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Assay Detail

CHEMBL4361954

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

Binding
Inhibition of human placental cytosolic fraction 17beta-HSD1 using [3H]-E1 as substrate in presence of NAD+ by radio-HPLC analysis
22
Total Activities
22
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

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 22 8.08 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4466918 1 9.22
CHEMBL4441152 1 8.92
CHEMBL4585585 1 8.70
CHEMBL4443578 1 8.64
CHEMBL4576023 1 8.51
CHEMBL4513439 1 8.41
CHEMBL4459275 1 8.41
CHEMBL4443361 1 8.37
CHEMBL4439604 1 8.34
CHEMBL4474456 1 8.30
CHEMBL4455556 1 8.20
CHEMBL4471724 1 8.16
CHEMBL4584616 1 8.06
CHEMBL4447938 1 8.00
CHEMBL4450450 1 8.00
CHEMBL4470668 1 7.94
CHEMBL4441313 1 7.76
CHEMBL4519484 1 7.68
CHEMBL4462505 1 7.34
CHEMBL4518587 1 7.34
CHEMBL4453509 1 6.77
CHEMBL4441357 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4466918 IC50 = 0.6 nM 9.22
CHEMBL4441152 IC50 = 1.2 nM 8.92
CHEMBL4585585 IC50 = 2.0 nM 8.70
CHEMBL4443578 IC50 = 2.3 nM 8.64
CHEMBL4576023 IC50 = 3.1 nM 8.51
CHEMBL4513439 IC50 = 3.9 nM 8.41
CHEMBL4459275 IC50 = 3.9 nM 8.41
CHEMBL4443361 IC50 = 4.3 nM 8.37
CHEMBL4439604 IC50 = 4.6 nM 8.34
CHEMBL4474456 IC50 = 5.0 nM 8.30
CHEMBL4455556 IC50 = 6.3 nM 8.20
CHEMBL4471724 IC50 = 6.9 nM 8.16
CHEMBL4584616 IC50 = 8.8 nM 8.06
CHEMBL4447938 IC50 = 10.1 nM 8.00
CHEMBL4450450 IC50 = 10.0 nM 8.00
CHEMBL4470668 IC50 = 11.4 nM 7.94
CHEMBL4441313 IC50 = 17.2 nM 7.76
CHEMBL4519484 IC50 = 21.0 nM 7.68
CHEMBL4462505 IC50 = 45.4 nM 7.34
CHEMBL4518587 IC50 = 45.8 nM 7.34
CHEMBL4453509 IC50 = 170.0 nM 6.77
CHEMBL4441357 IC50 = 198.0 nM 6.70