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Assay Detail

CHEMBL4054226

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

Binding
Inhibition of full-length mouse 11beta-HSD1 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 1 hr by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of selective 11β-HSD1 inhibitors based on dammarane scaffold.
Shao LD, Bao Y, Shen Y, Su J, Leng Y, Zhao QS.
Eur J Med Chem (2017) 135 : 324 -338
PubMed 28458137 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.62 8.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230006 ENOXOLONE 2.0 1 8.13
CHEMBL4102864 1 6.67
CHEMBL4060927 1 6.40
CHEMBL4084451 1 6.34
CHEMBL4065535 1 6.32
CHEMBL4102413 1 6.23
CHEMBL4059599 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230006 ENOXOLONE IC50 = 7.4 nM 8.13
CHEMBL4102864 IC50 = 213.0 nM 6.67
CHEMBL4060927 IC50 = 400.0 nM 6.40
CHEMBL4084451 IC50 = 454.0 nM 6.34
CHEMBL4065535 IC50 = 476.0 nM 6.32
CHEMBL4102413 IC50 = 592.0 nM 6.23
CHEMBL4059599 IC50 = 601.0 nM 6.22