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Assay Detail

CHEMBL971477

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

Functional
Antagonist activity at DP1 in washed human platelet assessed as inhibition of PGD2-induced [125I]cAMP production preincubated 10 mins before PGD2 challenge by scintillation proximity assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostaglandin D2 receptor (CHEMBL4427)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective DP1 receptor antagonists in the azaindole series.
Leblanc Y, Roy P, Dufresne C, Lachance N, Wang Z, O'Neill G, Greig G, Denis D, Mathieu MC, Slipetz D, Sawyer N, Tsou N.
Bioorg Med Chem Lett (2009) 19 : 2125 -2128
PubMed 19307115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.76 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483991 1 9.85
CHEMBL484778 1 9.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483991 IC50 = 0.14 nM 9.85
CHEMBL484778 IC50 = 0.22 nM 9.66