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Assay Detail

CHEMBL813726

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

Functional
Inhibition of thromboxane A2 synthetase as reduced ADP-induced aggregation of human platelet rich plasma in the presence of pig aortal microsomes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Aorta
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thromboxane-A synthase (CHEMBL1835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
Martinez GR, Walker KA, Hirschfeld DR, Maloney PJ, Yang DS, Rosenkranz RP.
J Med Chem (1989) 32 : 890 -897
PubMed 2704033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.76 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL353950 1 7.38
CHEMBL170754 1 7.36
CHEMBL352763 1 7.30
CHEMBL170776 1 6.00
CHEMBL11662 OZAGREL 4.0 1 5.85
CHEMBL169331 1 5.80
CHEMBL352512 1 5.68
CHEMBL167601 1 5.42
CHEMBL352874 1 5.34
CHEMBL170615 1 5.04
CHEMBL169905 1 5.04
CHEMBL354424 1 4.62
CHEMBL262055 1 4.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL353950 IC50 = 42.0 nM 7.38
CHEMBL170754 IC50 = 44.0 nM 7.36
CHEMBL352763 IC50 = 50.0 nM 7.30
CHEMBL170776 IC50 = 1000.0 nM 6.00
CHEMBL11662 OZAGREL IC50 = 1400.0 nM 5.85
CHEMBL169331 IC50 = 1600.0 nM 5.80
CHEMBL352512 IC50 = 2100.0 nM 5.68
CHEMBL167601 IC50 = 3800.0 nM 5.42
CHEMBL352874 IC50 = 4600.0 nM 5.34
CHEMBL170615 IC50 = 9100.0 nM 5.04
CHEMBL169905 IC50 = 9100.0 nM 5.04
CHEMBL354424 IC50 = 24000.0 nM 4.62
CHEMBL262055 IC50 = 78000.0 nM 4.11