compound 14n [PMID: 25589934] [Ligand Id: 9423] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3092468
  • 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/Serine/threonine-protein kinase Sgk2 in Human [ChEMBL: CHEMBL5794] [GtoPdb: 1535] [UniProtKB: Q9HBY8]
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  • serum/glucocorticoid regulated kinase family member 3/Serine/threonine-protein kinase Sgk3 in Human [ChEMBL: CHEMBL6186] [GtoPdb: 1536] [UniProtKB: Q96BR1]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]