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Assay Detail

CHEMBL4339580

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

Binding
Inhibition of C-terminal fluorescein-labeled human TCF4 (7 to 51 residues) binding to wild-type C-terminal His6-tagged beta-catenin (138 to 781 residues) expressed in Escherichia coli BL21 DE3 measured after 2.5 hrs by fluorescence polarization assay
ChEMBL ↗
116
Total Activities
58
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Catenin beta-1 (CHEMBL5866) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Peptidomimetics as Selective Inhibitors for the β-Catenin/T-Cell Factor Protein-Protein Interaction.
Wang Z, Zhang M, Wang J, Ji H.
J Med Chem (2019) 62 : 3617 -3635
PubMed 30856332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 4.69 5.77
Ki 58 5.23 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4548532 — — 2 6.36
CHEMBL4451478 — — 2 6.19
CHEMBL4464142 — — 2 5.82
CHEMBL4464433 — — 2 5.72
CHEMBL4450852 — — 2 5.72
CHEMBL4449577 — — 2 5.66
CHEMBL4515157 — — 2 5.64
CHEMBL4579221 — — 2 5.62
CHEMBL4460073 — — 2 5.60
CHEMBL4455488 — — 2 5.58
CHEMBL4565782 — — 2 5.58
CHEMBL4532791 — — 2 5.57
CHEMBL4560197 — — 2 5.54
CHEMBL4456139 — — 2 5.51
CHEMBL4538548 — — 2 5.48
CHEMBL4535419 — — 2 5.48
CHEMBL4464915 — — 2 5.48
CHEMBL4515538 — — 2 5.44
CHEMBL4451874 — — 2 5.43
CHEMBL3260853 — — 2 5.42
CHEMBL4561695 — — 2 5.41
CHEMBL4544508 — — 2 5.37
CHEMBL4591545 — — 2 5.35
CHEMBL4577989 — — 2 5.31
CHEMBL4465565 — — 2 5.28
CHEMBL4590084 — — 2 5.18
CHEMBL4483303 — — 2 5.17
CHEMBL4446715 — — 2 5.12
CHEMBL4437760 — — 2 5.10
CHEMBL4437433 — — 2 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4548532 — Ki = 440.0 nM 6.36
CHEMBL4451478 — Ki = 640.0 nM 6.19
CHEMBL4464142 — Ki = 1500.0 nM 5.82
CHEMBL4548532 — IC50 = 1700.0 nM 5.77
CHEMBL4450852 — Ki = 1900.0 nM 5.72
CHEMBL4464433 — Ki = 1900.0 nM 5.72
CHEMBL4449577 — Ki = 2200.0 nM 5.66
CHEMBL4515157 — Ki = 2300.0 nM 5.64
CHEMBL4579221 — Ki = 2400.0 nM 5.62
CHEMBL4460073 — Ki = 2500.0 nM 5.60
CHEMBL4451478 — IC50 = 2500.0 nM 5.60
CHEMBL4455488 — Ki = 2600.0 nM 5.58
CHEMBL4565782 — Ki = 2600.0 nM 5.58
CHEMBL4532791 — Ki = 2700.0 nM 5.57
CHEMBL4560197 — Ki = 2900.0 nM 5.54
CHEMBL4456139 — Ki = 3100.0 nM 5.51
CHEMBL4464915 — Ki = 3300.0 nM 5.48
CHEMBL4535419 — Ki = 3300.0 nM 5.48
CHEMBL4538548 — Ki = 3300.0 nM 5.48
CHEMBL4515538 — Ki = 3600.0 nM 5.44
CHEMBL4451874 — Ki = 3700.0 nM 5.43
CHEMBL3260853 — Ki = 3800.0 nM 5.42
CHEMBL4561695 — Ki = 3900.0 nM 5.41
CHEMBL4544508 — Ki = 4300.0 nM 5.37
CHEMBL4591545 — Ki = 4500.0 nM 5.35
CHEMBL4577989 — Ki = 4900.0 nM 5.31
CHEMBL4465565 — Ki = 5200.0 nM 5.28
CHEMBL4464142 — IC50 = 5900.0 nM 5.23
CHEMBL4590084 — Ki = 6600.0 nM 5.18
CHEMBL4483303 — Ki = 6700.0 nM 5.17
CHEMBL4464433 — IC50 = 7300.0 nM 5.14
CHEMBL4450852 — IC50 = 7500.0 nM 5.12
CHEMBL4446715 — Ki = 7600.0 nM 5.12
CHEMBL4437760 — Ki = 8000.0 nM 5.10
CHEMBL4437433 — Ki = 8500.0 nM 5.07
CHEMBL4449577 — IC50 = 8500.0 nM 5.07
CHEMBL4515157 — IC50 = 8900.0 nM 5.05
CHEMBL4471868 — Ki = 8900.0 nM 5.05
CHEMBL4471027 — Ki = 9300.0 nM 5.03
CHEMBL4579221 — IC50 = 9300.0 nM 5.03
CHEMBL4561875 — Ki = 9600.0 nM 5.02
CHEMBL4452305 — Ki = 9700.0 nM 5.01
CHEMBL4460073 — IC50 = 9800.0 nM 5.01
CHEMBL4583661 — Ki = 10000.0 nM 5.00
CHEMBL4584378 — Ki = 10000.0 nM 5.00
CHEMBL4565782 — IC50 = 10000.0 nM 5.00
CHEMBL4455488 — IC50 = 10000.0 nM 5.00
CHEMBL4552917 — Ki = 11000.0 nM 4.96
CHEMBL4532791 — IC50 = 11000.0 nM 4.96
CHEMBL4560197 — IC50 = 11000.0 nM 4.96