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Assay Detail

CHEMBL4000116

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

Binding
Displacement of [3H]NVP-QAW039 from human DP2 receptor expressed in CHO cell membranes by TopCount scintillation assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin D2 receptor 2 (CHEMBL5071)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Kd 4 8.28 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3137332 FEVIPIPRANT 3.0 1 8.99
CHEMBL3931906 1 8.72
CHEMBL2442750 QAV680 2.0 1 7.82
CHEMBL4094939 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3137332 FEVIPIPRANT Kd = 1.023 nM 8.99
CHEMBL3931906 Kd = 1.905 nM 8.72
CHEMBL2442750 QAV680 Kd = 15.14 nM 7.82
CHEMBL4094939 Kd = 25.12 nM 7.60