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Assay Detail

CHEMBL3107402

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

Binding
Inhibition of COX-2 in human whole blood assessed as prostaglandin E2 production by RIA
7
Total Activities
5
Compounds Tested
2
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

Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors.
Biava M, Battilocchio C, Poce G, Alfonso S, Consalvi S, Di Capua A, Calderone V, Martelli A, Testai L, Sautebin L, Rossi A, Ghelardini C, Di Cesare Mannelli L, Giordani A, Persiani S, Colovic M, Dovizio M, Patrignani P, Anzini M.
Bioorg Med Chem (2014) 22 : 772 -786
PubMed 24373735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.49 6.27
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 6.27
CHEMBL3104539 1 5.85
CHEMBL3104556 2 5.77
CHEMBL3104551 1 4.86
CHEMBL3104549 2 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 540.0 nM 6.27
CHEMBL3104539 IC50 = 1400.0 nM 5.85
CHEMBL3104556 IC50 = 1700.0 nM 5.77
CHEMBL3104551 IC50 = 13700.0 nM 4.86
CHEMBL3104549 IC50 = 21000.0 nM 4.68
CHEMBL3104549 Inhibition - % -
CHEMBL3104556 Inhibition - % -