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Assay Detail

CHEMBL808531

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

Binding
In vitro inhibitory activity against human microsomal 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

A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
Ackerley N, Brewster AG, Brown GR, Clarke DS, Foubister AJ, Griffin SJ, Hudson JA, Smithers MJ, Whittamore PR.
J Med Chem (1995) 38 : 1608 -1628
PubMed 7752186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.34 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297385 1 8.00
CHEMBL291167 1 8.00
CHEMBL42677 1 8.00
CHEMBL40425 1 7.70
CHEMBL26820 (E)-ISBOGREL 1 7.70
CHEMBL290483 1 7.52
CHEMBL290882 1 7.52
CHEMBL263516 1 7.52
CHEMBL41945 1 7.52
CHEMBL44422 1 7.52
CHEMBL290281 1 7.52
CHEMBL417163 1 7.40
CHEMBL41904 1 7.40
CHEMBL288194 1 7.40
CHEMBL42738 1 7.40
CHEMBL43468 1 7.40
CHEMBL44865 1 7.40
CHEMBL290205 1 7.30
CHEMBL43488 1 7.30
CHEMBL287720 1 7.30
CHEMBL43756 1 7.22
CHEMBL44094 1 7.22
CHEMBL41989 1 7.16
CHEMBL267473 DAZOXIBEN 2.0 1 7.16
CHEMBL288118 1 5.77
CHEMBL294952 1 5.42
CHEMBL42263 1 -
CHEMBL24984 1 -
CHEMBL30024 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297385 IC50 = 10.0 nM 8.00
CHEMBL291167 IC50 = 10.0 nM 8.00
CHEMBL42677 IC50 = 10.0 nM 8.00
CHEMBL40425 IC50 = 20.0 nM 7.70
CHEMBL26820 (E)-ISBOGREL IC50 = 20.0 nM 7.70
CHEMBL290483 IC50 = 30.0 nM 7.52
CHEMBL290882 IC50 = 30.0 nM 7.52
CHEMBL263516 IC50 = 30.0 nM 7.52
CHEMBL41945 IC50 = 30.0 nM 7.52
CHEMBL44422 IC50 = 30.0 nM 7.52
CHEMBL290281 IC50 = 30.0 nM 7.52
CHEMBL417163 IC50 = 40.0 nM 7.40
CHEMBL41904 IC50 = 40.0 nM 7.40
CHEMBL288194 IC50 = 40.0 nM 7.40
CHEMBL42738 IC50 = 40.0 nM 7.40
CHEMBL43468 IC50 = 40.0 nM 7.40
CHEMBL44865 IC50 = 40.0 nM 7.40
CHEMBL290205 IC50 = 50.0 nM 7.30
CHEMBL43488 IC50 = 50.0 nM 7.30
CHEMBL287720 IC50 = 50.0 nM 7.30
CHEMBL43756 IC50 = 60.0 nM 7.22
CHEMBL44094 IC50 = 60.0 nM 7.22
CHEMBL41989 IC50 = 70.0 nM 7.16
CHEMBL267473 DAZOXIBEN IC50 = 70.0 nM 7.16
CHEMBL288118 IC50 = 1700.0 nM 5.77
CHEMBL294952 IC50 = 3800.0 nM 5.42
CHEMBL42263 IC50 > 10000.0 nM -
CHEMBL24984 IC50 > 10000.0 nM -
CHEMBL30024 IC50 > 100000.0 nM -