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Assay Detail

CHEMBL5058469

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

Binding
Inhibition of human placental microsomal fraction 17beta-HSD2 using [3H]-E2 as substrate in presence of NAD+ measured after 20 mins by HPLC method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Placenta
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

17β-Hydroxysteroid Dehydrogenase Type 1 Inhibition: A Potential Treatment Option for Non-Small Cell Lung Cancer.
Gargano EM, Mohamed A, Abdelsamie AS, Mangiatordi GF, Drzewiecka H, Jagodziński PP, Mazzini A, van Koppen CJ, Laschke MW, Nicolotti O, Carotti A, Marchais-Oberwinkler S, Hartmann RW, Frotscher M.
ACS Med Chem Lett (2021) 12 : 1920 -1924
PubMed 34917255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.25 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087553 1 7.25
CHEMBL5090458 1 7.15
CHEMBL5089787 1 6.69
CHEMBL5074435 1 6.37
CHEMBL5089172 1 6.03
CHEMBL5078630 1 6.03
CHEMBL5084876 1 5.97
CHEMBL5076534 1 5.93
CHEMBL5093589 1 5.55
CHEMBL5080299 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087553 IC50 = 56.0 nM 7.25
CHEMBL5090458 IC50 = 71.0 nM 7.15
CHEMBL5089787 IC50 = 203.0 nM 6.69
CHEMBL5074435 IC50 = 426.0 nM 6.37
CHEMBL5089172 IC50 = 928.0 nM 6.03
CHEMBL5078630 IC50 = 927.0 nM 6.03
CHEMBL5084876 IC50 = 1077.0 nM 5.97
CHEMBL5076534 IC50 = 1171.0 nM 5.93
CHEMBL5093589 IC50 = 2786.0 nM 5.55
CHEMBL5080299 IC50 = 3155.0 nM 5.50