ChEMBL ligand: CHEMBL3092461
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!
ribosomal protein S6 kinase B1 in Human [GtoPdb: 1525] [UniProtKB: P23443] There should be some charts here, you may need to enable JavaScript!
serum/glucocorticoid regulated kinase family member 3 in Human [GtoPdb: 1536] [UniProtKB: Q96BR1] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase kinase kinase 11 in Human [GtoPdb: 2071] [UniProtKB: Q16584] 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	6.2	pIC50	630	nM	IC50	ACS Med Chem Lett (2013) 4: 1022-1024 [PMID:24900601]
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	7.6	pIC50	25	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
GtoPdb	-	-	8	pIC50	10	nM	IC50	EMBO J (2016) 35: 1902-22 [PMID:27481935]
GtoPdb	Inhibition of enzyme activity in a biochemical assay.	-	8.3	pIC50	5	nM	IC50	ACS Med Chem Lett (2015) 6: 73-8 [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	8.3	pIC50	5	nM	IC50	ACS Med Chem Lett (2013) 4: 1022-1024 [PMID:24900601]
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	8.3	pIC50	5	nM	IC50	ACS Med Chem Lett (2015) 6: 73-78 [PMID:25589934]
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	8.3	pIC50	5	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	8.3	pIC50	5	nM	IC50	US-9221828-B2. N-[4-(1H-pyrazolo[3,4-b]pyrazin-6-yl)phenyl]sulfonamides as pharmaceuticals (2015)
ribosomal protein S6 kinase B1 in Human [GtoPdb: 1525] [UniProtKB: P23443]
GtoPdb	-	-	7.12	pIC50	76	nM	IC50	EMBO J (2016) 35: 1902-22 [PMID:27481935]
serum/glucocorticoid regulated kinase family member 3 in Human [GtoPdb: 1536] [UniProtKB: Q96BR1]
GtoPdb	-	-	8.4	pIC50	4	nM	IC50
mitogen-activated protein kinase kinase kinase 11 in Human [GtoPdb: 2071] [UniProtKB: Q16584]
GtoPdb	-	-	7.08	pIC50	84	nM	IC50	EMBO J (2016) 35: 1902-22 [PMID:27481935]

ChEMBL data shown on this page come from version 34:

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]