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Assay Detail

CHEMBL3095702

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

Binding
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
9
Total Activities
9
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

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 8.62 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092468 1 9.00
CHEMBL3092467 1 8.70
CHEMBL3092466 1 8.70
CHEMBL3092463 1 8.70
CHEMBL3092462 1 8.70
CHEMBL3092465 1 8.52
CHEMBL3092460 1 8.52
CHEMBL3092464 1 8.40
CHEMBL3092461 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092468 IC50 = 1.0 nM 9.00
CHEMBL3092467 IC50 = 2.0 nM 8.70
CHEMBL3092466 IC50 = 2.0 nM 8.70
CHEMBL3092463 IC50 = 2.0 nM 8.70
CHEMBL3092462 IC50 = 2.0 nM 8.70
CHEMBL3092465 IC50 = 3.0 nM 8.52
CHEMBL3092460 IC50 = 3.0 nM 8.52
CHEMBL3092464 IC50 = 4.0 nM 8.40
CHEMBL3092461 IC50 = 5.0 nM 8.30