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Assay Detail

CHEMBL3631247

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

Binding
Inhibition of mouse liver microsomal 17beta HSD2 using unlabeled- and labelled [2,4,6,7-3H]-E2 as substrate incubated for 20 mins by HPLC analysis
3
Total Activities
3
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

Estradiol 17-beta-dehydrogenase 2 (CHEMBL1914270)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.
Abdelsamie AS, Bey E, Gargano EM, van Koppen CJ, Empting M, Frotscher M.
Eur J Med Chem (2015) 103 : 56 -68
PubMed 26322835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.28 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3629587 1 7.70
CHEMBL3629591 1 7.26
CHEMBL3629592 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3629587 IC50 = 20.0 nM 7.70
CHEMBL3629591 IC50 = 55.0 nM 7.26
CHEMBL3629592 IC50 = 129.0 nM 6.89