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Assay Detail

CHEMBL940137

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

Binding
Inhibition of 17beta-HSD1 expressed in intact human T47D cells after 30 mins
36
Total Activities
36
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type T47D
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

17-beta-hydroxysteroid dehydrogenase type 1 (CHEMBL3181)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel inhibitors of 17beta-hydroxysteroid dehydrogenase type 1: templates for design.
Allan GM, Vicker N, Lawrence HR, Tutill HJ, Day JM, Huchet M, Ferrandis E, Reed MJ, Purohit A, Potter BV.
Bioorg Med Chem (2008) 16 : 4438 -4456
PubMed 18329273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 22 - -
IC50 14 5.53 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407968 1 7.57
CHEMBL408487 1 5.77
CHEMBL410224 1 5.75
CHEMBL259000 1 5.70
CHEMBL408485 1 5.54
CHEMBL261578 1 5.43
CHEMBL260518 1 5.43
CHEMBL408594 1 5.43
CHEMBL260227 1 5.33
CHEMBL260234 1 5.32
CHEMBL260075 1 5.27
CHEMBL259815 1 5.08
CHEMBL407865 1 5.00
CHEMBL259814 1 4.81
CHEMBL260590 1 -
CHEMBL260802 1 -
CHEMBL258783 1 -
CHEMBL427905 1 -
CHEMBL258784 1 -
CHEMBL261157 1 -
CHEMBL261158 1 -
CHEMBL260710 1 -
CHEMBL261335 1 -
CHEMBL406542 1 -
CHEMBL260512 1 -
CHEMBL259205 1 -
CHEMBL259204 1 -
CHEMBL259203 1 -
CHEMBL259817 1 -
CHEMBL261844 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407968 IC50 = 27.0 nM 7.57
CHEMBL408487 IC50 = 1700.0 nM 5.77
CHEMBL410224 IC50 = 1800.0 nM 5.75
CHEMBL259000 IC50 = 2000.0 nM 5.70
CHEMBL408485 IC50 = 2900.0 nM 5.54
CHEMBL261578 IC50 = 3700.0 nM 5.43
CHEMBL260518 IC50 = 3700.0 nM 5.43
CHEMBL408594 IC50 = 3700.0 nM 5.43
CHEMBL260227 IC50 = 4700.0 nM 5.33
CHEMBL260234 IC50 = 4800.0 nM 5.32
CHEMBL260075 IC50 = 5400.0 nM 5.27
CHEMBL259815 IC50 = 8300.0 nM 5.08
CHEMBL407865 IC50 = 9900.0 nM 5.00
CHEMBL259814 IC50 = 15600.0 nM 4.81
CHEMBL261576 Inhibition - % -
CHEMBL261843 Inhibition - % -
CHEMBL261842 Inhibition - % -
CHEMBL261740 Inhibition - % -
CHEMBL259228 Inhibition - % -
CHEMBL260589 Inhibition - % -
CHEMBL260590 Inhibition - % -
CHEMBL260802 Inhibition - % -
CHEMBL258783 Inhibition - % -
CHEMBL427905 Inhibition - % -
CHEMBL258784 Inhibition - % -
CHEMBL261157 Inhibition - % -
CHEMBL261158 Inhibition - % -
CHEMBL260710 Inhibition - % -
CHEMBL261335 Inhibition - % -
CHEMBL406542 Inhibition - % -
CHEMBL260512 Inhibition - % -
CHEMBL259205 Inhibition - % -
CHEMBL259204 Inhibition - % -
CHEMBL259203 Inhibition - % -
CHEMBL259817 Inhibition - % -
CHEMBL261844 Inhibition - % -