compound 20 [PMID: 23489211] [Ligand Id: 8124] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2322989 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| EPH receptor A1/Ephrin type-A receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA1 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| GtoPdb | - | - | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317] | ||||||||
| ChEMBL | Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| ChEMBL | Antagonist activity at EphA2 receptor in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated cell retraction pretreated for 15 mins by fluorescence microscopy | B | 5.29 | pIC50 | 5100 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| ChEMBL | Displacement of ephrin-A1-Fc from EphA2 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.66 | pIC50 | 2200 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| ChEMBL | Inhibition of ephrin-A1-Fc binding to EphA2-Fc receptor (unknown origin) after 1 hr by ELISA | B | 5.69 | pIC50 | 2041.74 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A2 in Mouse [GtoPdb: 1822] [UniProtKB: Q03145] | ||||||||
| GtoPdb | - | - | 5.66 | pIC50 | 2200 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA3 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A3 in Mouse [GtoPdb: 1823] [UniProtKB: P29319] | ||||||||
| GtoPdb | - | - | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA4 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A4 in Mouse [GtoPdb: 1824] [UniProtKB: Q03137] | ||||||||
| GtoPdb | - | - | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA5 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A5 in Rat [GtoPdb: 1825] [UniProtKB: P54757] | ||||||||
| GtoPdb | - | - | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A6/Ephrin type-A receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA6 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A6 in Mouse [GtoPdb: 1826] [UniProtKB: Q62413] | ||||||||
| GtoPdb | - | - | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA7 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A7 in Mouse [GtoPdb: 1827] [UniProtKB: Q61772] | ||||||||
| GtoPdb | - | - | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322] | ||||||||
| ChEMBL | Displacement of ephrin-A1-Fc from EphA8 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor A8 in Mouse [GtoPdb: 1828] [UniProtKB: O09127] | ||||||||
| GtoPdb | - | - | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762] | ||||||||
| ChEMBL | Displacement of ephrin-B1-Fc from EphB1 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor B1 in Rat [GtoPdb: 1830] [UniProtKB: P09759] | ||||||||
| GtoPdb | - | - | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323] | ||||||||
| ChEMBL | Displacement of ephrin-B1-Fc from EphB2 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor B2 in Mouse [GtoPdb: 1831] [UniProtKB: P54763] | ||||||||
| GtoPdb | - | - | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753] | ||||||||
| ChEMBL | Displacement of ephrin-B1-Fc from EphB3 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.36 | pIC50 | 4400 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor B3 in Mouse [GtoPdb: 1832] [UniProtKB: P54754] | ||||||||
| GtoPdb | - | - | 5.36 | pIC50 | 4400 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760] | ||||||||
| ChEMBL | Displacement of ephrin-B1-Fc from EphB4 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.36 | pIC50 | 4400 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor B4 in Mouse [GtoPdb: 1833] [UniProtKB: P54761] | ||||||||
| GtoPdb | - | - | 5.36 | pIC50 | 4400 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
| EPH receptor B6/Ephrin type-B receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197] | ||||||||
| ChEMBL | Displacement of ephrin-B1-Fc from EphB6 receptor Fc ectodomain (unknown origin) after 1 hr by ELISA | B | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (2013) 56: 2936-2947 [PMID:23489211] |
| EPH receptor B6 in Mouse [GtoPdb: 1834] [UniProtKB: O08644] | ||||||||
| GtoPdb | - | - | 5.24 | pIC50 | 5800 | nM | IC50 | J Med Chem (2013) 56: 2936-47 [PMID:23489211] |
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]
