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Assay Detail

CHEMBL3772154

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

Binding
Inhibition of microsomal PGES1 in ILbeta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E synthase (CHEMBL5658)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting microsomal prostaglandin E2synthase-1 (mPGES-1): the development of inhibitors as an alternative to non-steroidal anti-inflammatory drugs (NSAIDs)
Chen Y, Liu H, Xu S, Wang T, Li W
Medchemcomm (2015) 6 : 2081 -2123
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.06 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140 CURCUMIN 3.0 1 6.70
CHEMBL225421 ARZANOL 1 6.40
CHEMBL3134416 1 6.40
CHEMBL171637 PHYSODIC ACID 1 6.37
CHEMBL3770045 1 6.10
CHEMBL3770744 1 6.00
CHEMBL3770253 1 5.94
CHEMBL218693 CARNOSOL 1 5.30
CHEMBL484853 CARNOSIC ACID 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140 CURCUMIN IC50 = 200.0 nM 6.70
CHEMBL225421 ARZANOL IC50 = 400.0 nM 6.40
CHEMBL3134416 IC50 = 400.0 nM 6.40
CHEMBL171637 PHYSODIC ACID IC50 = 430.0 nM 6.37
CHEMBL3770045 IC50 = 800.0 nM 6.10
CHEMBL3770744 IC50 = 1000.0 nM 6.00
CHEMBL3770253 IC50 = 1150.0 nM 5.94
CHEMBL218693 CARNOSOL IC50 = 5000.0 nM 5.30
CHEMBL484853 CARNOSIC ACID IC50 = 5000.0 nM 5.30