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Assay Detail

CHEMBL1058022

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

Binding
Inhibition of SGK1-mediated epithelial sodium channel activity in human M-1 cells assessed as short circuit current by whole cell electrophysiological transepithelial experiment
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors.
Hammond M, Washburn DG, Hoang HT, Manns S, Frazee JS, Nakamura H, Patterson JR, Trizna W, Wu C, Azzarano LM, Nagilla R, Nord M, Trejo R, Head MS, Zhao B, Smallwood AM, Hightower K, Laping NJ, Schnackenberg CG, Thompson SK.
Bioorg Med Chem Lett (2009) 19 : 4441 -4445
PubMed 19497745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.02 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL564555 1 6.24
CHEMBL558642 GSK-650394 1 6.24
CHEMBL550110 1 6.15
CHEMBL549906 1 6.06
CHEMBL561526 1 6.06
CHEMBL550795 1 5.89
CHEMBL541759 1 5.84
CHEMBL562931 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL564555 IC50 = 580.0 nM 6.24
CHEMBL558642 GSK-650394 IC50 = 580.0 nM 6.24
CHEMBL550110 IC50 = 710.0 nM 6.15
CHEMBL549906 IC50 = 880.0 nM 6.06
CHEMBL561526 IC50 = 870.0 nM 6.06
CHEMBL550795 IC50 = 1300.0 nM 5.89
CHEMBL541759 IC50 = 1460.0 nM 5.84
CHEMBL562931 IC50 = 2000.0 nM 5.70