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Assay Detail

CHEMBL3413189

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Binding
Inhibition of WNT signaling in human T-Rex HEK293 Tet-O cells harboring dominant negative form of Axin GSK3beta-interacting domain after 4 days by luciferase reporter assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.
Mallinger A, Crumpler S, Pichowicz M, Waalboer D, Stubbs M, Adeniji-Popoola O, Wood B, Smith E, Thai C, Henley AT, Georgi K, Court W, Hobbs S, Box G, Ortiz-Ruiz MJ, Valenti M, De Haven Brandon A, TePoele R, Leuthner B, Workman P, Aherne W, Poeschke O, Dale T, Wienke D, Esdar C, Rohdich F, Raynaud F, Clarke PA, Eccles SA, Stieber F, Schiemann K, Blagg J.
J Med Chem (2015) 58 : 1717 -1735
PubMed 25680029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.72 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408184 1 7.62
CHEMBL1673059 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408184 IC50 = 24.0 nM 7.62
CHEMBL1673059 IC50 = 1500.0 nM 5.82