pizotifen [Ligand Id: 93] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL294951 (BC-105, Pizotifen, Pizotyline, Sandomigran)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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  • 5-HT1A receptor in Human [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 to dopamine D2 receptor (unknown origin) B 8.62 pKi 2.4 nM Ki Bioorg Med Chem (2013) 21: 7841-7852 [PMID:24189186]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity to muscarinic M1 receptor (unknown origin) B 8.7 pKi 2 nM Ki Bioorg Med Chem (2013) 21: 7841-7852 [PMID:24189186]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 5.73 pIC50 1860 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity to 5-HT2A receptor (unknown origin) B 8.12 pKi 7.5 nM Ki Bioorg Med Chem (2013) 21: 7841-7852 [PMID:24189186]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]Mesulergine from human 5-HT2B receptor expressed in HEK293 cells by liquid scintillation counting analysis B 8.7 pKi 2 nM Ki Bioorg Med Chem (2013) 21: 7841-7852 [PMID:24189186]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Binding affinity to 5-HT2C receptor (unknown origin) B 8.85 pKi 1.4 nM Ki Bioorg Med Chem (2013) 21: 7841-7852 [PMID:24189186]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysis B 7.6 pKi 25 nM Ki Bioorg Med Chem (2013) 21: 7841-7852 [PMID:24189186]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1997) 355: 682-8 [PMID:9205951]

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]