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Assay Detail

CHEMBL4477397

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

Binding
Inhibition of mouse microsomal 11beta-HSD1 overexpressed in HEK293 cells using [3H]-cortisone as substrate assessed as formation of [3H]-cortisol using [3H]cortisone by scintillation proximity assay in presence of NADPH
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Limonoids and Triterpenoids as 11β-HSD1 Inhibitors from Walsura robusta.
Wang GC, Yu JH, Shen Y, Leng Y, Zhang H, Yue JM.
J Nat Prod (2016) 79 : 899 -906
PubMed 26936592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.32 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230006 ENOXOLONE 2.0 1 8.03
CHEMBL4532570 1 6.16
CHEMBL1508930 1 6.06
CHEMBL4551399 1 5.92
CHEMBL4529492 1 5.42
CHEMBL4575439 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230006 ENOXOLONE IC50 = 9.4 nM 8.03
CHEMBL4532570 IC50 = 690.0 nM 6.16
CHEMBL1508930 IC50 = 880.0 nM 6.06
CHEMBL4551399 IC50 = 1200.0 nM 5.92
CHEMBL4529492 IC50 = 3800.0 nM 5.42
CHEMBL4575439 IC50 - -