Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4603663

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

Binding
Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL3910)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Optimization of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.
Lee JH, Bok JH, Park SB, Pagire HS, Na YJ, Rim E, Jung WH, Song JS, Kang NS, Seo HW, Jung KY, Lee BH, Kim KY, Ahn JH.
Bioorg Med Chem Lett (2020) 30 : 126787 -126787
PubMed 31759849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.36 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3951168 1 9.00
CHEMBL4633146 1 9.00
CHEMBL4645319 1 9.00
CHEMBL3663671 1 8.70
CHEMBL4648389 1 8.43
CHEMBL4646414 1 7.17
CHEMBL4638272 1 6.76
CHEMBL499915 CARBENOXOLONE 2.0 1 6.61
CHEMBL4638268 1 6.16
CHEMBL4649416 1 6.03
CHEMBL4632806 1 5.92
CHEMBL4647977 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3951168 IC50 = 1.0 nM 9.00
CHEMBL4633146 IC50 = 1.0 nM 9.00
CHEMBL4645319 IC50 = 1.0 nM 9.00
CHEMBL3663671 IC50 = 2.0 nM 8.70
CHEMBL4648389 IC50 = 3.7 nM 8.43
CHEMBL4646414 IC50 = 68.0 nM 7.17
CHEMBL4638272 IC50 = 174.0 nM 6.76
CHEMBL499915 CARBENOXOLONE IC50 = 243.0 nM 6.61
CHEMBL4638268 IC50 = 695.0 nM 6.16
CHEMBL4649416 IC50 = 940.0 nM 6.03
CHEMBL4632806 IC50 = 1207.0 nM 5.92
CHEMBL4647977 IC50 = 2803.0 nM 5.55