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Assay Detail

CHEMBL4810405

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

Functional
Chemo-protective activity in C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as reduction in 18F-FDG uptake in ileum at 300 mg/kg, po incorporated into chow diet administered daily for 2 weeks and measured after 14 days by ex vivo PET imaging analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Zhang Z, Ghosh A, Connolly PJ, King P, Wilde T, Wang J, Dong Y, Li X, Liao D, Chen H, Tian G, Suarez J, Bonnette WG, Pande V, Diloreto KA, Shi Y, Patel S, Pietrak B, Szewczuk L, Sensenhauser C, Dallas S, Edwards JP, Bachman KE, Evans DC.
J Med Chem (2021) 64 : 11570 -11596
PubMed 34279934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.15 5.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4868446 1 5.38
CHEMBL4862802 1 5.36
CHEMBL4870569 1 5.26
CHEMBL4865464 1 4.89
CHEMBL4857474 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4868446 IC50 = 4200.0 nM 5.38
CHEMBL4862802 IC50 = 4400.0 nM 5.36
CHEMBL4870569 IC50 = 5500.0 nM 5.26
CHEMBL4865464 IC50 = 13000.0 nM 4.89
CHEMBL4857474 IC50 = 14000.0 nM 4.85