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Assay Detail

CHEMBL4810396

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

Binding
Inhibition of COX2 in human whole blood assessed as reduction in LPS stimulated PGE2 production incubated for 1 hr by ELISA
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin G/H synthase 2 (CHEMBL230)
Type SINGLE PROTEIN
Organism Homo sapiens

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 8 6.15 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4870569 1 6.84
CHEMBL4865464 1 6.46
CHEMBL4859571 1 6.46
CHEMBL118 CELECOXIB 4.0 1 6.36
CHEMBL416146 ETORICOXIB 4.0 1 6.21
CHEMBL4868446 1 6.06
CHEMBL4862802 1 5.63
CHEMBL4857474 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4870569 IC50 = 146.0 nM 6.84
CHEMBL4865464 IC50 = 346.0 nM 6.46
CHEMBL4859571 IC50 = 345.0 nM 6.46
CHEMBL118 CELECOXIB IC50 = 440.0 nM 6.36
CHEMBL416146 ETORICOXIB IC50 = 611.0 nM 6.21
CHEMBL4868446 IC50 = 877.0 nM 6.06
CHEMBL4862802 IC50 = 2341.0 nM 5.63
CHEMBL4857474 IC50 = 7232.0 nM 5.14