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Assay Detail

CHEMBL4000103

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

Functional
In vivo antagonist activity at DP2 receptor in Sprague-Dawley rat DK-PGD2-induced pulmonary eosinophilia mechanistic model assessed inhibition of eosinophilia in broncho alveolar lavage fluid at 0.1 to 0.3 mg/kg, po pretreated for 40 mins starting at 2 hrs post IL-5 administration followed by DK-PGD2 administration measured after 2 hrs
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Autocuration

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma.
Sandham DA, Barker L, Brown L, Brown Z, Budd D, Charlton SJ, Chatterjee D, Cox B, Dubois G, Duggan N, Hall E, Hatto J, Maas J, Manini J, Profit R, Riddy D, Ritchie C, Sohal B, Shaw D, Stringer R, Sykes DA, Thomas M, Turner KL, Watson SJ, West R, Willard E, Williams G, Willis J.
ACS Med Chem Lett (2017) 8 : 582 -586
PubMed 28523115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.40 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442750 QAV680 2.0 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442750 QAV680 IC50 = 40.0 nM 7.40