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Assay Detail

CHEMBL809291

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Functional
In vitro for antagonistic activity against thromboxane synthase receptor
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounds.
Takeuchi K, Kohn TJ, True TA, Mais DE, Wikel JH, Utterback BG, Wyss VL, Jakubowski JA.
J Med Chem (1998) 41 : 5362 -5374
PubMed 9876106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 25 6.69 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147444 1 7.56
CHEMBL346644 1 7.36
CHEMBL150252 1 7.28
CHEMBL150206 1 7.24
CHEMBL151519 2 7.20
CHEMBL150436 1 7.19
CHEMBL151083 1 7.13
CHEMBL150563 1 7.08
CHEMBL150660 1 7.06
CHEMBL150289 1 6.95
CHEMBL151091 1 6.92
CHEMBL357723 1 6.92
CHEMBL57576 1 6.87
CHEMBL291539 1 6.82
CHEMBL151860 1 6.81
CHEMBL434449 1 6.78
CHEMBL347343 1 6.76
CHEMBL147308 1 6.32
CHEMBL60710 1 6.10
CHEMBL358012 1 5.85
CHEMBL150598 1 5.17
CHEMBL280728 RIDOGREL 2.0 1 5.10
CHEMBL26820 (E)-ISBOGREL 1 5.09
CHEMBL424139 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147444 Kd = 27.3 nM 7.56
CHEMBL346644 Kd = 43.3 nM 7.36
CHEMBL150252 Kd = 52.2 nM 7.28
CHEMBL150206 Kd = 58.2 nM 7.24
CHEMBL151519 Kd = 62.6 nM 7.20
CHEMBL150436 Kd = 64.3 nM 7.19
CHEMBL151083 Kd = 74.3 nM 7.13
CHEMBL150563 Kd = 82.4 nM 7.08
CHEMBL150660 Kd = 86.7 nM 7.06
CHEMBL151519 Kd = 104.7 nM 6.98
CHEMBL150289 Kd = 113.3 nM 6.95
CHEMBL357723 Kd = 121.7 nM 6.92
CHEMBL151091 Kd = 119.3 nM 6.92
CHEMBL57576 Kd = 135.2 nM 6.87
CHEMBL291539 Kd = 153.1 nM 6.82
CHEMBL151860 Kd = 155.8 nM 6.81
CHEMBL434449 Kd = 165.4 nM 6.78
CHEMBL347343 Kd = 173.3 nM 6.76
CHEMBL147308 Kd = 483.0 nM 6.32
CHEMBL60710 Kd = 791.2 nM 6.10
CHEMBL358012 Kd = 1404.9 nM 5.85
CHEMBL150598 Kd = 6724.2 nM 5.17
CHEMBL280728 RIDOGREL Kd = 8000.0 nM 5.10
CHEMBL26820 (E)-ISBOGREL Kd = 8200.0 nM 5.09
CHEMBL424139 Kd > 10000.0 nM -