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Assay Detail

CHEMBL4054231

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

Binding
Inhibition of full-length human 11beta-HSD2 expressed in HEK293 microsomal fraction using [3H]cortisone as substrate after 2 hr by scintillation proximity assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

11-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL3746)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.37 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230006 ENOXOLONE 2.0 1 8.89
CHEMBL4064979 1 5.20
CHEMBL4103361 1 5.02
CHEMBL4071679 1 -
CHEMBL4088895 1 -
CHEMBL4087459 1 -
CHEMBL4102864 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230006 ENOXOLONE IC50 = 1.3 nM 8.89
CHEMBL4064979 IC50 = 6261.0 nM 5.20
CHEMBL4103361 IC50 = 9582.0 nM 5.02
CHEMBL4071679 IC50 - -
CHEMBL4088895 IC50 - -
CHEMBL4087459 IC50 - -
CHEMBL4102864 IC50 > 10000.0 nM -