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Assay Detail

CHEMBL4361968

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

Binding
Inhibition of recombinant rat 17beta-HSD1 expressed in HEK293 cells using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estradiol 17-beta-dehydrogenase 1 (CHEMBL1914267)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, Synthesis, and Biological Characterization of Orally Active 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.
Abdelsamie AS, Salah M, Siebenbürger L, Merabet A, Scheuer C, Frotscher M, Müller ST, Zierau O, Vollmer G, Menger MD, Laschke MW, van Koppen CJ, Marchais-Oberwinkler S, Hartmann RW.
J Med Chem (2019) 62 : 7289 -7301
PubMed 31343176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.70 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4518587 1 8.05
CHEMBL4441313 1 6.46
CHEMBL4513439 1 6.41
CHEMBL4447938 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4518587 IC50 = 9.0 nM 8.05
CHEMBL4441313 IC50 = 350.0 nM 6.46
CHEMBL4513439 IC50 = 388.0 nM 6.41
CHEMBL4447938 IC50 = 1334.0 nM 5.88