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ChEMBL ligand: CHEMBL558642 (GSK-650394) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 1/CaM-kinase kinase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9] | ||||||||
ChEMBL | Inhibition of human CAMKK1 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2021) 64: 10849-10877 [PMID:34264658] |
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] |
ChEMBL | Inhibition of human CAMKK2 using CAMKKtide as substrate assessed as residual activity by [gamma-33P]-ATP assay relative to control | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 10849-10877 [PMID:34264658] |
ChEMBL | Inhibition of NanoLuc-fused CAMKK2 (unknown origin) expressed in HEK293 cells after 24 hrs by NanoBRET assay | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2021) 64: 10849-10877 [PMID:34264658] |
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 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]