GSK650394 [Ligand Id: 8040] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL558642 (GSK-650394)
  • calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Mouse [ChEMBL: CHEMBL4295888] [GtoPdb: 1957] [UniProtKB: Q8C078]
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  • calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
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  • serum/glucocorticoid regulated kinase 2 in Human [GtoPdb: 1535] [UniProtKB: Q9HBY8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
calcium/calmodulin dependent protein kinase kinase 2/Calcium/calmodulin-dependent protein kinase kinase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295888] [GtoPdb: 1957] [UniProtKB: Q8C078]
ChEMBL Inhibition of CAMKK2 in mouse N39 cells assessed as decrease in AMPKalpha phosphorylation at T172 preincubated for 80 mins followed by inomycin addition by ELISA B 5.9 pIC50 1258.93 nM IC50 Bioorg Med Chem Lett (2018) 28: 1958-1963 [PMID:29653895]
calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
ChEMBL Inhibition of full-length human GST-tagged CAMKK2 using 5FAM-AKPKGNKDYHLQTCCGSLAYRRR-amide as substrate preincubated for 30 mins followed by substrate addition measured after 120 mins by fluorescence polarization assay B 8.1 pIC50 7.94 nM IC50 Bioorg Med Chem Lett (2018) 28: 1958-1963 [PMID:29653895]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Further kinetic evaluation of compounds supplied by Sanofi against AuroraA within a BIAcore3000 instrument B 6.53 pKd 298.01 nM Kd K4DD drug target binding kinetics data
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
ChEMBL Inhibition of SGK1-mediated epithelial sodium channel activity in human M-1 cells assessed as short circuit current by whole cell electrophysiological transepithelial experiment B 6.24 pIC50 580 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4441-4445 [PMID:19497745]
GtoPdb - - 7.21 pIC50 62 nM IC50 Cancer Res (2008) 68: 7475-83 [PMID:18794135]
ChEMBL Inhibition of SGK1 by fluorescence polarization assay B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 4441-4445 [PMID:19497745]
ChEMBL Inhibition of SGK1 expressed in Escherichia coli or baculovirus-infected insect cells by IMAP assay B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2011) 54: 5131-5143 [PMID:21699136]
serum/glucocorticoid regulated kinase 2 in Human [GtoPdb: 1535] [UniProtKB: Q9HBY8]
GtoPdb - - 6.99 pIC50 103 nM IC50 Cancer Res (2008) 68: 7475-83 [PMID:18794135]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]