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Assay Detail

CHEMBL4000099

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

Binding
Displacement of [3H]PGD2 from human DP2 receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay
16
Total Activities
16
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
Ki 16 7.39 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3981414 1 8.40
CHEMBL3137332 FEVIPIPRANT 3.0 1 8.40
CHEMBL3931906 1 8.22
CHEMBL3932668 1 8.15
CHEMBL4094939 1 7.72
CHEMBL3912535 1 7.54
CHEMBL3983909 1 7.51
CHEMBL3975922 1 7.51
CHEMBL2442750 QAV680 2.0 1 7.44
CHEMBL4086277 1 7.33
CHEMBL4073398 1 7.30
CHEMBL4064804 1 7.14
CHEMBL3922383 1 7.07
CHEMBL4067518 1 6.45
CHEMBL4102679 1 6.13
CHEMBL4078419 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3981414 Ki = 4.0 nM 8.40
CHEMBL3137332 FEVIPIPRANT Ki = 4.0 nM 8.40
CHEMBL3931906 Ki = 6.0 nM 8.22
CHEMBL3932668 Ki = 7.0 nM 8.15
CHEMBL4094939 Ki = 19.0 nM 7.72
CHEMBL3912535 Ki = 29.0 nM 7.54
CHEMBL3983909 Ki = 31.0 nM 7.51
CHEMBL3975922 Ki = 31.0 nM 7.51
CHEMBL2442750 QAV680 Ki = 36.0 nM 7.44
CHEMBL4086277 Ki = 47.0 nM 7.33
CHEMBL4073398 Ki = 50.0 nM 7.30
CHEMBL4064804 Ki = 72.0 nM 7.14
CHEMBL3922383 Ki = 86.0 nM 7.07
CHEMBL4067518 Ki = 356.0 nM 6.45
CHEMBL4102679 Ki = 735.0 nM 6.13
CHEMBL4078419 Ki = 1335.0 nM 5.88