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Assay Detail

CHEMBL954745

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

Binding
Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cell lysate assessed as conversion of radiolabeled estrone to estradiol
14
Total Activities
14
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

Discovery of nonsteroidal 17beta-hydroxysteroid dehydrogenase 1 inhibitors by pharmacophore-based screening of virtual compound libraries.
Schuster D, Nashev LG, Kirchmair J, Laggner C, Wolber G, Langer T, Odermatt A.
J Med Chem (2008) 51 : 4188 -4199
PubMed 18533708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.11 5.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469909 1 5.42
CHEMBL469911 1 5.21
CHEMBL472508 1 4.70
CHEMBL530555 1 -
CHEMBL488681 1 -
CHEMBL511844 1 -
CHEMBL512532 1 -
CHEMBL513427 1 -
CHEMBL1628094 1 -
CHEMBL472167 1 -
CHEMBL470948 1 -
CHEMBL446912 1 -
CHEMBL512535 1 -
CHEMBL471998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469909 IC50 = 3800.0 nM 5.42
CHEMBL469911 IC50 = 6200.0 nM 5.21
CHEMBL472508 IC50 = 20000.0 nM 4.70
CHEMBL530555 IC50 - -
CHEMBL488681 IC50 - -
CHEMBL511844 IC50 - -
CHEMBL512532 IC50 - -
CHEMBL513427 IC50 - -
CHEMBL1628094 IC50 - -
CHEMBL472167 IC50 - -
CHEMBL470948 IC50 > 50000.0 nM -
CHEMBL446912 IC50 - -
CHEMBL512535 IC50 - -
CHEMBL471998 IC50 - -