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Assay Detail

CHEMBL814434

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

Binding
Tested for inhibition of thromboxane synthetase from spontaneously hypertensive rats
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane-A synthase (CHEMBL4028)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
Wright WB, Tomcufcik AS, Chan PS, Marsico JW, Press JB.
J Med Chem (1987) 30 : 2277 -2283
PubMed 3681898 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.06 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309960 1 8.70
CHEMBL75787 1 8.70
CHEMBL76234 1 8.52
CHEMBL420931 1 8.52
CHEMBL72450 1 8.40
CHEMBL72684 1 8.15
CHEMBL541827 1 8.15
CHEMBL74733 1 8.10
CHEMBL76341 1 8.05
CHEMBL74627 1 8.00
CHEMBL554990 1 8.00
CHEMBL307631 1 8.00
CHEMBL73143 1 7.92
CHEMBL307725 1 7.70
CHEMBL75451 1 7.52
CHEMBL73065 1 7.52
CHEMBL73620 1 7.52
CHEMBL73236 1 7.40
CHEMBL73426 1 7.40
CHEMBL73158 1 7.40
CHEMBL72382 1 7.30
CHEMBL1743616 1 7.30
CHEMBL75609 1 7.30
CHEMBL1743613 1 7.22
CHEMBL73769 1 7.16
CHEMBL73748 1 7.05
CHEMBL311689 1 7.05
CHEMBL310904 1 7.00
CHEMBL75449 1 6.82
CHEMBL267473 DAZOXIBEN 2.0 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309960 IC50 = 2.0 nM 8.70
CHEMBL75787 IC50 = 2.0 nM 8.70
CHEMBL420931 IC50 = 3.0 nM 8.52
CHEMBL76234 IC50 = 3.0 nM 8.52
CHEMBL72450 IC50 = 4.0 nM 8.40
CHEMBL72684 IC50 = 7.0 nM 8.15
CHEMBL541827 IC50 = 7.0 nM 8.15
CHEMBL74733 IC50 = 8.0 nM 8.10
CHEMBL76341 IC50 = 9.0 nM 8.05
CHEMBL74627 IC50 = 10.0 nM 8.00
CHEMBL554990 IC50 = 10.0 nM 8.00
CHEMBL307631 IC50 = 10.0 nM 8.00
CHEMBL73143 IC50 = 12.0 nM 7.92
CHEMBL307725 IC50 = 20.0 nM 7.70
CHEMBL73620 IC50 = 30.0 nM 7.52
CHEMBL73065 IC50 = 30.0 nM 7.52
CHEMBL75451 IC50 = 30.0 nM 7.52
CHEMBL73236 IC50 = 40.0 nM 7.40
CHEMBL73426 IC50 = 40.0 nM 7.40
CHEMBL73158 IC50 = 40.0 nM 7.40
CHEMBL72382 IC50 = 50.0 nM 7.30
CHEMBL1743616 IC50 = 50.0 nM 7.30
CHEMBL75609 IC50 = 50.0 nM 7.30
CHEMBL1743613 IC50 = 60.0 nM 7.22
CHEMBL73769 IC50 = 70.0 nM 7.16
CHEMBL73748 IC50 = 90.0 nM 7.05
CHEMBL311689 IC50 = 90.0 nM 7.05
CHEMBL310904 IC50 = 100.0 nM 7.00
CHEMBL75449 IC50 = 150.0 nM 6.82
CHEMBL267473 DAZOXIBEN IC50 = 150.0 nM 6.82
CHEMBL74973 IC50 = 170.0 nM 6.77
CHEMBL310955 IC50 = 180.0 nM 6.75
CHEMBL307382 IC50 = 200.0 nM 6.70
CHEMBL73407 IC50 = 240.0 nM 6.62
CHEMBL75249 IC50 = 290.0 nM 6.54
CHEMBL74915 IC50 = 340.0 nM 6.47
CHEMBL75252 IC50 = 350.0 nM 6.46
CHEMBL312536 IC50 = 350.0 nM 6.46
CHEMBL74207 IC50 = 400.0 nM 6.40
CHEMBL74821 IC50 = 500.0 nM 6.30
CHEMBL72070 IC50 = 500.0 nM 6.30
CHEMBL75334 IC50 = 600.0 nM 6.22
CHEMBL73779 IC50 = 700.0 nM 6.16
CHEMBL72690 IC50 = 800.0 nM 6.10
CHEMBL74516 IC50 = 820.0 nM 6.09
CHEMBL1743611 IC50 = 900.0 nM 6.05
CHEMBL75344 IC50 = 1000.0 nM 6.00
CHEMBL74693 IC50 = 1300.0 nM 5.89
CHEMBL72273 IC50 = 1500.0 nM 5.82
CHEMBL73850 IC50 = 1700.0 nM 5.77