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Assay Detail

CHEMBL2155294

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

Binding
Inhibition of COX2-mediated 2-arachidonoylglycerol oxygenation in LPS/IFN-gamma-stimulated mouse RAW264.7 cells assessed as 2-AG to PGE2-G/PGD2-G conversion treated 2 hrs after LPS/IFN-gamma stimulation measured after 6 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type RAW264.7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL4321)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Substrate-Selective Inhibition of Cyclooxygenase-2: Development and Evaluation of Achiral Profen Probes.
Windsor MA, Hermanson DJ, Kingsley PJ, Xu S, Crews BC, Ho W, Keenan CM, Banerjee S, Sharkey KA, Marnett LJ.
ACS Med Chem Lett (2012) 3 : 759 -763
PubMed 22984634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.60 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152245 DESMETHYLFLURBIPROFEN 1 6.22
CHEMBL190083 TARENFLURBIL 3.0 1 5.89
CHEMBL380853 1 5.28
CHEMBL194760 1 4.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152245 DESMETHYLFLURBIPROFEN IC50 = 600.0 nM 6.22
CHEMBL190083 TARENFLURBIL IC50 = 1300.0 nM 5.89
CHEMBL380853 IC50 = 5200.0 nM 5.28
CHEMBL194760 IC50 = 10200.0 nM 4.99