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Assay Detail

CHEMBL2155279

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

Binding
Inhibition of mouse 11betaHSD1 by scintillation proximity assay
12
Total Activities
12
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

Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.
Yu J, Liu H, Xia G, Liu L, Xu Z, Chen Q, Ma C, Sun X, Xu J, Li H, Li P, Shi Y, Xiong B, Liu X, Shen J.
ACS Med Chem Lett (2012) 3 : 793 -798
PubMed 24900382 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.28 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152223 1 8.89
CHEMBL2152237 1 7.96
CHEMBL2152227 1 7.20
CHEMBL2152222 1 7.19
CHEMBL2152243 1 7.06
CHEMBL2152236 1 7.01
CHEMBL2152235 1 6.95
CHEMBL2152231 1 6.90
CHEMBL2152230 1 6.84
CHEMBL2152242 1 6.79
CHEMBL2152225 1 -
CHEMBL2152226 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152223 IC50 = 1.3 nM 8.89
CHEMBL2152237 IC50 = 11.0 nM 7.96
CHEMBL2152227 IC50 = 63.0 nM 7.20
CHEMBL2152222 IC50 = 64.0 nM 7.19
CHEMBL2152243 IC50 = 87.0 nM 7.06
CHEMBL2152236 IC50 = 97.0 nM 7.01
CHEMBL2152235 IC50 = 112.0 nM 6.95
CHEMBL2152231 IC50 = 125.0 nM 6.90
CHEMBL2152230 IC50 = 146.0 nM 6.84
CHEMBL2152242 IC50 = 164.0 nM 6.79
CHEMBL2152225 IC50 - -
CHEMBL2152226 IC50 - -