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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]