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Assay Detail

CHEMBL4178554

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

Binding
Inhibition of human 17beta-HSD1 expressed in HEK293 cell lysates incubated for 10 mins using [2,4,6,7-3H]-estrone and NADPH by scintillation counting method
10
Total Activities
10
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 1 (CHEMBL3181)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potential Antiosteoporotic Natural Product Lead Compounds That Inhibit 17β-Hydroxysteroid Dehydrogenase Type 2.
Vuorinen A, Engeli RT, Leugger S, Bachmann F, Akram M, Atanasov AG, Waltenberger B, Temml V, Stuppner H, Krenn L, Ateba SB, Njamen D, Davis RA, Odermatt A, Schuster D.
J Nat Prod (2017) 80 : 965 -974
PubMed 28319389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.84 7.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312186 1 7.31
CHEMBL6665 1 5.96
CHEMBL129795 ISOLIQUIRITIGENIN 1 5.55
CHEMBL52 NORDIHYDROGUAIARETIC ACID 1 5.26
CHEMBL375927 (-)-DIHYDROGUAIARETICACID 1 5.11
CHEMBL324842 ROSMARINIC ACID 1 -
CHEMBL4206971 1 -
CHEMBL601464 1 -
CHEMBL589354 1 -
CHEMBL4205522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312186 IC50 = 49.0 nM 7.31
CHEMBL6665 IC50 = 1090.0 nM 5.96
CHEMBL129795 ISOLIQUIRITIGENIN IC50 = 2830.0 nM 5.55
CHEMBL52 NORDIHYDROGUAIARETIC ACID IC50 = 5500.0 nM 5.26
CHEMBL375927 (-)-DIHYDROGUAIARETICACID IC50 = 7700.0 nM 5.11
CHEMBL324842 ROSMARINIC ACID IC50 - -
CHEMBL4206971 IC50 - -
CHEMBL601464 IC50 - -
CHEMBL589354 IC50 - -
CHEMBL4205522 IC50 - -