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Assay Detail

CHEMBL949067

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Binding
Inhibition of human 11beta-HSD1
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.
Yang H, Dou W, Lou J, Leng Y, Shen J.
Bioorg Med Chem Lett (2008) 18 : 1340 -1345
PubMed 18242087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.81 7.93
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL230006 ENOXOLONE 2.0 1 7.93
CHEMBL403586 1 6.58
CHEMBL401901 1 6.16
CHEMBL255846 1 6.11
CHEMBL255190 1 5.73
CHEMBL269976 1 5.71
CHEMBL271265 1 5.45
CHEMBL271468 1 5.43
CHEMBL404357 1 5.34
CHEMBL258133 1 5.23
CHEMBL256790 1 5.20
CHEMBL269978 1 4.84
CHEMBL255992 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL230006 ENOXOLONE IC50 = 11.78 nM 7.93
CHEMBL403586 IC50 = 260.0 nM 6.58
CHEMBL401901 IC50 = 690.0 nM 6.16
CHEMBL255846 IC50 = 770.0 nM 6.11
CHEMBL255190 IC50 = 1850.0 nM 5.73
CHEMBL269976 IC50 = 1950.0 nM 5.71
CHEMBL271265 IC50 = 3570.0 nM 5.45
CHEMBL271468 IC50 = 3740.0 nM 5.43
CHEMBL404357 IC50 = 4580.0 nM 5.34
CHEMBL258133 IC50 = 5870.0 nM 5.23
CHEMBL256790 IC50 = 6280.0 nM 5.20
CHEMBL269978 IC50 = 14600.0 nM 4.84
CHEMBL255992 Activity - -