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Assay Detail

CHEMBL880940

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Binding
Activity against human platelet microsome Thromboxane synthase
29
Total Activities
29
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 (CHEMBL1835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thromboxane modulating agents. 3. 1H-imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists.
Dickinson RP, Dack KN, Long CJ, Steele J.
J Med Chem (1997) 40 : 3442 -3452
PubMed 9341919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.44 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117752 1 7.75
CHEMBL115387 1 7.70
CHEMBL326356 1 7.66
CHEMBL119670 1 7.66
CHEMBL115636 1 7.66
CHEMBL114063 1 7.57
CHEMBL283656 DAZMEGREL 2.0 1 7.55
CHEMBL113753 1 7.54
CHEMBL115806 1 7.54
CHEMBL295512 1 7.47
CHEMBL116704 1 7.43
CHEMBL117538 1 7.43
CHEMBL118084 1 7.42
CHEMBL114456 1 7.42
CHEMBL418852 1 7.42
CHEMBL117373 1 7.42
CHEMBL324059 1 7.41
CHEMBL432958 1 7.41
CHEMBL63090 1 7.41
CHEMBL117224 1 7.37
CHEMBL119035 1 7.37
CHEMBL116196 1 7.35
CHEMBL47612 1 7.32
CHEMBL115805 1 7.32
CHEMBL118008 1 7.31
CHEMBL117561 1 7.28
CHEMBL117294 1 7.27
CHEMBL116970 1 7.21
CHEMBL320235 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117752 IC50 = 18.0 nM 7.75
CHEMBL115387 IC50 = 20.0 nM 7.70
CHEMBL326356 IC50 = 22.0 nM 7.66
CHEMBL119670 IC50 = 22.0 nM 7.66
CHEMBL115636 IC50 = 22.0 nM 7.66
CHEMBL114063 IC50 = 27.0 nM 7.57
CHEMBL283656 DAZMEGREL IC50 = 28.0 nM 7.55
CHEMBL113753 IC50 = 29.0 nM 7.54
CHEMBL115806 IC50 = 29.0 nM 7.54
CHEMBL295512 IC50 = 34.0 nM 7.47
CHEMBL116704 IC50 = 37.0 nM 7.43
CHEMBL117538 IC50 = 37.0 nM 7.43
CHEMBL118084 IC50 = 38.0 nM 7.42
CHEMBL114456 IC50 = 38.0 nM 7.42
CHEMBL418852 IC50 = 38.0 nM 7.42
CHEMBL117373 IC50 = 38.0 nM 7.42
CHEMBL324059 IC50 = 39.0 nM 7.41
CHEMBL432958 IC50 = 39.0 nM 7.41
CHEMBL63090 IC50 = 39.0 nM 7.41
CHEMBL117224 IC50 = 43.0 nM 7.37
CHEMBL119035 IC50 = 43.0 nM 7.37
CHEMBL116196 IC50 = 45.0 nM 7.35
CHEMBL47612 IC50 = 48.0 nM 7.32
CHEMBL115805 IC50 = 48.0 nM 7.32
CHEMBL118008 IC50 = 49.0 nM 7.31
CHEMBL117561 IC50 = 53.0 nM 7.28
CHEMBL117294 IC50 = 54.0 nM 7.27
CHEMBL116970 IC50 = 61.0 nM 7.21
CHEMBL320235 IC50 = 61.0 nM 7.21