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Assay Detail

CHEMBL814728

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Binding
In vitro thromboxane-A2 receptor binding affinity to displace by 50% [3H]-SQ 29548 binding from washed human platelets
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane A2 receptor (CHEMBL2069) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 5.95 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120041 — — 1 7.70
CHEMBL333237 — — 1 7.52
CHEMBL339877 — — 1 7.40
CHEMBL118188 — — 1 7.40
CHEMBL275256 — — 1 7.30
CHEMBL120250 — — 1 7.16
CHEMBL331218 — — 1 7.16
CHEMBL120181 — — 1 7.10
CHEMBL120165 — — 1 6.92
CHEMBL120207 — — 1 6.85
CHEMBL71685 DALTROBAN 2.0 1 6.82
CHEMBL120284 — — 1 6.80
CHEMBL118184 — — 1 6.77
CHEMBL120496 — — 1 6.77
CHEMBL338741 — — 1 6.72
CHEMBL120249 — — 1 6.64
CHEMBL123307 — — 1 6.64
CHEMBL120259 — — 1 6.55
CHEMBL333236 — — 1 6.52
CHEMBL122008 — — 1 6.28
CHEMBL122472 — — 1 6.28
CHEMBL120943 — — 1 6.06
CHEMBL118124 — — 1 6.01
CHEMBL444856 — — 1 6.01
CHEMBL326521 — — 1 5.98
CHEMBL122123 — — 1 5.94
CHEMBL121043 — — 1 5.89
CHEMBL118568 — — 1 5.72
CHEMBL280728 RIDOGREL 2.0 1 5.68
CHEMBL121304 — — 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120041 — IC50 = 20.0 nM 7.70
CHEMBL333237 — IC50 = 30.0 nM 7.52
CHEMBL118188 — IC50 = 40.0 nM 7.40
CHEMBL339877 — IC50 = 40.0 nM 7.40
CHEMBL275256 — IC50 = 50.0 nM 7.30
CHEMBL120250 — IC50 = 70.0 nM 7.16
CHEMBL331218 — IC50 = 70.0 nM 7.16
CHEMBL120181 — IC50 = 80.0 nM 7.10
CHEMBL120165 — IC50 = 120.0 nM 6.92
CHEMBL120207 — IC50 = 140.0 nM 6.85
CHEMBL71685 DALTROBAN IC50 = 150.0 nM 6.82
CHEMBL120284 — IC50 = 160.0 nM 6.80
CHEMBL118184 — IC50 = 170.0 nM 6.77
CHEMBL120496 — IC50 = 170.0 nM 6.77
CHEMBL338741 — IC50 = 190.0 nM 6.72
CHEMBL120249 — IC50 = 230.0 nM 6.64
CHEMBL123307 — IC50 = 230.0 nM 6.64
CHEMBL120259 — IC50 = 280.0 nM 6.55
CHEMBL333236 — IC50 = 300.0 nM 6.52
CHEMBL122008 — IC50 = 530.0 nM 6.28
CHEMBL122472 — IC50 = 520.0 nM 6.28
CHEMBL120943 — IC50 = 880.0 nM 6.06
CHEMBL118124 — IC50 = 970.0 nM 6.01
CHEMBL444856 — IC50 = 970.0 nM 6.01
CHEMBL326521 — IC50 = 1040.0 nM 5.98
CHEMBL122123 — IC50 = 1160.0 nM 5.94
CHEMBL121043 — IC50 = 1300.0 nM 5.89
CHEMBL118568 — IC50 = 1900.0 nM 5.72
CHEMBL280728 RIDOGREL IC50 = 2100.0 nM 5.68
CHEMBL121304 — IC50 = 2390.0 nM 5.62
CHEMBL120019 — IC50 = 3000.0 nM 5.52
CHEMBL120228 — IC50 = 3280.0 nM 5.48
CHEMBL120811 — IC50 = 4160.0 nM 5.38
CHEMBL119661 — IC50 = 7500.0 nM 5.12
CHEMBL120904 — IC50 = 12200.0 nM 4.91
CHEMBL121507 — IC50 = 14700.0 nM 4.83
CHEMBL121306 — IC50 = 19700.0 nM 4.71
CHEMBL121289 — IC50 = 21000.0 nM 4.68
CHEMBL330837 — IC50 = 23400.0 nM 4.63
CHEMBL121314 — IC50 = 23900.0 nM 4.62
CHEMBL121307 — IC50 = 27300.0 nM 4.56
CHEMBL120947 — IC50 = 46200.0 nM 4.33
CHEMBL118619 — IC50 = 49300.0 nM 4.31
CHEMBL439790 — IC50 = 53100.0 nM 4.28
CHEMBL333868 — IC50 = 73000.0 nM 4.14
CHEMBL120370 — IC50 = 74500.0 nM 4.13
CHEMBL121300 — IC50 > 100000.0 nM -
CHEMBL121261 — IC50 > 100000.0 nM -
CHEMBL120372 — IC50 > 100000.0 nM -
CHEMBL11662 OZAGREL IC50 > 100000.0 nM -