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Assay Detail

CHEMBL844149

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

Functional
In vitro thromboxane receptor antagonist activity was determined by inhibition of U-46619 induced aggregation of washed human platelets
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Thia-prostanoid analogs with combined thromboxane receptor antagonist/thromboxane synthase inhibitor activities. Synthesis and pharmacological evaluation
Vlattas I, Dellureficio J, Cohen D, Lee W, Clarke F, Dotson R, Mathis J, Zoganas H
Bioorg Med Chem Lett (1994) 4 : 2067 -2072
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.28 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65030 VAPIPROST 2.0 1 7.92
CHEMBL63056 1 7.75
CHEMBL65414 1 7.75
CHEMBL292331 2 7.66
CHEMBL292740 1 7.62
CHEMBL62834 1 7.34
CHEMBL62852 1 7.24
CHEMBL2115559 1 7.11
CHEMBL2115518 1 6.98
CHEMBL65161 1 6.64
CHEMBL48092 PIRMAGREL 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65030 VAPIPROST IC50 = 12.0 nM 7.92
CHEMBL63056 IC50 = 18.0 nM 7.75
CHEMBL65414 IC50 = 18.0 nM 7.75
CHEMBL292331 IC50 = 22.0 nM 7.66
CHEMBL292740 IC50 = 24.0 nM 7.62
CHEMBL62834 IC50 = 46.0 nM 7.34
CHEMBL62852 IC50 = 57.0 nM 7.24
CHEMBL2115559 IC50 = 77.0 nM 7.11
CHEMBL2115518 IC50 = 105.0 nM 6.98
CHEMBL65161 IC50 = 228.0 nM 6.64
CHEMBL292331 IC50 = 806.0 nM 6.09
CHEMBL48092 PIRMAGREL IC50 - nM -