CP-226269 [Ligand Id: 973] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL77395 (CP-226269)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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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/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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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 Binding affinity towards human Dopamine receptor D2 B 6.92 pKi 120 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay B 6.28 pEC50 527 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay B 7.26 pEC50 55 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards human Dopamine receptor D3 B 6.25 pKi 560 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity towards human D4.4 receptor B 8.44 pKi 3.6 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL Effective concentration against human Dopamine receptor D4 B 7.49 pEC50 32 nM EC50 J Med Chem (2004) 47: 2348-2355 [PMID:15084133]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay B 7.49 pEC50 32 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
GtoPdb - - 9.4 pKi - - - Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay B 7.44 pEC50 36 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay B 7.66 pEC50 22 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity towards human Opioid receptor kappa 1 B 6.52 pKi 300 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1A receptor B 6.7 pKi 200 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]