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Assay Detail

CHEMBL3095701

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

Binding
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
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

N-[4-(1H-Pyrazolo[3,4-B]pyrazin-6yl)-phenyl]-sulonamides and Their Use As Pharmaceuticals.
Blass B.
ACS Med Chem Lett (2013) 4 : 1022 -1024
PubMed 24900601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.81 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092461 1 6.20
CHEMBL3092468 1 6.16
CHEMBL3092460 1 5.85
CHEMBL3092467 1 5.82
CHEMBL3092464 1 5.82
CHEMBL3092462 1 5.68
CHEMBL3092466 1 5.62
CHEMBL3092463 1 5.58
CHEMBL3092465 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092461 IC50 = 630.0 nM 6.20
CHEMBL3092468 IC50 = 690.0 nM 6.16
CHEMBL3092460 IC50 = 1400.0 nM 5.85
CHEMBL3092467 IC50 = 1500.0 nM 5.82
CHEMBL3092464 IC50 = 1500.0 nM 5.82
CHEMBL3092462 IC50 = 2100.0 nM 5.68
CHEMBL3092466 IC50 = 2400.0 nM 5.62
CHEMBL3092463 IC50 = 2600.0 nM 5.58
CHEMBL3092465 IC50 = 2900.0 nM 5.54