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Assay Detail

CHEMBL815547

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 contraction of rat isolated thoracic aortic strip
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane A2 receptor (CHEMBL3156)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 7.56 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162409 1 8.50
CHEMBL161532 1 8.50
CHEMBL345876 1 8.50
CHEMBL352040 1 8.00
CHEMBL158576 1 8.00
CHEMBL159787 1 7.90
CHEMBL350292 1 7.80
CHEMBL162133 1 7.80
CHEMBL159860 1 7.70
CHEMBL158875 1 7.60
CHEMBL159517 1 7.50
CHEMBL349625 1 7.50
CHEMBL433884 1 7.40
CHEMBL162691 1 7.10
CHEMBL280728 RIDOGREL 2.0 1 5.90
CHEMBL26820 (E)-ISBOGREL 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162409 Kd = 3.162 nM 8.50
CHEMBL161532 Kd = 3.162 nM 8.50
CHEMBL345876 Kd = 3.162 nM 8.50
CHEMBL352040 Kd = 10.0 nM 8.00
CHEMBL158576 Kd = 10.0 nM 8.00
CHEMBL159787 Kd = 12.59 nM 7.90
CHEMBL350292 Kd = 15.85 nM 7.80
CHEMBL162133 Kd = 15.85 nM 7.80
CHEMBL159860 Kd = 19.95 nM 7.70
CHEMBL158875 Kd = 25.12 nM 7.60
CHEMBL159517 Kd = 31.62 nM 7.50
CHEMBL349625 Kd = 31.62 nM 7.50
CHEMBL433884 Kd = 39.81 nM 7.40
CHEMBL162691 Kd = 79.43 nM 7.10
CHEMBL280728 RIDOGREL Kd = 1258.93 nM 5.90
CHEMBL26820 (E)-ISBOGREL Kd = 6309.57 nM 5.20