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Assay Detail

CHEMBL3388004

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

Binding
Inhibition of mPGES-1 in human whole blood assessed as inhibition of LPS-induced PGE2 production incubated for 30 mins prior to LPS challenge measured after 20 to 24 hrs by LC/MS/MS analysis
1
Total Activities
1
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 E synthase (CHEMBL5658)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of 2-aryl substituted quinazolin-4(3H)-one, pyrido[4,3-d]pyrimidin-4(3H)-one and pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as microsomal prostaglandin E(2) synthase-1 inhibitors.
Banerjee A, Pawar MY, Patil S, Yadav PS, Kadam PA, Kattige VG, Deshpande DS, Pednekar PV, Pisat MK, Gharat LA.
Bioorg Med Chem Lett (2014) 24 : 4838 -4844
PubMed 25260492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.92 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342693 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342693 IC50 = 12.0 nM 7.92