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Assay Detail

CHEMBL880221

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Binding
In vitro inhibition of thromboxane-A2 synthase in rat whole blood during clotting at 37 degrees Centigrade
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Agents combining thromboxane receptor antagonism with thromboxane synthase inhibition: [[[2-(1H-imidazol-1-yl)ethylidene]amino]oxy]alkanoic acids.
Cozzi P, Giordani A, Menichincheri M, Pillan A, Pinciroli V, Rossi A, Tonani R, Volpi D, Tamburin M, Ferrario R.
J Med Chem (1994) 37 : 3588 -3604
PubMed 7932586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122123 — — 1 7.70
CHEMBL280728 RIDOGREL 2.0 1 7.52
CHEMBL120904 — — 1 7.40
CHEMBL439790 — — 1 7.40
CHEMBL120019 — — 1 7.30
CHEMBL118184 — — 1 7.30
CHEMBL122008 — — 1 7.22
CHEMBL120181 — — 1 7.22
CHEMBL338741 — — 1 7.16
CHEMBL444856 — — 1 7.00
CHEMBL120259 — — 1 7.00
CHEMBL120250 — — 1 6.85
CHEMBL122181 — — 1 6.80
CHEMBL121507 — — 1 6.77
CHEMBL330837 — — 1 6.70
CHEMBL120207 — — 1 6.60
CHEMBL120496 — — 1 6.60
CHEMBL333237 — — 1 6.57
CHEMBL120947 — — 1 6.57
CHEMBL120228 — — 1 6.52
CHEMBL331218 — — 1 6.50
CHEMBL333236 — — 1 6.46
CHEMBL121306 — — 1 6.44
CHEMBL120041 — — 1 6.43
CHEMBL118188 — — 1 6.41
CHEMBL121043 — — 1 6.37
CHEMBL123307 — — 1 6.28
CHEMBL121307 — — 1 6.19
CHEMBL11662 OZAGREL 4.0 1 6.19
CHEMBL122472 — — 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122123 — IC50 = 20.0 nM 7.70
CHEMBL280728 RIDOGREL IC50 = 30.0 nM 7.52
CHEMBL439790 — IC50 = 40.0 nM 7.40
CHEMBL120904 — IC50 = 40.0 nM 7.40
CHEMBL120019 — IC50 = 50.0 nM 7.30
CHEMBL118184 — IC50 = 50.0 nM 7.30
CHEMBL122008 — IC50 = 60.0 nM 7.22
CHEMBL120181 — IC50 = 60.0 nM 7.22
CHEMBL338741 — IC50 = 70.0 nM 7.16
CHEMBL444856 — IC50 = 100.0 nM 7.00
CHEMBL120259 — IC50 = 100.0 nM 7.00
CHEMBL120250 — IC50 = 140.0 nM 6.85
CHEMBL122181 — IC50 = 160.0 nM 6.80
CHEMBL121507 — IC50 = 170.0 nM 6.77
CHEMBL330837 — IC50 = 200.0 nM 6.70
CHEMBL120207 — IC50 = 250.0 nM 6.60
CHEMBL120496 — IC50 = 250.0 nM 6.60
CHEMBL333237 — IC50 = 270.0 nM 6.57
CHEMBL120947 — IC50 = 270.0 nM 6.57
CHEMBL120228 — IC50 = 300.0 nM 6.52
CHEMBL331218 — IC50 = 320.0 nM 6.50
CHEMBL333236 — IC50 = 350.0 nM 6.46
CHEMBL121306 — IC50 = 360.0 nM 6.44
CHEMBL120041 — IC50 = 370.0 nM 6.43
CHEMBL118188 — IC50 = 390.0 nM 6.41
CHEMBL121043 — IC50 = 430.0 nM 6.37
CHEMBL123307 — IC50 = 530.0 nM 6.28
CHEMBL121307 — IC50 = 640.0 nM 6.19
CHEMBL11662 OZAGREL IC50 = 640.0 nM 6.19
CHEMBL122472 — IC50 = 710.0 nM 6.15
CHEMBL120811 — IC50 = 760.0 nM 6.12
CHEMBL339877 — IC50 = 890.0 nM 6.05
CHEMBL275256 — IC50 = 900.0 nM 6.05
CHEMBL120284 — IC50 = 1100.0 nM 5.96
CHEMBL120943 — IC50 > 1000.0 nM -
CHEMBL120370 — IC50 > 1000.0 nM -
CHEMBL71685 DALTROBAN IC50 > 100000.0 nM -
CHEMBL118619 — IC50 > 1000.0 nM -
CHEMBL118568 — IC50 > 1000.0 nM -
CHEMBL120165 — IC50 > 1000.0 nM -
CHEMBL121300 — IC50 > 1000.0 nM -
CHEMBL333868 — IC50 > 1000.0 nM -
CHEMBL120249 — IC50 > 1000.0 nM -
CHEMBL121314 — IC50 > 1000.0 nM -
CHEMBL121289 — IC50 > 1000.0 nM -
CHEMBL121261 — IC50 > 1000.0 nM -
CHEMBL118124 — IC50 > 1000.0 nM -
CHEMBL121304 — IC50 > 1000.0 nM -
CHEMBL326521 — IC50 > 1000.0 nM -
CHEMBL120372 — IC50 > 1000.0 nM -