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Assay Detail

CHEMBL4051804

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

ADMET
Inhibition of human placental cytosolic 17beta-HSD2 using [3H]-E2/E2 substrate and NAD+ after 20 mins by HPLC based radio-detection method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

17-beta-hydroxysteroid dehydrogenase type 2 (CHEMBL2789)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First Dual Inhibitors of Steroid Sulfatase (STS) and 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Designed Multiple Ligands as Novel Potential Therapeutics for Estrogen-Dependent Diseases.
Salah M, Abdelsamie AS, Frotscher M.
J Med Chem (2017) 60 : 4086 -4092
PubMed 28406629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.64 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088890 1 8.39
CHEMBL4102153 1 7.86
CHEMBL4066635 1 7.76
CHEMBL4072794 1 7.74
CHEMBL4064200 1 7.72
CHEMBL4091943 1 7.65
CHEMBL4099681 1 7.63
CHEMBL4076477 1 7.55
CHEMBL4083248 1 7.51
CHEMBL4078356 1 7.50
CHEMBL4071245 1 7.44
CHEMBL4084183 1 7.40
CHEMBL4071588 1 7.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088890 IC50 = 4.1 nM 8.39
CHEMBL4102153 IC50 = 13.7 nM 7.86
CHEMBL4066635 IC50 = 17.4 nM 7.76
CHEMBL4072794 IC50 = 18.4 nM 7.74
CHEMBL4064200 IC50 = 19.1 nM 7.72
CHEMBL4091943 IC50 = 22.2 nM 7.65
CHEMBL4099681 IC50 = 23.2 nM 7.63
CHEMBL4076477 IC50 = 28.0 nM 7.55
CHEMBL4083248 IC50 = 31.2 nM 7.51
CHEMBL4078356 IC50 = 31.3 nM 7.50
CHEMBL4071245 IC50 = 36.1 nM 7.44
CHEMBL4084183 IC50 = 40.0 nM 7.40
CHEMBL4071588 IC50 = 71.3 nM 7.15