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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL280164 (Apafant, WEB-2086, 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]
1 CHEMBL280164_lig_chart_1 Platelet activating factor receptor HumanGuinea pig
There should be some charts here, you may need to enable JavaScript!
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 27:

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]