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Assay Detail

CHEMBL816758

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

Functional
In vitro TXA2 synthase antagonism through inhibition of collagen induced thromboxane-A2 production in human citreated whole blood
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Blood
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and pharmacological evaluation of combined Thromboxane receptor antagonists/thromboxane synthase inhibitors: Pyridine-containing amino-prostanoids
Campbell I, Collington E, Finch H, Hayes R, Lumley P, Mills K, Robertson G, Wharton K, Watts I
Bioorg Med Chem Lett (1991) 1 : 695 -698
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.50 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280728 RIDOGREL 2.0 1 7.50
CHEMBL26820 (E)-ISBOGREL 1 7.00
CHEMBL159517 1 7.00
CHEMBL158576 1 7.00
CHEMBL349625 1 7.00
CHEMBL350292 1 6.40
CHEMBL433884 1 6.20
CHEMBL162691 1 6.20
CHEMBL159787 1 5.80
CHEMBL159860 1 5.80
CHEMBL352040 1 5.60
CHEMBL162409 1 -
CHEMBL158875 1 -
CHEMBL161532 1 -
CHEMBL345876 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280728 RIDOGREL IC50 = 31.62 nM 7.50
CHEMBL26820 (E)-ISBOGREL IC50 = 100.0 nM 7.00
CHEMBL159517 IC50 = 100.0 nM 7.00
CHEMBL158576 IC50 = 100.0 nM 7.00
CHEMBL349625 IC50 = 100.0 nM 7.00
CHEMBL350292 IC50 = 398.11 nM 6.40
CHEMBL433884 IC50 = 630.96 nM 6.20
CHEMBL162691 IC50 = 630.96 nM 6.20
CHEMBL159787 IC50 = 1584.89 nM 5.80
CHEMBL159860 IC50 = 1584.89 nM 5.80
CHEMBL352040 IC50 = 2511.89 nM 5.60
CHEMBL162409 IC50 < 10000.0 nM -
CHEMBL158875 IC50 < 10000.0 nM -
CHEMBL161532 IC50 < 10000.0 nM -
CHEMBL345876 IC50 < 10000.0 nM -