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]
calcium/calmodulin dependent protein kinase kinase 1/CaM-kinase kinase alpha in Human [ChEMBL: CHEMBL5256] [GtoPdb: 1956] [UniProtKB: Q8N5S9]
calcium/calmodulin dependent protein kinase kinase 2/CaM-kinase kinase beta in Human [ChEMBL: CHEMBL5284] [GtoPdb: 1957] [UniProtKB: Q96RR4]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
serum/glucocorticoid regulated kinase 2 in Human [GtoPdb: 1535] [UniProtKB: Q9HBY8]

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 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]
ChEMBL	Inhibition of CaMKK1 (unknown origin) incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	B	8.51	pIC50	3.1	nM	IC50	J Med Chem (2023) 66: 15750-15760 [PMID:38009718]
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]
ChEMBL	Inhibition of CaMKK2 (161 to 449 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) star cells incubated for 20 mins in presence of kinase tracer 236 by TR-FRET	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (2023) 66: 15750-15760 [PMID:38009718]
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 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]