apafant [Ligand Id: 1860] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL280164 (Apafant, WEB-2086, WEB 2086 BS, WEB-2086-BS)
  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
  • Platelet activating factor receptor in Guinea pig [ChEMBL: CHEMBL5136] [UniProtKB: P21556]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
GtoPdb - - 7.5 pKi - - - J Biol Chem (1996) 271: 23298-303 [PMID:8798529];
Biochem Biophys Res Commun (1993) 190: 162-6 [PMID:8380690]
ChEMBL Inhibition of [3H]PAF binding to dog platelets. B 6.7 pIC50 200 nM IC50 J. Med. Chem. (1989) 32: 1820-1835 [PMID:2754709]
ChEMBL In vitro for platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets. B 6.7 pIC50 200 nM IC50 J. Med. Chem. (1991) 34: 1440-1446 [PMID:2016721]
ChEMBL PAF-antagonist activity determined in dog platelets by PAF-binding assay B 6.7 pIC50 200 nM IC50 J. Med. Chem. (1991) 34: 1209-1221 [PMID:2002463]
ChEMBL Displacement of [3H]PAF from PAF receptor of human platelet membranes B 7.03 pIC50 94 nM IC50 J. Med. Chem. (1998) 41: 1970-1979 [PMID:9599246]
ChEMBL Antagonistic activity for inhibition of [3H]PAF receptor binding to washed human platelet membranes. B 7.3 pIC50 50 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 597-602
ChEMBL Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF. F 7.4 pIC50 40 nM IC50 J. Med. Chem. (1991) 34: 457-461 [PMID:1671420]
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 7.01 pKi 98.3 nM Ki J. Med. Chem. (1994) 37: 2011-2032 [PMID:8027984]
ChEMBL In vitro intrinsic binding affinity at platelet activating factor receptor using rabbit platelet membranes B 7.01 pKi 98 nM Ki J. Med. Chem. (1992) 35: 2055-2061 [PMID:1317924]
ChEMBL Competitive inhibition of Platelet activating factor receptor in rabbit-washed platelets B 8.15 pKi 7.08 nM Ki J. Med. Chem. (1995) 38: 2130-2137 [PMID:7783144]
ChEMBL In vitro inhibition of PAF-induced aggregation of rabbit washed platelets. F 6.84 pIC50 146 nM IC50 J. Med. Chem. (1992) 35: 3115-3129 [PMID:1507200]
ChEMBL Inhibition of PAF-induced platelet aggregation F 7.04 pIC50 91 nM IC50 J. Med. Chem. (1993) 36: 2984-2997 [PMID:8411016]
ChEMBL Concentration tested in vitro to inhibit PAF-induced maximum aggregation (PAF-Antagonistic activity) by 50%. F 7.04 pIC50 91 nM IC50 J. Med. Chem. (1992) 35: 4118-4134 [PMID:1433215]

ChEMBL data shown on this page come from version 31:

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