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Assay Detail

CHEMBL816693

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

Functional
In vitro thromboxane A2 receptor antagonism through inhibition of U-46619-induced platelet aggregation in human whole blood.
16
Total Activities
16
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 A2 receptor (CHEMBL2069)
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
Kd 16 7.99 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352040 1 9.00
CHEMBL159517 1 8.60
CHEMBL349625 1 8.60
CHEMBL162409 1 8.50
CHEMBL161532 1 8.50
CHEMBL162133 1 8.50
CHEMBL159787 1 8.50
CHEMBL345876 1 8.50
CHEMBL158576 1 8.40
CHEMBL158875 1 8.20
CHEMBL350292 1 8.20
CHEMBL159860 1 8.20
CHEMBL162691 1 8.00
CHEMBL433884 1 7.90
CHEMBL280728 RIDOGREL 2.0 1 5.40
CHEMBL26820 (E)-ISBOGREL 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352040 Kd = 1.0 nM 9.00
CHEMBL159517 Kd = 2.512 nM 8.60
CHEMBL349625 Kd = 2.512 nM 8.60
CHEMBL162409 Kd = 3.162 nM 8.50
CHEMBL161532 Kd = 3.162 nM 8.50
CHEMBL162133 Kd = 3.162 nM 8.50
CHEMBL159787 Kd = 3.162 nM 8.50
CHEMBL345876 Kd = 3.162 nM 8.50
CHEMBL158576 Kd = 3.981 nM 8.40
CHEMBL158875 Kd = 6.31 nM 8.20
CHEMBL350292 Kd = 6.31 nM 8.20
CHEMBL159860 Kd = 6.31 nM 8.20
CHEMBL162691 Kd = 10.0 nM 8.00
CHEMBL433884 Kd = 12.59 nM 7.90
CHEMBL280728 RIDOGREL Kd = 3981.07 nM 5.40
CHEMBL26820 (E)-ISBOGREL Kd = 15848.93 nM 4.80