compound 66 [PMID: 19788238] [Ligand Id: 8141] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL566515
  • 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]
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  • EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
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  • EPH receptor A4/Ephrin type-A receptor 4 in Human [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
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  • EPH receptor A5/Ephrin type-A receptor 5 in Human [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
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  • EPH receptor A7/Ephrin type-A receptor 7 in Human [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
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  • EPH receptor A8/Ephrin type-A receptor 8 in Human [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
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  • EPH receptor B1/Ephrin type-B receptor 1 in Human [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762]
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  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
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  • EPH receptor B3/Ephrin type-B receptor 3 in Human [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
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  • EPH receptor B4/Ephrin type-B receptor 4 in Human [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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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 Inhibition of EphA1 by [gamma33-P]ATP based assay B 8.54 pIC50 2.9 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
GtoPdb - - 8.54 pIC50 2.9 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Inhibition of EphA2 by [gamma33-P]ATP based assay B 8.64 pIC50 2.3 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
GtoPdb - - 8.64 pIC50 2.3 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
ChEMBL Inhibition of EphA3 by [gamma33-P]ATP based assay B 7.4 pIC50 40 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
GtoPdb - - 7.4 pIC50 40 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
EPH receptor A4/Ephrin type-A receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988] [GtoPdb: 1824] [UniProtKB: P54764]
GtoPdb - - 8.48 pIC50 3.3 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
ChEMBL Inhibition of EphA4 by [gamma33-P]ATP based assay B 8.48 pIC50 3.3 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
EPH receptor A5/Ephrin type-A receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3987] [GtoPdb: 1825] [UniProtKB: P54756]
GtoPdb - - 8.52 pIC50 3 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
ChEMBL Inhibition of EphA5 by [gamma33-P]ATP based assay B 8.52 pIC50 3 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
EPH receptor A7/Ephrin type-A receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4602] [GtoPdb: 1827] [UniProtKB: Q15375]
GtoPdb - - 5.95 pIC50 1118 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
ChEMBL Inhibition of EphA7 by [gamma33-P]ATP based assay B 5.95 pIC50 1118 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
EPH receptor A8/Ephrin type-A receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4134] [GtoPdb: 1828] [UniProtKB: P29322]
ChEMBL Inhibition of EphA8 by [gamma33-P]ATP based assay B 8.35 pIC50 4.5 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
GtoPdb - - 8.35 pIC50 4.5 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
EPH receptor B1/Ephrin type-B receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5072] [GtoPdb: 1830] [UniProtKB: P54762]
ChEMBL Inhibition of EphB1 by [gamma33-P]ATP based assay B 8.96 pIC50 1.1 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
GtoPdb - - 8.96 pIC50 1.1 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
GtoPdb - - 8.92 pIC50 1.2 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
ChEMBL Inhibition of EphB2 by [gamma33-P]ATP based assay B 8.92 pIC50 1.2 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
EPH receptor B3/Ephrin type-B receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4901] [GtoPdb: 1832] [UniProtKB: P54753]
GtoPdb - - 7.82 pIC50 15 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
ChEMBL Inhibition of EphB3 by [gamma33-P]ATP based assay B 7.82 pIC50 15 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
EPH receptor B4/Ephrin type-B receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5147] [GtoPdb: 1833] [UniProtKB: P54760]
ChEMBL Inhibition of human myc-tagged full length EphB4 expressed in MEF cells assessed as inhibition of ephrinB2-Fc-induced autophosphorylation incubated for 90 mins prior to ephrinB2-Fc-induction measured after 2 hrs by sandwich ELISA B 6.89 pIC50 130 nM IC50 J Med Chem (2013) 56: 84-96 [PMID:23253074]
ChEMBL Inhibition of EphB4 assessed as blockade of synthetic substrate phosphorylation by FRET assay B 8.3 pIC50 5 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
ChEMBL Inhibition of EphB4 (unknown origin) using Z'-LYTE TYR-1 peptide as substrate after 2 hrs by FRET assay B 8.3 pIC50 5 nM IC50 J Med Chem (2013) 56: 84-96 [PMID:23253074]
ChEMBL Inhibition of EphB4 by [gamma33-P]ATP based assay B 8.8 pIC50 1.6 nM IC50 J Med Chem (2009) 52: 6433-6446 [PMID:19788238]
ChEMBL Inhibition of EphB4 (unknown origin) using [gamma-33P]ATP by radiometric assay B 8.8 pIC50 1.6 nM IC50 J Med Chem (2013) 56: 84-96 [PMID:23253074]
GtoPdb - - 8.8 pIC50 1.6 nM IC50 J Med Chem (2009) 52: 6433-46 [PMID:19788238]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of Abl (unknown origin) using [gamma-33P]ATP after 30 mins by radiometric assay B 9.04 pIC50 0.92 nM IC50 J Med Chem (2013) 56: 84-96 [PMID:23253074]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239]
ChEMBL Inhibition of Lck (unknown origin) using [gamma-33P]ATP after 30 mins by radiometric assay B 8.89 pIC50 1.3 nM IC50 J Med Chem (2013) 56: 84-96 [PMID:23253074]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of Src (unknown origin) using [gamma-33P]ATP after 30 mins by radiometric assay B 8.94 pIC50 1.14 nM IC50 J Med Chem (2013) 56: 84-96 [PMID:23253074]

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]