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Assay Detail

CHEMBL975501

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

Binding
Inhibition of human placental 17beta-HSD2 assessed as conversion of [3H]17beta-estradiol to [3H]estrone
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokinetics.
Marchais-Oberwinkler S, Kruchten P, Frotscher M, Ziegler E, Neugebauer A, Bhoga U, Bey E, Müller-Vieira U, Messinger J, Thole H, Hartmann RW.
J Med Chem (2008) 51 : 4685 -4698
PubMed 18630892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.90 6.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469227 1 6.27
CHEMBL467151 1 6.19
CHEMBL195217 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469227 IC50 = 540.0 nM 6.27
CHEMBL467151 IC50 = 639.0 nM 6.19
CHEMBL195217 IC50 = 5641.0 nM 5.25