compound 10 [PMID: 23147077] [Ligand Id: 8133] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1642655
  • protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit in Human [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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  • mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
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  • MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
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  • erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
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  • IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • mitogen-activated protein kinase kinase kinase 6 in Human [GtoPdb: 2081] [UniProtKB: O95382]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
ChEMBL Inhibition of PRKAA1 (unknown origin) B 4.86 pIC50 13803.84 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 (unknown origin) B 6.81 pIC50 154.88 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
ChEMBL Inhibition of recombinant human His-tagged EPHA3 cytoplasmic domain (569 to 976 residues) expressed in baculovirus expression system B 4.7 pIC50 >19952.62 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system B 4.7 pIC50 >19952.62 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of recombinant full length human His-tagged GSK3B expressed in baculovirus expression system B 6.08 pIC50 831.76 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Inhibition of recombinant human GST-tagged RON cytoplasmic domain expressed in baculovirus expression system B 4.7 pIC50 >19952.62 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
ChEMBL Inhibition of ASK1 assessed as phosphorylated fluorescent peptide by mobility shift assay B 7.85 pIC50 14 nM IC50 Bioorg Med Chem (2011) 19: 486-489 [PMID:21134755]
ChEMBL Competitive inhibition of human recombinant N-terminal FLAG-tagged ASK1 expressed in baculovirus infected Sf2 cells after 60 mins by scintillation counting analysis in presence of [gamma-33P]ATP B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2012) 22: 7326-7329 [PMID:23147077]
GtoPdb - - 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2012) 22: 7326-9 [PMID:23147077]
MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
ChEMBL Inhibition of recombinant human GST-tagged MER cytoplasmic domain expressed in baculovirus expression system B 5.19 pIC50 6456.54 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged ERBB4 cytoplasmic domain (708 to 993 residues) expressed in baculovirus expression system B 4.7 pIC50 >19952.62 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL Inhibition of recombinant human GST-tagged ROCK1 catalytic domain expressed in baculovirus expression system B 5.31 pIC50 4897.79 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL Inhibition of recombinant full length human GST-tagged ITK expressed in baculovirus expression system B 5.26 pIC50 5495.41 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of recombinant human GST-tagged RET cytoplasmic domain expressed in baculovirus expression system B 4.94 pIC50 11481.54 nM IC50 Bioorg Med Chem Lett (2017) 27: 1709-1713 [PMID:28291695]
mitogen-activated protein kinase kinase kinase 6 in Human [GtoPdb: 2081] [UniProtKB: O95382]
GtoPdb - - 6.29 pIC50 510 nM IC50 Bioorg Med Chem Lett (2012) 22: 7326-9 [PMID:23147077]

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]