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Assay Detail

CHEMBL808526

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

Binding
In vitro inhibition of thromboxane synthase
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane-A synthase (CHEMBL1835)
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 8.03 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65414 1 8.70
CHEMBL48092 PIRMAGREL 2.0 1 8.52
CHEMBL292331 3 8.00
CHEMBL62834 1 7.96
CHEMBL65161 1 7.37
CHEMBL2115559 1 -
CHEMBL292740 1 -
CHEMBL63056 1 -
CHEMBL62852 1 -
CHEMBL2115518 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65414 IC50 = 2.0 nM 8.70
CHEMBL48092 PIRMAGREL IC50 = 3.0 nM 8.52
CHEMBL292331 IC50 = 10.0 nM 8.00
CHEMBL62834 IC50 = 11.0 nM 7.96
CHEMBL292331 IC50 = 13.0 nM 7.89
CHEMBL292331 IC50 = 18.0 nM 7.75
CHEMBL65161 IC50 = 43.0 nM 7.37
CHEMBL2115559 IC50 > 200.0 nM -
CHEMBL292740 IC50 > 200.0 nM -
CHEMBL63056 IC50 > 200.0 nM -
CHEMBL62852 IC50 > 100.0 nM -
CHEMBL2115518 IC50 > 200.0 nM -