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 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]
