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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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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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 Inverse agonist activity at 5-HT2A receptor (unknown origin) F 9.3 pKi 0.5 nM Ki J Med Chem (2022) 65: 10755-10808 [PMID:35939391]
ChEMBL Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs F 7.3 pIC50 50 nM IC50 Eur J Med Chem (2022) 234: 114246-114246 [PMID:35279606]
ChEMBL Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay F 7.56 pIC50 27.3 nM IC50 Eur J Med Chem (2022) 234: 114246-114246 [PMID:35279606]
ChEMBL Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay F 7.66 pIC50 22 nM IC50 J Med Chem (2020) 63: 4171-4182 [PMID:32285676]
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 Inverse agonist activity at human full-length 5-HT2A B 8.73 pIC50 1.86 nM IC50 RSC Med Chem (2021) 12: 1459-1475 [PMID:34671731]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Inverse agonist activity at 5-HT2C receptor (unknown origin) F 8.82 pKi 1.5 nM Ki J Med Chem (2022) 65: 10755-10808 [PMID:35939391]

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]