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Assay Detail

CHEMBL3821983

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

Binding
Competitive inhibition of wild type beta-catenin (unknown origin) expressed in Escherichia coli BL21 DE3 interaction with N-terminally biotinylated human BCL9 (350 to 375 residues) by alpha screen assay
24
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

beta-catenin-B-cell lymphoma 9 protein complex (CHEMBL3885525)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Structure-Based Design of 1,4-Dibenzoylpiperazines as β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction Inhibitors.
Wisniewski JA, Yin J, Teuscher KB, Zhang M, Ji H.
ACS Med Chem Lett (2016) 7 : 508 -513
PubMed 27190602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 4.53 5.68
IC50 1 5.25 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3819630 1 5.68
CHEMBL3819506 2 5.28
CHEMBL484853 CARNOSIC ACID 1 5.28
CHEMBL3819020 1 4.80
CHEMBL3818707 1 4.72
CHEMBL3819288 1 4.70
CHEMBL3819165 1 4.60
CHEMBL3818097 1 4.46
CHEMBL3819088 1 4.43
CHEMBL3818263 1 4.35
CHEMBL3819332 1 4.32
CHEMBL3818667 1 4.28
CHEMBL3818058 1 4.26
CHEMBL3819368 1 4.24
CHEMBL3818956 1 4.17
CHEMBL3818207 1 4.16
CHEMBL3818280 1 4.16
CHEMBL3817935 1 4.12
CHEMBL3818949 1 4.09
CHEMBL3818029 1 -
CHEMBL3819443 1 -
CHEMBL3818748 1 -
CHEMBL3818840 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3819630 Ki = 2100.0 nM 5.68
CHEMBL3819506 Ki = 5200.0 nM 5.28
CHEMBL484853 CARNOSIC ACID Ki = 5300.0 nM 5.28
CHEMBL3819506 IC50 = 5600.0 nM 5.25
CHEMBL3819020 Ki = 16000.0 nM 4.80
CHEMBL3818707 Ki = 19000.0 nM 4.72
CHEMBL3819288 Ki = 20000.0 nM 4.70
CHEMBL3819165 Ki = 25000.0 nM 4.60
CHEMBL3818097 Ki = 35000.0 nM 4.46
CHEMBL3819088 Ki = 37000.0 nM 4.43
CHEMBL3818263 Ki = 45000.0 nM 4.35
CHEMBL3819332 Ki = 48000.0 nM 4.32
CHEMBL3818667 Ki = 53000.0 nM 4.28
CHEMBL3818058 Ki = 55000.0 nM 4.26
CHEMBL3819368 Ki = 57000.0 nM 4.24
CHEMBL3818956 Ki = 67000.0 nM 4.17
CHEMBL3818207 Ki = 70000.0 nM 4.16
CHEMBL3818280 Ki = 69000.0 nM 4.16
CHEMBL3817935 Ki = 76000.0 nM 4.12
CHEMBL3818949 Ki = 82000.0 nM 4.09
CHEMBL3818029 Ki = 490000.0 nM -
CHEMBL3819443 Ki = 170000.0 nM -
CHEMBL3818748 Ki > 500000.0 nM -
CHEMBL3818840 Ki = 130000.0 nM -