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Assay Detail

CHEMBL3295154

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

Binding
Inhibition of COX2-mediated PGF2alpha formation in LPS-stimulated human monocytes preincubated for 15 mins before arachidonic acid substrate addition measured after 30 mins by UPLC-MS/MS analysis
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

SAR studies on curcumin's pro-inflammatory targets: discovery of prenylated pyrazolocurcuminoids as potent and selective novel inhibitors of 5-lipoxygenase.
Koeberle A, Muñoz E, Appendino GB, Minassi A, Pace S, Rossi A, Weinigel C, Barz D, Sautebin L, Caprioglio D, Collado JA, Werz O.
J Med Chem (2014) 57 : 5638 -5648
PubMed 24920381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 3 - -
IC50 2 6.91 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3290441 1 7.89
CHEMBL6 INDOMETHACIN 4.0 1 5.92
CHEMBL180239 CURCUMIN PYRAZOLE 1 -
CHEMBL2413471 1 -
CHEMBL140 CURCUMIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3290441 IC50 = 13.0 nM 7.89
CHEMBL6 INDOMETHACIN IC50 = 1200.0 nM 5.92
CHEMBL180239 CURCUMIN PYRAZOLE Inhibition - % -
CHEMBL2413471 Inhibition - % -
CHEMBL140 CURCUMIN Inhibition - % -