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Assay Detail

CHEMBL3994284

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

Binding
Inhibition of Wnt/beta-catenin signaling (unknown origin) expressed in HEK293 cells assessed as inhibition of Wnt3A-stimulated beta-catenin response transcription after 6 hrs by TOPflash dual luciferase reporter gene assay
17
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Benzimidazole inhibitors from the Niclosamide chemotype inhibit Wnt/β-catenin signaling with selectivity over effects on ATP homeostasis.
Mook RA, Ren XR, Wang J, Piao H, Barak LS, Kim Lyerly H, Chen W.
Bioorg Med Chem (2017) 25 : 1804 -1816
PubMed 28233680 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.88 6.92
Inhibition 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1448 NICLOSAMIDE 4.0 2 6.92
CHEMBL4063414 2 6.64
CHEMBL1944805 2 6.44
CHEMBL4102601 2 6.21
CHEMBL4061607 1 5.90
CHEMBL4087103 1 5.82
CHEMBL1944796 1 5.81
CHEMBL4097451 1 5.77
CHEMBL4091270 1 5.57
CHEMBL4096490 1 5.50
CHEMBL4083896 1 5.38
CHEMBL1944806 1 5.35
CHEMBL4093926 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1448 NICLOSAMIDE IC50 = 120.0 nM 6.92
CHEMBL4063414 IC50 = 230.0 nM 6.64
CHEMBL1944805 IC50 = 360.0 nM 6.44
CHEMBL4102601 IC50 = 620.0 nM 6.21
CHEMBL4061607 IC50 = 1270.0 nM 5.90
CHEMBL4087103 IC50 = 1500.0 nM 5.82
CHEMBL1944796 IC50 = 1540.0 nM 5.81
CHEMBL4097451 IC50 = 1690.0 nM 5.77
CHEMBL4091270 IC50 = 2670.0 nM 5.57
CHEMBL4096490 IC50 = 3200.0 nM 5.50
CHEMBL4083896 IC50 = 4190.0 nM 5.38
CHEMBL1944806 IC50 = 4440.0 nM 5.35
CHEMBL4093926 IC50 = 7650.0 nM 5.12
CHEMBL1944805 Inhibition - % -
CHEMBL4063414 Inhibition - % -
CHEMBL4102601 Inhibition - % -
CHEMBL1448 NICLOSAMIDE Inhibition - % -