[3H]apafant [Ligand Id: 1859] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL280164 (Apafant, WEB-2086, WEB 2086 BS, WEB-2086-BS) |
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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 | - | - | 8 | pKd | - | - | - |
J Biol Chem (1991) 266: 20400-5 [PMID:1657923]; J Biol Chem (2001) 276: 43025-30 [PMID:11560941]; J Immunol Methods (1995) 186: 225-31 [PMID:7594622] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
