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Assay Detail

CHEMBL997251

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

Binding
Inhibition of human 11beta-HSD1 in HEK293 cells
8
Total Activities
8
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

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.
Siu M, Johnson TO, Wang Y, Nair SK, Taylor WD, Cripps SJ, Matthews JJ, Edwards MP, Pauly TA, Ermolieff J, Castro A, Hosea NA, LaPaglia A, Fanjul AN, Vogel JE.
Bioorg Med Chem Lett (2009) 19 : 3493 -3497
PubMed 19473839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.44 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495841 1 8.30
CHEMBL495840 1 8.30
CHEMBL489857 1 8.00
CHEMBL496082 1 7.40
CHEMBL526098 1 7.40
CHEMBL497105 1 7.30
CHEMBL495842 1 6.74
CHEMBL523284 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495841 EC50 = 5.0 nM 8.30
CHEMBL495840 EC50 = 5.0 nM 8.30
CHEMBL489857 EC50 = 10.0 nM 8.00
CHEMBL496082 EC50 = 40.0 nM 7.40
CHEMBL526098 EC50 = 40.0 nM 7.40
CHEMBL497105 EC50 = 50.0 nM 7.30
CHEMBL495842 EC50 = 184.0 nM 6.74
CHEMBL523284 EC50 = 846.0 nM 6.07