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Assay Detail

CHEMBL4261346

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 after 20 mins in presence of NAD+ by radio-flow detector based analysis
36
Total Activities
36
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

Highly Potent 17β-HSD2 Inhibitors with a Promising Pharmacokinetic Profile for Targeted Osteoporosis Therapy.
Siebenbuerger L, Hernandez-Olmos V, Abdelsamie AS, Frotscher M, van Koppen CJ, Marchais-Oberwinkler S, Scheuer C, Laschke MW, Menger MD, Boerger C, Hartmann RW.
J Med Chem (2018) 61 : 10724 -10738
PubMed 30480443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 8.48 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4293115 1 9.49
CHEMBL4295076 1 9.20
CHEMBL4276934 1 9.07
CHEMBL4287575 1 8.96
CHEMBL4284771 1 8.96
CHEMBL4293119 1 8.96
CHEMBL4286251 1 8.89
CHEMBL4292910 1 8.89
CHEMBL4092593 1 8.85
CHEMBL4283851 1 8.80
CHEMBL4283199 1 8.74
CHEMBL4285743 1 8.70
CHEMBL4276985 1 8.66
CHEMBL4291052 1 8.64
CHEMBL4290218 1 8.64
CHEMBL4291714 1 8.59
CHEMBL4286141 1 8.57
CHEMBL4286097 1 8.51
CHEMBL4277596 1 8.47
CHEMBL4282320 1 8.42
CHEMBL4279043 1 8.40
CHEMBL4278956 1 8.36
CHEMBL4282780 1 8.35
CHEMBL4289526 1 8.28
CHEMBL4280913 1 8.27
CHEMBL4277362 1 8.27
CHEMBL4288656 1 8.24
CHEMBL4292504 1 8.22
CHEMBL4278851 1 8.20
CHEMBL4288245 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4293115 IC50 = 0.32 nM 9.49
CHEMBL4295076 IC50 = 0.63 nM 9.20
CHEMBL4276934 IC50 = 0.85 nM 9.07
CHEMBL4287575 IC50 = 1.1 nM 8.96
CHEMBL4284771 IC50 = 1.1 nM 8.96
CHEMBL4293119 IC50 = 1.1 nM 8.96
CHEMBL4286251 IC50 = 1.3 nM 8.89
CHEMBL4292910 IC50 = 1.3 nM 8.89
CHEMBL4092593 IC50 = 1.4 nM 8.85
CHEMBL4283851 IC50 = 1.6 nM 8.80
CHEMBL4283199 IC50 = 1.8 nM 8.74
CHEMBL4285743 IC50 = 2.0 nM 8.70
CHEMBL4276985 IC50 = 2.2 nM 8.66
CHEMBL4291052 IC50 = 2.3 nM 8.64
CHEMBL4290218 IC50 = 2.3 nM 8.64
CHEMBL4291714 IC50 = 2.6 nM 8.59
CHEMBL4286141 IC50 = 2.7 nM 8.57
CHEMBL4286097 IC50 = 3.1 nM 8.51
CHEMBL4277596 IC50 = 3.4 nM 8.47
CHEMBL4282320 IC50 = 3.8 nM 8.42
CHEMBL4279043 IC50 = 4.0 nM 8.40
CHEMBL4278956 IC50 = 4.4 nM 8.36
CHEMBL4282780 IC50 = 4.5 nM 8.35
CHEMBL4289526 IC50 = 5.2 nM 8.28
CHEMBL4280913 IC50 = 5.4 nM 8.27
CHEMBL4277362 IC50 = 5.4 nM 8.27
CHEMBL4288656 IC50 = 5.8 nM 8.24
CHEMBL4292504 IC50 = 6.0 nM 8.22
CHEMBL4278851 IC50 = 6.3 nM 8.20
CHEMBL4288245 IC50 = 7.1 nM 8.15
CHEMBL4287316 IC50 = 8.9 nM 8.05
CHEMBL4294197 IC50 = 9.2 nM 8.04
CHEMBL4286742 IC50 = 10.0 nM 8.00
CHEMBL4289240 IC50 = 10.0 nM 8.00
CHEMBL4289569 IC50 = 11.0 nM 7.96
CHEMBL4104610 IC50 = 299.0 nM 6.52