flibanserin [Ligand Id: 8182] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL231068 (Addyi, BIMT 17, BIMT-17, BIMT 17 BS, BIMT-17-BS, Ectris, Flibanserin, Flibanserina, Flibanserine)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 1a (5-HT1a) receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
Created with Highcharts 10.3.3ValuesChart context menu5-HT2A receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]-5-OH-DPAT from human 5-HT1AR in human brain tissue by radioligand binding assay B 7.93 pKi 11.8 nM Ki Eur J Med Chem (2022) 235: 114319-114319 [PMID:35367707]
GtoPdb - - 9 pKi 1 nM Ki CNS Drug Rev (2002) 8: 117-42 [PMID:12177684]
ChEMBL Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding F 6.2 pEC50 630.96 nM EC50 J Med Chem (2007) 50: 5024-5033 [PMID:17803293]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity to 5HT1A receptor in rat cortex membrane B 7.93 pKi 11.75 nM Ki J Med Chem (2007) 50: 5024-5033 [PMID:17803293]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 7.31 pKi 49 nM Ki CNS Drug Rev (2002) 8: 117-42 [PMID:12177684]

ChEMBL data shown on this page come from version 35:

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]