[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 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]
