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Assay Detail

CHEMBL2378091

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

Binding
Inhibition of 11beta-HSD1 in human HEK293 cells
19
Total Activities
19
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 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.
Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D.
Bioorg Med Chem Lett (2013) 23 : 2344 -2348
PubMed 23489629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.09 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2377209 1 10.52
CHEMBL495841 1 8.30
CHEMBL489857 1 8.00
CHEMBL2377205 1 7.68
CHEMBL2377211 1 7.31
CHEMBL2377216 1 7.29
CHEMBL526098 1 7.28
CHEMBL2377212 1 7.24
CHEMBL2377210 1 7.14
CHEMBL2377214 1 6.74
CHEMBL2377208 1 6.71
CHEMBL2377206 1 6.67
CHEMBL2377213 1 6.49
CHEMBL2377218 1 6.37
CHEMBL2377219 1 6.22
CHEMBL2377217 1 6.03
CHEMBL2377215 1 5.93
CHEMBL2377207 1 5.70
CHEMBL2377204 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2377209 EC50 = 0.03 nM 10.52
CHEMBL495841 EC50 = 5.0 nM 8.30
CHEMBL489857 EC50 = 10.0 nM 8.00
CHEMBL2377205 EC50 = 21.0 nM 7.68
CHEMBL2377211 EC50 = 49.0 nM 7.31
CHEMBL2377216 EC50 = 51.0 nM 7.29
CHEMBL526098 EC50 = 53.0 nM 7.28
CHEMBL2377212 EC50 = 58.0 nM 7.24
CHEMBL2377210 EC50 = 72.0 nM 7.14
CHEMBL2377214 EC50 = 184.0 nM 6.74
CHEMBL2377208 EC50 = 194.0 nM 6.71
CHEMBL2377206 EC50 = 213.0 nM 6.67
CHEMBL2377213 EC50 = 327.0 nM 6.49
CHEMBL2377218 EC50 = 423.0 nM 6.37
CHEMBL2377219 EC50 = 604.0 nM 6.22
CHEMBL2377217 EC50 = 936.0 nM 6.03
CHEMBL2377215 EC50 = 1161.0 nM 5.93
CHEMBL2377207 EC50 = 1980.0 nM 5.70
CHEMBL2377204 EC50 > 10000.0 nM -