D3 receptor 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
130431277 169091 0 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4441358 169091 0 DRD3 D3 receptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
ChEMBL 224 2 1 2 2.3 CCc1cccc(N2CCNCC2)c1Cl 10.1021/acs.jmedchem.6b00860
44309775 101966 0 DRD3 D3 receptor 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 101966 0 DRD3 D3 receptor 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 101966 0 DRD3 D3 receptor 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 101966 0 DRD3 D3 receptor 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 175663 1 DRD3 D3 receptor 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 175663 1 DRD3 D3 receptor 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 175663 1 DRD3 D3 receptor 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
127045814 139057 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 245 3 1 4 1.4 CCCn1c(=O)n2c3c(cccc31)C[C@@H](NC)C2 10.1021/acs.jmedchem.5b01612
CHEMBL3799157 139057 0 DRD3 D3 receptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 245 3 1 4 1.4 CCCn1c(=O)n2c3c(cccc31)C[C@@H](NC)C2 10.1021/acs.jmedchem.5b01612
25093832 155071 0 DRD3 D3 receptor 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 155071 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 77441 0 DRD3 D3 receptor 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 77441 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 160323 0 DRD3 D3 receptor 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 155071 0 DRD3 D3 receptor 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 155071 0 DRD3 D3 receptor 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
132955 167557 7 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 231 3 2 4 1.7 CCCN[C@@H]1Cc2cccc3nc(O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL434665 167557 7 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 231 3 2 4 1.7 CCCN[C@@H]1Cc2cccc3nc(O)n(c23)C1 10.1021/acs.jmedchem.5b01612
90467021 155858 0 DRD3 D3 receptor 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 155858 0 DRD3 D3 receptor 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 155663 0 DRD3 D3 receptor 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 155663 0 DRD3 D3 receptor 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
CHEMBL277301 97959 0 DRD3 D3 receptor 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
3949 3481 24 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.5b01612
9818479 3481 24 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.5b01612
CHEMBL419792 3481 24 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.5b01612
DB06477 3481 24 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 203 1 2 3 0.5 CN[C@@H]1Cc2cccc3c2n(C1)c(=O)[nH]3 10.1021/acs.jmedchem.5b01612
2 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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
15937765 139077 7 DRD3 D3 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 189 0 2 3 0.2 N[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3799271 139077 7 DRD3 D3 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assayAgonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay
ChEMBL 189 0 2 3 0.2 N[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
25072002 155305 0 DRD3 D3 receptor 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 155305 0 DRD3 D3 receptor 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 155663 0 DRD3 D3 receptor 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 155663 0 DRD3 D3 receptor 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 156871 0 DRD3 D3 receptor 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 156871 0 DRD3 D3 receptor 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 155305 0 DRD3 D3 receptor 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 155305 0 DRD3 D3 receptor 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 139311 0 DRD3 D3 receptor 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 139311 0 DRD3 D3 receptor 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 139311 0 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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 3168 48 DRD3 D3 receptor 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
242 451 110 DRD3 D3 receptor 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
34 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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
242 451 110 DRD3 D3 receptor 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
34 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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
127047230 139306 0 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 418 7 2 5 3.1 CN(CCCCNC(=O)c1cc2ccccc2o1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
CHEMBL3800633 139306 0 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 418 7 2 5 3.1 CN(CCCCNC(=O)c1cc2ccccc2o1)[C@@H]1Cc2cccc3[nH]c(=O)n(c23)C1 10.1021/acs.jmedchem.5b01612
90466867 155501 0 DRD3 D3 receptor 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 155501 0 DRD3 D3 receptor 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
71725006 171171 0 DRD3 D3 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 392 6 1 4 3.1 COc1ccc(N(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4471482 171171 0 DRD3 D3 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 392 6 1 4 3.1 COc1ccc(N(C)CCN2CCN(C(=O)c3cc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
71725061 173962 0 DRD3 D3 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3[nH]c4ccccc4c3C)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4562300 173962 0 DRD3 D3 receptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 393 6 1 4 3.3 COc1ccc(OCCN2CCN(C(=O)c3[nH]c4ccccc4c3C)CC2)cc1 10.1021/acs.jmedchem.0c00424
71724954 169265 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4443579 169265 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 380 6 1 5 2.4 COc1ccc(OCCN2CCN(C(=O)c3nc4ccccc4[nH]3)CC2)cc1 10.1021/acs.jmedchem.0c00424
130431317 172106 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4517102 172106 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
ChEMBL 455 8 2 5 4.0 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4o3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
44436605 148262 0 DRD3 D3 receptor 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 148262 0 DRD3 D3 receptor 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
CHEMBL364516 124407 0 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 1368 56 DRD3 D3 receptor 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 91129 0 DRD3 D3 receptor 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 91129 0 DRD3 D3 receptor 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 158572 0 DRD3 D3 receptor 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 158572 0 DRD3 D3 receptor 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 183466 0 DRD3 D3 receptor 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 183466 0 DRD3 D3 receptor 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
2 3062 14 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
54562 3062 14 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
CHEMBL240773 3062 14 DRD3 D3 receptor Human 8.7 pEC50 = 8.7 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm800895v
11316847 69770 0 DRD3 D3 receptor 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 69770 0 DRD3 D3 receptor 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 183509 0 DRD3 D3 receptor 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 183509 0 DRD3 D3 receptor 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 183585 0 DRD3 D3 receptor 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 183585 0 DRD3 D3 receptor 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 158489 0 DRD3 D3 receptor 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 158489 0 DRD3 D3 receptor 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
681 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
940 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
947 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
CHEMBL59 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
DB00988 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assayAgonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
54580906 61054 0 DRD3 D3 receptor 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 61054 0 DRD3 D3 receptor 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 158489 0 DRD3 D3 receptor 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 158489 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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
11230330 134402 0 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
CHEMBL372020 134402 0 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 245 5 0 3 2.8 CCCN(CCC)[C@H]1CCn2c(C#N)ccc2C1 10.1021/jm049269+
130431316 169843 0 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL4451683 169843 0 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of mitogenesis incubated for 16 hrs in presence of [3H]thymidine by scintillation spectrometric analysis
ChEMBL 454 8 3 4 3.7 CCc1cccc(N2CCN(CC(O)CCNC(=O)c3cc4ccccc4[nH]3)CC2)c1Cl 10.1021/acs.jmedchem.6b00860
CHEMBL3590081 121099 0 DRD3 D3 receptor 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 156096 0 DRD3 D3 receptor 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 156096 0 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00412
54562 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00412
CHEMBL240773 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assayAgonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/acs.jmedchem.9b00412
2 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
54562 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
CHEMBL240773 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration against dopamine D3 receptorEffective concentration against dopamine D3 receptor
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm0503805
2 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
54562 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
CHEMBL240773 3062 14 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assayEffective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay
ChEMBL 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 10.1021/jm049269+
2 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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
25139479 183441 0 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
CHEMBL484202 183441 0 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assayIntrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay
ChEMBL 438 10 0 4 6.2 C#CC1=CCC(N(CCC)CCCCn2cc(-c3ccc(-c4ccccc4)cc3)nn2)CC1 10.1021/jm800895v
155525527 170228 0 DRD3 D3 receptor 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 170228 0 DRD3 D3 receptor 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 156096 0 DRD3 D3 receptor 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 156096 0 DRD3 D3 receptor 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
681 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
940 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
947 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
CHEMBL59 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
DB00988 1368 56 DRD3 D3 receptor Human 8.6 pEC50 = 8.6 Binding
Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometryAgonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.5b01612
3038495 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 670 21 DRD3 D3 receptor 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 61056 0 DRD3 D3 receptor 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 61056 0 DRD3 D3 receptor 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 104061 1 DRD3 D3 receptor 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 104061 1 DRD3 D3 receptor 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
681 1368 56 DRD3 D3 receptor Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
940 1368 56 DRD3 D3 receptor Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
947 1368 56 DRD3 D3 receptor Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
CHEMBL59 1368 56 DRD3 D3 receptor Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
DB00988 1368 56 DRD3 D3 receptor Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1021/acs.jmedchem.0c00424
2 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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 3062 14 DRD3 D3 receptor 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
242 451 110 DRD3 D3 receptor 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
34 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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
86280005 121459 0 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 438 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
CHEMBL3597635 121459 0 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesisAgonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of quinpirole-stimulated mitogenesis
ChEMBL 438 7 1 4 4.7 O=C(NCCCCN1CCN(c2cccc3ccccc23)CC1)c1cnc2ccccc2c1 10.1021/acs.jmedchem.5b00776
242 451 110 DRD3 D3 receptor 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
34 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 451 110 DRD3 D3 receptor 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 155501 0 DRD3 D3 receptor 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 155501 0 DRD3 D3 receptor 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 92885 1 DRD3 D3 receptor 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 92885 1 DRD3 D3 receptor 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 174472 0 DRD3 D3 receptor 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 174472 0 DRD3 D3 receptor 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 138892 0 DRD3 D3 receptor 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 138892 0 DRD3 D3 receptor 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
71724968 175098 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 351 5 1 5 1.8 O=C(c1cc2ncccc2[nH]1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
CHEMBL4587874 175098 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 351 5 1 5 1.8 O=C(c1cc2ncccc2[nH]1)N1CCN(CCOc2cccnc2)CC1 10.1021/acs.jmedchem.0c00424
71724965 171280 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)cc1 10.1021/acs.jmedchem.0c00424
CHEMBL4472813 171280 0 DRD3 D3 receptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay
ChEMBL 379 6 1 4 3.0 COc1ccc(OCCN2CCN(C(=O)c3ccc4[nH]ccc4c3)CC2)cc1 10.1021/acs.jmedchem.0c00424
11596603 9661 0 DRD3 D3 receptor 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 9661 0 DRD3 D3 receptor 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
27842480 171575 15 DRD3 D3 receptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assayAgonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay