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Assay Detail

CHEMBL4400642

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
16
Total Activities
16
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

Targeted Endocrine Therapy: Design, Synthesis, and Proof-of-Principle of 17β-Hydroxysteroid Dehydrogenase Type 2 Inhibitors in Bone Fracture Healing.
Abdelsamie AS, Herath S, Biskupek Y, Börger C, Siebenbürger L, Salah M, Scheuer C, Marchais-Oberwinkler S, Frotscher M, Pohlemann T, Menger MD, Hartmann RW, Laschke MW, van Koppen CJ.
J Med Chem (2019) 62 : 1362 -1372
PubMed 30645111 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.49 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457145 1 10.00
CHEMBL4529443 1 10.00
CHEMBL4546082 1 9.15
CHEMBL4464314 1 9.10
CHEMBL4441152 1 8.92
CHEMBL4582194 1 8.85
CHEMBL4538007 1 8.77
CHEMBL4450585 1 8.62
CHEMBL4552641 1 8.32
CHEMBL4285743 1 8.22
CHEMBL4461477 1 8.14
CHEMBL4519897 1 8.09
CHEMBL4459887 1 7.81
CHEMBL4574253 1 7.69
CHEMBL3629438 1 7.68
CHEMBL4459492 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457145 IC50 = 0.1 nM 10.00
CHEMBL4529443 IC50 = 0.1 nM 10.00
CHEMBL4546082 IC50 = 0.7 nM 9.15
CHEMBL4464314 IC50 = 0.8 nM 9.10
CHEMBL4441152 IC50 = 1.2 nM 8.92
CHEMBL4582194 IC50 = 1.4 nM 8.85
CHEMBL4538007 IC50 = 1.7 nM 8.77
CHEMBL4450585 IC50 = 2.4 nM 8.62
CHEMBL4552641 IC50 = 4.8 nM 8.32
CHEMBL4285743 IC50 = 6.0 nM 8.22
CHEMBL4461477 IC50 = 7.2 nM 8.14
CHEMBL4519897 IC50 = 8.2 nM 8.09
CHEMBL4459887 IC50 = 15.6 nM 7.81
CHEMBL4574253 IC50 = 20.3 nM 7.69
CHEMBL3629438 IC50 = 21.0 nM 7.68
CHEMBL4459492 IC50 = 306.0 nM 6.51