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Assay Detail

CHEMBL1074444

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

Functional
Activity at EP4 receptor in human whole blood assessed as blockade of inhibition of TNF-alpha-induced IP10 release
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP4 subtype (CHEMBL1836)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Blouin M, Han Y, Burch J, Farand J, Mellon C, Gaudreault M, Wrona M, Lévesque JF, Denis D, Mathieu MC, Stocco R, Vigneault E, Therien A, Clark P, Rowland S, Xu D, O'Neill G, Ducharme Y, Friesen R.
J Med Chem (2010) 53 : 2227 -2238
PubMed 20163116 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.96 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL597997 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL597997 IC50 = 11.0 nM 7.96