benperidol [Ligand Id: 9215] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL297302 (Anquil, Benperidol, Benquil, MCN-JR-4584, NSC-170982, R-4584)
  • 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]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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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 to human dopamine D2 receptor by radioligand displacement assay B 10.57 pKi 0.03 nM Ki Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
GtoPdb - - 10.57 pKi 0.03 nM Ki Mol Psychiatry (1998) 3: 123-34 [PMID:9577836]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [125I]-IABN from human recombinant dopamine D3 receptor expressed in HEK293 cell membrane incubated for 60 mins filtration binding assay B 9.54 pKi 0.29 nM Ki Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 10.18 pKi 0.07 nM Ki Mol Psychiatry (1998) 3: 123-34 [PMID:9577836]
ChEMBL Binding affinity to human dopamine D4 receptor by radioligand displacement assay B 10.18 pKi 0.07 nM Ki Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity to 5HT2A receptor (unknown origin) B 8.92 pKi 1.2 nM Ki Bioorg Med Chem (2016) 24: 3671-3679 [PMID:27364609]

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]