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Assay Detail

CHEMBL2405595

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

Binding
Inhibition of human 11beta-HSD1 transfected in CHOP cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Mono-carbonyl curcumin analogues as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
Lin H, Hu GX, Guo J, Ge Y, Liang G, Lian QQ, Chu Y, Yuan X, Huang P, Ge RS.
Bioorg Med Chem Lett (2013) 23 : 4362 -4366
PubMed 23800686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.49 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093862 1 7.01
CHEMBL504452 1 6.94
CHEMBL476847 1 6.84
CHEMBL482409 1 6.71
CHEMBL128729 1 6.59
CHEMBL477256 1 6.58
CHEMBL476846 1 6.51
CHEMBL478480 1 6.46
CHEMBL476220 1 6.29
CHEMBL129134 1 6.08
CHEMBL140 CURCUMIN 3.0 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093862 IC50 = 97.0 nM 7.01
CHEMBL504452 IC50 = 115.0 nM 6.94
CHEMBL476847 IC50 = 144.0 nM 6.84
CHEMBL482409 IC50 = 195.0 nM 6.71
CHEMBL128729 IC50 = 257.0 nM 6.59
CHEMBL477256 IC50 = 263.0 nM 6.58
CHEMBL476846 IC50 = 310.0 nM 6.51
CHEMBL478480 IC50 = 346.0 nM 6.46
CHEMBL476220 IC50 = 507.0 nM 6.29
CHEMBL129134 IC50 = 832.0 nM 6.08
CHEMBL140 CURCUMIN IC50 = 4501.0 nM 5.35