ChEMBL ligand: CHEMBL3092468
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141] There should be some charts here, you may need to enable JavaScript!
serum/glucocorticoid regulated kinase 2/Serine/threonine-protein kinase Sgk2 in Human [ChEMBL: CHEMBL5794] [GtoPdb: 1535] [UniProtKB: Q9HBY8] There should be some charts here, you may need to enable JavaScript!
serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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 recombinant human SGK1 (S61 to L431, S422D) expressed in human U20S cells assessed as inhibition of GSK3beta phosphorylation after 6 hrs by fluorescence assay	B	6.16	pIC50	690	nM	IC50	ACS Med Chem Lett (2013) 4: 1022-1024 [PMID:24900601]
ChEMBL	Inhibition of SGK1 in human U2OS cells assessed as phosphorylation of GSK3beta	B	6.16	pIC50	690	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
ChEMBL	Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 500 uM ATP	B	7.39	pIC50	41	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
GtoPdb	at low (10μM) ATP concentration	-	9	pIC50	1	nM	IC50	ACS Med Chem Lett (2015) 6: 73-8 [PMID:25589934]
ChEMBL	Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP	B	9	pIC50	1	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
ChEMBL	Inhibition of recombinant human SGK-1 expressed in baculovirus expression system using (5(6)-carboxyfluorescein)-RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay	B	9	pIC50	1	nM	IC50	ACS Med Chem Lett (2013) 4: 1022-1024 [PMID:24900601]
ChEMBL	Enzymatic Activity Assay: The compounds were tested for serum and glucocorticoid-regulated kinase 1 (SGK-1) inhibitory activity in a substrate phosphorylation assay designed to measure the ability of the isolated enzyme to catalyze the transfer of phosphate from ATP to serine/threonine residues in a fluorescein-labeled substrate peptide, using recombinant human SGK-1 enzyme produced in a baculovirus system (Biomol, Hamburg, Germany, Cat. No. 4-331). The synthesized fluorescent labeled peptide substrate contained (5(6)-Carboxyfluorescein)-RPRAATF-NH2. The phosphorylated substrate peptide and non-phosphorylated substrate peptide were separated with caliper life science's lab-chip technology based on a micro fluidics method. All fluid flow was established on the chip by applying a vacuum of a few psi to the waste well transporting fluid from various sources through interconnecting channels. Because the phosphoryl group is doubly negatively charged, under the pressure-driven hydrodynamic flow.	B	9	pIC50	1	nM	IC50	US-9174993-B2. N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides and their use as pharmaceuticals (2015)
ChEMBL	Enzymatic Activity Assay: The enzyme reaction was carried out in a buffer containing 25 mM Tris-HCl (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 2 mM DTT, and 0.03% bovine serum albumine. The enzyme was pre-incubated with the test compound for 30 min at 24° C. The kinase reaction was initiated by addition of the substrate mixture containing the peptide substrate (final concentration 1 uM) and ATP (final concentration 10 uM). After 60 min incubation at 37° C., the enzyme reaction was terminated by adding a buffer containing 100 mM Hepes (pH 7.4) and 35 mM EDTA. For the determination of the compound dose response, a 10 mM DMSO stock solution was diluted and tested in a ten-point, three-fold dilution series run in duplicate beginning at 30 uM final concentration.	B	9	pIC50	1	nM	IC50	US-9221828-B2. N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]sulfonamides as pharmaceuticals (2015)
serum/glucocorticoid regulated kinase 2/Serine/threonine-protein kinase Sgk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5794] [GtoPdb: 1535] [UniProtKB: Q9HBY8]
GtoPdb	at high (500μM) ATP concentration	-	6.89	pIC50	128	nM	IC50	ACS Med Chem Lett (2015) 6: 73-8 [PMID:25589934]
ChEMBL	Inhibition of human SGK2 in presence of 500 uM ATP	B	6.89	pIC50	128	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1]
ChEMBL	Inhibition of human SGK3 in presence of 500 uM ATP	B	5.51	pIC50	3100	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
GtoPdb	at high (500μM) ATP concentration	-	5.51	pIC50	3100	nM	IC50	ACS Med Chem Lett (2015) 6: 73-8 [PMID:25589934]

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]