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Assay Detail

CHEMBL3375440

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 10 uM ATP
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase Sgk1 (CHEMBL2343)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Halland N, Schmidt F, Weiss T, Saas J, Li Z, Czech J, Dreyer M, Hofmeister A, Mertsch K, Dietz U, Strübing C, Nazare M.
ACS Med Chem Lett (2015) 6 : 73 -78
PubMed 25589934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 7.78 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356029 1 9.00
CHEMBL3092468 1 9.00
CHEMBL3092467 1 8.70
CHEMBL3356044 1 8.70
CHEMBL3356048 1 8.70
CHEMBL3356049 1 8.70
CHEMBL3356050 1 8.70
CHEMBL3356053 1 8.70
CHEMBL3092463 1 8.70
CHEMBL3092462 1 8.70
CHEMBL3356024 1 8.70
CHEMBL3356059 1 8.70
CHEMBL3092466 1 8.70
CHEMBL3092465 1 8.52
CHEMBL3356054 1 8.52
CHEMBL3356018 1 8.52
CHEMBL3356052 1 8.52
CHEMBL3092460 1 8.52
CHEMBL3356060 1 8.52
CHEMBL3356039 1 8.40
CHEMBL3092464 1 8.40
CHEMBL3092461 1 8.30
CHEMBL3356026 1 8.22
CHEMBL3356031 1 8.05
CHEMBL3356051 1 8.00
CHEMBL3356058 1 7.89
CHEMBL3356019 1 7.85
CHEMBL3356041 1 7.85
CHEMBL3356047 1 7.82
CHEMBL3356038 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356029 IC50 = 1.0 nM 9.00
CHEMBL3092468 IC50 = 1.0 nM 9.00
CHEMBL3356044 IC50 = 2.0 nM 8.70
CHEMBL3356048 IC50 = 2.0 nM 8.70
CHEMBL3356049 IC50 = 2.0 nM 8.70
CHEMBL3356050 IC50 = 2.0 nM 8.70
CHEMBL3356053 IC50 = 2.0 nM 8.70
CHEMBL3092463 IC50 = 2.0 nM 8.70
CHEMBL3092462 IC50 = 2.0 nM 8.70
CHEMBL3356024 IC50 = 2.0 nM 8.70
CHEMBL3356059 IC50 = 2.0 nM 8.70
CHEMBL3092466 IC50 = 2.0 nM 8.70
CHEMBL3092467 IC50 = 2.0 nM 8.70
CHEMBL3092460 IC50 = 3.0 nM 8.52
CHEMBL3356054 IC50 = 3.0 nM 8.52
CHEMBL3356018 IC50 = 3.0 nM 8.52
CHEMBL3356052 IC50 = 3.0 nM 8.52
CHEMBL3092465 IC50 = 3.0 nM 8.52
CHEMBL3356060 IC50 = 3.0 nM 8.52
CHEMBL3356039 IC50 = 4.0 nM 8.40
CHEMBL3092464 IC50 = 4.0 nM 8.40
CHEMBL3092461 IC50 = 5.0 nM 8.30
CHEMBL3356026 IC50 = 6.0 nM 8.22
CHEMBL3356031 IC50 = 9.0 nM 8.05
CHEMBL3356051 IC50 = 10.0 nM 8.00
CHEMBL3356058 IC50 = 13.0 nM 7.89
CHEMBL3356041 IC50 = 14.0 nM 7.85
CHEMBL3356019 IC50 = 14.0 nM 7.85
CHEMBL3356047 IC50 = 15.0 nM 7.82
CHEMBL3356038 IC50 = 16.0 nM 7.80
CHEMBL3356020 IC50 = 19.0 nM 7.72
CHEMBL3356042 IC50 = 21.0 nM 7.68
CHEMBL3356046 IC50 = 22.0 nM 7.66
CHEMBL3356016 IC50 = 28.0 nM 7.55
CHEMBL3356061 IC50 = 29.0 nM 7.54
CHEMBL3356027 IC50 = 46.0 nM 7.34
CHEMBL3356022 IC50 = 124.0 nM 6.91
CHEMBL3356040 IC50 = 196.0 nM 6.71
CHEMBL3356015 IC50 = 315.0 nM 6.50
CHEMBL3356045 IC50 = 407.0 nM 6.39
CHEMBL3356057 IC50 = 419.0 nM 6.38
CHEMBL3356055 IC50 = 439.0 nM 6.36
CHEMBL3356056 IC50 = 496.0 nM 6.30
CHEMBL3356014 IC50 = 1800.0 nM 5.75
CHEMBL3356013 IC50 = 2260.0 nM 5.65
CHEMBL3356012 IC50 = 7140.0 nM 5.15
CHEMBL3356017 IC50 = 13200.0 nM 4.88
CHEMBL3356025 IC50 < 1.0 nM -
CHEMBL3356028 IC50 < 2.0 nM -
CHEMBL3356030 IC50 < 1.0 nM -