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Assay Detail

CHEMBL4415263

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

Binding
Inhibition of COX2 in LPS-stimulated human monocytes assessed as reduction in PGE2 production by LC-tandem MIS analysis
2
Total Activities
2
Compounds Tested
1
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

Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.
Kramer JS, Woltersdorf S, Duflot T, Hiesinger K, Lillich FF, Knöll F, Wittmann SK, Klingler FM, Brunst S, Chaikuad A, Morisseau C, Hammock BD, Buccellati C, Sala A, Rovati GE, Leuillier M, Fraineau S, Rondeaux J, Hernandez-Olmos V, Heering J, Merk D, Pogoryelov D, Steinhilber D, Knapp S, Bellien J, Proschak E.
J Med Chem (2019) 62 : 8443 -8460
PubMed 31436984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.67 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1071 OXAPROZIN 4.0 1 6.96
CHEMBL4445524 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1071 OXAPROZIN IC50 = 110.0 nM 6.96
CHEMBL4445524 IC50 = 420.0 nM 6.38