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Assay Detail

CHEMBL4810416

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

Functional
In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant ileum exposures
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL4321)
Type SINGLE PROTEIN
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 4 6.76 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 8.49
CHEMBL4859571 1 6.80
CHEMBL4868446 1 6.13
CHEMBL4862802 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 3.2 nM 8.49
CHEMBL4859571 IC50 = 160.0 nM 6.80
CHEMBL4868446 IC50 = 741.8 nM 6.13
CHEMBL4862802 IC50 = 2384.0 nM 5.62