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Assay Detail

CHEMBL3424219

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

Binding
Inhibition of human 11beta-HSD1 overexpressed in microsomal fraction of HEK293 cells assessed as formation of [3H]-cortisol from [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 Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

11-beta-hydroxysteroid dehydrogenase 1 (CHEMBL4235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hupehenols A-E, selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors from Viburnum hupehense.
Chen XQ, Shao LD, Pal M, Shen Y, Cheng X, Xu G, Peng LY, Wang K, Pan ZH, Li MM, Leng Y, He J, Zhao QS.
J Nat Prod (2015) 78 : 330 -334
PubMed 25590374 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.18 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422265 1 7.82
CHEMBL230006 ENOXOLONE 2.0 1 7.54
CHEMBL3422416 1 7.47
CHEMBL3422266 1 7.12
CHEMBL3422264 1 6.71
CHEMBL3422415 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422265 IC50 = 15.3 nM 7.82
CHEMBL230006 ENOXOLONE IC50 = 29.1 nM 7.54
CHEMBL3422416 IC50 = 34.1 nM 7.47
CHEMBL3422266 IC50 = 75.5 nM 7.12
CHEMBL3422264 IC50 = 194.5 nM 6.71
CHEMBL3422415 IC50 = 395.2 nM 6.40