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Assay Detail

CHEMBL1054927

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

Binding
Displacement of [3H]SQ-29548 from thromboxane receptor in human platelet membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane A2 receptor (CHEMBL2069)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP.
Bioorg Med Chem Lett (2009) 19 : 4647 -4651
PubMed 19608418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.03 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361812 RAMATROBAN 4.0 1 7.85
CHEMBL551813 BI-671800 2.0 1 4.20
CHEMBL560993 TIMAPIPRANT 3.0 1 -
CHEMBL563664 1 -
CHEMBL561132 MK-7246 1.0 1 -
CHEMBL564920 1 -
CHEMBL564845 1 -
CHEMBL550465 1 -
CHEMBL550868 1 -
CHEMBL552211 1 -
CHEMBL556849 1 -
CHEMBL557117 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361812 RAMATROBAN IC50 = 14.0 nM 7.85
CHEMBL551813 BI-671800 IC50 = 62600.0 nM 4.20
CHEMBL560993 TIMAPIPRANT IC50 > 100000.0 nM -
CHEMBL563664 IC50 > 100000.0 nM -
CHEMBL561132 MK-7246 IC50 > 100000.0 nM -
CHEMBL564920 IC50 > 100000.0 nM -
CHEMBL564845 IC50 - -
CHEMBL550465 IC50 > 100000.0 nM -
CHEMBL550868 IC50 > 100000.0 nM -
CHEMBL552211 IC50 > 100000.0 nM -
CHEMBL556849 IC50 > 100000.0 nM -
CHEMBL557117 IC50 > 100000.0 nM -