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Assay Detail

CHEMBL3606286

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

Binding
Inhibition of Wnt/beta-catenin in HEK293 cells assessed as inhibition of Wnt3A-stimulated TOPFlash activity after 8 hrs
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 1 — Organism
Curated By Autocuration

Target

HEK293 (CHEMBL614818)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-activity studies of Wnt/β-catenin inhibition in the Niclosamide chemotype: Identification of derivatives with improved drug exposure.
Mook RA, Wang J, Ren XR, Chen M, Spasojevic I, Barak LS, Lyerly HK, Chen W.
Bioorg Med Chem (2015) 23 : 5829 -5838
PubMed 26272032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.87 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3604905 1 6.64
CHEMBL2088014 1 6.54
CHEMBL3604908 1 6.50
CHEMBL3604904 1 6.50
CHEMBL3604907 1 6.48
CHEMBL3604906 1 6.47
CHEMBL1448 NICLOSAMIDE 4.0 1 6.47
CHEMBL3604909 1 6.43
CHEMBL3604895 1 6.38
CHEMBL3604893 1 6.26
CHEMBL2313077 1 6.25
CHEMBL2179173 1 6.16
CHEMBL100633 1 6.14
CHEMBL3604896 1 6.12
CHEMBL589733 1 6.05
CHEMBL2088010 1 6.00
CHEMBL2313091 1 5.92
CHEMBL2088012 1 5.89
CHEMBL3604898 1 5.85
CHEMBL2088011 1 5.78
CHEMBL3604903 1 5.59
CHEMBL3604894 1 5.52
CHEMBL2312822 1 5.42
CHEMBL2313078 1 5.40
CHEMBL3604890 1 5.19
CHEMBL3604891 1 5.12
CHEMBL1892375 1 4.93
CHEMBL3604901 1 4.82
CHEMBL3604892 1 4.82
CHEMBL2312829 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3604905 IC50 = 230.0 nM 6.64
CHEMBL2088014 IC50 = 290.0 nM 6.54
CHEMBL3604904 IC50 = 320.0 nM 6.50
CHEMBL3604908 IC50 = 320.0 nM 6.50
CHEMBL3604907 IC50 = 330.0 nM 6.48
CHEMBL3604906 IC50 = 340.0 nM 6.47
CHEMBL1448 NICLOSAMIDE IC50 = 340.0 nM 6.47
CHEMBL3604909 IC50 = 370.0 nM 6.43
CHEMBL3604895 IC50 = 420.0 nM 6.38
CHEMBL3604893 IC50 = 550.0 nM 6.26
CHEMBL2313077 IC50 = 560.0 nM 6.25
CHEMBL2179173 IC50 = 700.0 nM 6.16
CHEMBL100633 IC50 = 730.0 nM 6.14
CHEMBL3604896 IC50 = 750.0 nM 6.12
CHEMBL589733 IC50 = 890.0 nM 6.05
CHEMBL2088010 IC50 = 990.0 nM 6.00
CHEMBL2313091 IC50 = 1210.0 nM 5.92
CHEMBL2088012 IC50 = 1300.0 nM 5.89
CHEMBL3604898 IC50 = 1410.0 nM 5.85
CHEMBL2088011 IC50 = 1650.0 nM 5.78
CHEMBL3604903 IC50 = 2570.0 nM 5.59
CHEMBL3604894 IC50 = 3050.0 nM 5.52
CHEMBL2312822 IC50 = 3840.0 nM 5.42
CHEMBL2313078 IC50 = 4020.0 nM 5.40
CHEMBL3604890 IC50 = 6420.0 nM 5.19
CHEMBL3604891 IC50 = 7660.0 nM 5.12
CHEMBL1892375 IC50 = 11810.0 nM 4.93
CHEMBL3604901 IC50 = 15100.0 nM 4.82
CHEMBL3604892 IC50 = 15040.0 nM 4.82
CHEMBL2312829 IC50 = 32890.0 nM 4.48
CHEMBL2313086 IC50 > 12000.0 nM -
CHEMBL3604899 IC50 > 12000.0 nM -
CHEMBL3604900 IC50 > 12000.0 nM -
CHEMBL3604902 IC50 > 12000.0 nM -
CHEMBL3604897 IC50 > 12000.0 nM -
CHEMBL2312828 IC50 > 12000.0 nM -