A412997 [Ligand Id: 3301] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL375596
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [125I]7-OH-PIPAT from human D2L receptor expressed in HEK293 cell membrane B 5.54 pKi 2900 nM Ki J. Med. Chem. (2006) 49: 7450-7465 [PMID:17149874]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method B 5.77 pKi 1680 nM Ki J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Displacement of [3H](R)-(+)-7-OH-DPAT from human D3 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method B 6.78 pKi 167 nM Ki J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Antagonist activity at human D3 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay B 4 pIC50 >100000 nM IC50 J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Agonist activity at human D3 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay B 4 pEC50 >100000 nM EC50 J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293 cell membranes measured after 60 mins by scintillation counting method B 7.27 pKi 54.2 nM Ki J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Displacement of [3H]A369508 from human D4 receptor expressed in HEK293 cell membrane B 8.1 pKi 8 nM Ki J. Med. Chem. (2006) 49: 7450-7465 [PMID:17149874]
GtoPdb - - 8.1 pKi 7.9 nM Ki Pharmacol Biochem Behav (2005) 82: 140-7 [PMID:16153699]
ChEMBL Displacement of [3H](R)-(+)-7-OH-DPAT from human D4.4 receptor expressed in HEK293 cell membranes measured after 90 mins by scintillation counting method B 8.4 pKi 3.95 nM Ki J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of dopamine-induced beta-arrestin recruitment measured after 90 mins by luminescence assay B 6.72 pIC50 191 nM IC50 J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Antagonist activity at human D4 receptor expressed in CHOK1 cells assessed as suppression of dopamine-induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay F 7.16 pIC50 68.4 nM IC50 J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay B 6.33 pEC50 473 nM EC50 J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
ChEMBL Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR F 7.85 pEC50 14 nM EC50 J. Med. Chem. (2006) 49: 7450-7465 [PMID:17149874]
ChEMBL Agonist activity at human D4 receptor expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay F 8.57 pEC50 2.7 nM EC50 J Med Chem (2019) 62: 3722-3740 [PMID:30883109]
D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729]
GtoPdb - - 8.1 pKi 7.9 nM Ki Pharmacol Biochem Behav (2005) 82: 140-7 [PMID:16153699]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]