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Assay Detail

CHEMBL2020637

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

Binding
Inhibition of beta-casein/TCF4 pathway expressed in HCT116 cells containing delta45S mutant after 24 hrs by luciferase reporter gene assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HCT-116
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

TCF4/beta-catenin (CHEMBL3038511)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors.
Mao Y, Lin N, Tian W, Han X, Han X, Huang Z, An J.
J Med Chem (2012) 55 : 1346 -1359
PubMed 22229647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.61 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018626 1 6.00
CHEMBL2018615 1 5.82
CHEMBL2018726 1 5.82
CHEMBL2018727 1 5.70
CHEMBL2018623 1 5.70
CHEMBL2018734 1 5.60
CHEMBL2018597 1 5.60
CHEMBL2018621 1 5.60
CHEMBL2018622 1 5.60
CHEMBL2018733 1 5.52
CHEMBL2018617 1 5.52
CHEMBL2018598 1 5.52
CHEMBL2018728 1 5.52
CHEMBL2018732 1 5.52
CHEMBL2018614 1 5.52
CHEMBL569102 1 5.46
CHEMBL2018729 1 5.46
CHEMBL2018612 1 5.46
CHEMBL2018618 1 -
CHEMBL2018735 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018626 IC50 = 1000.0 nM 6.00
CHEMBL2018615 IC50 = 1500.0 nM 5.82
CHEMBL2018726 IC50 = 1500.0 nM 5.82
CHEMBL2018727 IC50 = 2000.0 nM 5.70
CHEMBL2018623 IC50 = 2000.0 nM 5.70
CHEMBL2018734 IC50 = 2500.0 nM 5.60
CHEMBL2018597 IC50 = 2500.0 nM 5.60
CHEMBL2018621 IC50 = 2500.0 nM 5.60
CHEMBL2018622 IC50 = 2500.0 nM 5.60
CHEMBL2018733 IC50 = 3000.0 nM 5.52
CHEMBL2018617 IC50 = 3000.0 nM 5.52
CHEMBL2018598 IC50 = 3000.0 nM 5.52
CHEMBL2018728 IC50 = 3000.0 nM 5.52
CHEMBL2018732 IC50 = 3000.0 nM 5.52
CHEMBL2018614 IC50 = 3000.0 nM 5.52
CHEMBL569102 IC50 = 3500.0 nM 5.46
CHEMBL2018729 IC50 = 3500.0 nM 5.46
CHEMBL2018612 IC50 = 3500.0 nM 5.46
CHEMBL2018618 IC50 > 5000.0 nM -
CHEMBL2018735 IC50 > 5000.0 nM -