compound 20 [PMID: 23489211] [Ligand Id: 8124] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2322989
  • EPH receptor A1/Ephrin type-A receptor 1 in Human [ChEMBL: CHEMBL5810] [GtoPdb: 1821] [UniProtKB: P21709]
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  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
  • EPH receptor A2 in Mouse [GtoPdb: 1822] [UniProtKB: Q03145]
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  • EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
  • EPH receptor A3 in Mouse [GtoPdb: 1823] [UniProtKB: P29319]
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  • EPH receptor A4/Ephrin type-A receptor 4 in Human [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
  • EPH receptor A4 in Mouse [GtoPdb: 1824] [UniProtKB: Q03137]
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  • EPH receptor A5/Ephrin type-A receptor 5 in Human [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
  • EPH receptor A5 in Rat [GtoPdb: 1825] [UniProtKB: P54757]
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  • EPH receptor A6/Ephrin type-A receptor 6 in Human [ChEMBL: CHEMBL4526] [GtoPdb: 1826] [UniProtKB: Q9UF33]
  • EPH receptor A6 in Mouse [GtoPdb: 1826] [UniProtKB: Q62413]
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  • EPH receptor A7/Ephrin type-A receptor 7 in Human [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
  • EPH receptor A7 in Mouse [GtoPdb: 1827] [UniProtKB: Q61772]
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  • EPH receptor A8/Ephrin type-A receptor 8 in Human [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
  • EPH receptor A8 in Mouse [GtoPdb: 1828] [UniProtKB: O09127]
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  • EPH receptor B1/Ephrin type-B receptor 1 in Human [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762]
  • EPH receptor B1 in Rat [GtoPdb: 1830] [UniProtKB: P09759]
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  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
  • EPH receptor B2 in Mouse [GtoPdb: 1831] [UniProtKB: P54763]
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  • EPH receptor B3/Ephrin type-B receptor 3 in Human [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
  • EPH receptor B3 in Mouse [GtoPdb: 1832] [UniProtKB: P54754]
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  • EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
  • EPH receptor B4 in Mouse [GtoPdb: 1833] [UniProtKB: P54761]
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  • EPH receptor B6/Ephrin type-B receptor 6 in Human [ChEMBL: CHEMBL5836] [GtoPdb: 1834] [UniProtKB: O15197]
  • EPH receptor B6 in Mouse [GtoPdb: 1834] [UniProtKB: O08644]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]