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Assay Detail

CHEMBL814436

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

Functional
Tested for antagonistic activity on isolated rat thoracic aorta (thromboxane A2 receptor) precontracted by U-46619 (3 x 10 e-8 M)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Role of sulfonamide moiety in non-prostanoid txa2 receptor antagonist kt2-962 : modifications of this moiety and the resulting activities
Yokota M, Imamaki K, Uchibori S, Kondo M, Kosakai K, Tomiyama T
Bioorg Med Chem Lett (1993) 3 : 1687 -1692
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.63 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262655 1 9.05
CHEMBL298462 1 6.66
CHEMBL46338 1 6.07
CHEMBL430569 1 6.07
CHEMBL47605 1 5.85
CHEMBL297275 1 5.82
CHEMBL8273 SULOTROBAN 2.0 1 5.82
CHEMBL48013 1 5.82
CHEMBL47743 1 5.77
CHEMBL297808 1 5.58
CHEMBL47510 1 5.06
CHEMBL43726 1 5.06
CHEMBL47658 1 5.04
CHEMBL48117 1 4.92
CHEMBL45471 1 4.72
CHEMBL297989 1 4.27
CHEMBL45623 1 4.19
CHEMBL47635 1 -
CHEMBL296652 1 -
CHEMBL43880 1 -
CHEMBL45360 1 -
CHEMBL44769 1 -
CHEMBL413055 1 -
CHEMBL297315 1 -
CHEMBL296727 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262655 IC50 = 0.9 nM 9.05
CHEMBL298462 IC50 = 220.0 nM 6.66
CHEMBL46338 IC50 = 860.0 nM 6.07
CHEMBL430569 IC50 = 860.0 nM 6.07
CHEMBL47605 IC50 = 1400.0 nM 5.85
CHEMBL297275 IC50 = 1500.0 nM 5.82
CHEMBL8273 SULOTROBAN IC50 = 1500.0 nM 5.82
CHEMBL48013 IC50 = 1500.0 nM 5.82
CHEMBL47743 IC50 = 1700.0 nM 5.77
CHEMBL297808 IC50 = 2600.0 nM 5.58
CHEMBL47510 IC50 = 8700.0 nM 5.06
CHEMBL43726 IC50 = 8700.0 nM 5.06
CHEMBL47658 IC50 = 9100.0 nM 5.04
CHEMBL48117 IC50 = 12000.0 nM 4.92
CHEMBL45471 IC50 = 19000.0 nM 4.72
CHEMBL297989 IC50 = 54000.0 nM 4.27
CHEMBL45623 IC50 = 65000.0 nM 4.19
CHEMBL47635 IC50 = 590000.0 nM -
CHEMBL296652 IC50 > 100000.0 nM -
CHEMBL43880 IC50 > 100000.0 nM -
CHEMBL45360 IC50 > 100000.0 nM -
CHEMBL44769 IC50 > 100000.0 nM -
CHEMBL413055 IC50 > 100000.0 nM -
CHEMBL297315 IC50 > 100000.0 nM -
CHEMBL296727 IC50 > 100000.0 nM -