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Assay Detail

CHEMBL3873629

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

Binding
Inhibition of mPGES-1 in guinea pig whole blood assessed as reduction in LPS-induced PGE2 production preincubated followed by LPS stimulation for 20 to 24 hrs
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Blood
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of 2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2',3':3,4]benzo[1,2-d]imidazole-5-carboxamide as potent, selective and efficacious microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor.
Muthukaman N, Deshmukh S, Sarode N, Tondlekar S, Tambe M, Pisal D, Shaikh M, Kattige VG, Honnegowda S, Karande V, Kulkarni A, Jadhav SB, Mahat MYA, Gudi GS, Khairatkar-Joshi N, Gharat LA.
Bioorg Med Chem Lett (2016) 26 : 5977 -5984
PubMed 27865703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.42 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3897959 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3897959 IC50 = 380.9 nM 6.42