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Assay Detail

CHEMBL815546

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

Functional
In vitro Thromboxane A2 (TXA2) receptor antagonism was tested by its ability to inhibit the contraction of rat aorta induced by the stable thromboxane agonist U-46,619
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Aorta
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Thromboxane modulating agents. 4. Design and synthesis of 3-(2-[[(4-chlorophenyl)sulfonyl]-amino]ethyl)benzenepropanoic acid derivatives as potent thromboxane receptor antagonists.
Dack KN, Dickinson RP, Long CJ, Steele J.
Bioorg Med Chem Lett (1998) 8 : 2061 -2066
PubMed 9873486 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 15 10.02 10.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65478 1 10.80
CHEMBL66194 1 10.60
CHEMBL62666 1 10.60
CHEMBL65780 1 10.40
CHEMBL65571 1 10.20
CHEMBL65167 1 10.20
CHEMBL303097 1 10.10
CHEMBL65175 1 10.00
CHEMBL65779 1 9.70
CHEMBL64971 1 9.50
CHEMBL63090 1 9.40
CHEMBL65121 1 8.70
CHEMBL66136 1 -
CHEMBL417742 1 -
CHEMBL65378 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65478 Kd = 0.01585 nM 10.80
CHEMBL66194 Kd = 0.02512 nM 10.60
CHEMBL62666 Kd = 0.02512 nM 10.60
CHEMBL65780 Kd = 0.03981 nM 10.40
CHEMBL65571 Kd = 0.0631 nM 10.20
CHEMBL65167 Kd = 0.0631 nM 10.20
CHEMBL303097 Kd = 0.07943 nM 10.10
CHEMBL65175 Kd = 0.1 nM 10.00
CHEMBL65779 Kd = 0.1995 nM 9.70
CHEMBL64971 Kd = 0.3162 nM 9.50
CHEMBL63090 Kd = 0.3981 nM 9.40
CHEMBL65121 Kd = 1.995 nM 8.70
CHEMBL66136 Kd = 0.003981 nM -
CHEMBL417742 Kd = 0.003981 nM -
CHEMBL65378 Kd = 0.002512 nM -