pimavanserin [Ligand Id: 8423] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2111101 (Pimavanserin)
  • 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
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb Ki determined in membrane radioligand binding assay. - 9.3 pKi - - - J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927];
J Pharmacol Exp Ther (2007) 322: 862-70 [PMID:17519387]
ChEMBL Antagonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 30 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay F 8.05 pIC50 9 nM IC50 Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]