bepafant [Ligand Id: 6078] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL325439 (Bepafant, WEB-2170)
  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
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  • PAF receptor in Human [GtoPdb: 334] [UniProtKB: P25105]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Platelet activating factor receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
ChEMBL Antagonist activity against platelet activating factor (PAF) receptor in rabbit platelet membranes using [3H]C18-PAF as radioligand F 7.53 pKi 29.2 nM Ki J Med Chem (1994) 37: 2011-2032 [PMID:8027984]
ChEMBL In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets F 7.14 pIC50 73 nM IC50 J Med Chem (1995) 38: 3524-3535 [PMID:7658439]
ChEMBL Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. F 7.14 pIC50 73 nM IC50 J Med Chem (1995) 38: 3514-3523 [PMID:7658438]
PAF receptor in Human [GtoPdb: 334] [UniProtKB: P25105]
GtoPdb - - 6.49 pIC50 320 nM IC50 J Pharmacol Exp Ther (1990) 255: 962-8 [PMID:2262914]
GtoPdb - - 6.52 pIC50 300 nM IC50 J Pharmacol Exp Ther (1990) 255: 34-9 [PMID:2170626]

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]