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Assay Detail

CHEMBL4373434

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

Binding
Inhibition of Wnt3a activated Wnt/beta-catenin signaling (unknown origin) expressed in HEK293 cells harboring TCF/LEF-responsive luciferase preincubated with cells followed by Wnt3a addition and measured after 24 hrs by luciferase reporter gene assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Triazole-Based Inhibitors of the Wnt/β-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice.
Obianom ON, Ai Y, Li Y, Yang W, Guo D, Yang H, Sakamuru S, Xia M, Xue F, Shu Y.
J Med Chem (2019) 62 : 727 -741
PubMed 30605343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.76 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4588097 1 8.92
CHEMBL4454905 1 8.39
CHEMBL4443889 1 8.33
CHEMBL4518078 1 8.12
CHEMBL4483450 1 7.75
CHEMBL4587547 1 7.60
CHEMBL4466405 1 7.47
CHEMBL4483069 1 6.85
CHEMBL4457105 1 6.64
CHEMBL4534612 1 6.57
CHEMBL4446719 1 6.41
CHEMBL1201303 PYRVINIUM 4.0 1 6.12
CHEMBL4439672 1 6.08
CHEMBL4524301 1 5.92
CHEMBL4458449 1 5.89
CHEMBL4462558 1 5.72
CHEMBL4472031 1 5.31
CHEMBL4584567 1 5.26
CHEMBL4566481 1 5.06
CHEMBL4439010 1 -
CHEMBL4465410 1 -
CHEMBL4438746 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4588097 IC50 = 1.2 nM 8.92
CHEMBL4454905 IC50 = 4.1 nM 8.39
CHEMBL4443889 IC50 = 4.7 nM 8.33
CHEMBL4518078 IC50 = 7.6 nM 8.12
CHEMBL4483450 IC50 = 18.0 nM 7.75
CHEMBL4587547 IC50 = 25.0 nM 7.60
CHEMBL4466405 IC50 = 34.0 nM 7.47
CHEMBL4483069 IC50 = 140.0 nM 6.85
CHEMBL4457105 IC50 = 230.0 nM 6.64
CHEMBL4534612 IC50 = 270.0 nM 6.57
CHEMBL4446719 IC50 = 390.0 nM 6.41
CHEMBL1201303 PYRVINIUM IC50 = 750.0 nM 6.12
CHEMBL4439672 IC50 = 830.0 nM 6.08
CHEMBL4524301 IC50 = 1200.0 nM 5.92
CHEMBL4458449 IC50 = 1300.0 nM 5.89
CHEMBL4462558 IC50 = 1900.0 nM 5.72
CHEMBL4472031 IC50 = 4900.0 nM 5.31
CHEMBL4584567 IC50 = 5500.0 nM 5.26
CHEMBL4566481 IC50 = 8800.0 nM 5.06
CHEMBL4439010 IC50 > 10000.0 nM -
CHEMBL4465410 IC50 > 10000.0 nM -
CHEMBL4438746 IC50 > 10000.0 nM -