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Assay Detail

CHEMBL808525

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

Binding
In vitro Inhibition of thromboxane synthase from human blood platelet microsomes
ChEMBL ↗
57
Total Activities
52
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

Dual-acting thromboxane receptor antagonist/synthase inhibitors: synthesis and biological properties of [2-substituted-4-(3-pyridyl)-1,3-dioxan-5-yl] alkenoic acids.
Faull AW, Brewster AG, Brown GR, Smithers MJ, Jackson R.
J Med Chem (1995) 38 : 686 -694
PubMed 7861416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 7.35 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346590 — — 1 7.92
CHEMBL161063 — — 1 7.82
CHEMBL26820 (E)-ISBOGREL — 1 7.77
CHEMBL352668 — — 3 7.72
CHEMBL159243 — — 1 7.70
CHEMBL159859 — — 3 7.66
CHEMBL159778 — — 1 7.66
CHEMBL159699 — — 1 7.62
CHEMBL445644 — — 2 7.60
CHEMBL435049 — — 1 7.58
CHEMBL161911 — — 1 7.54
CHEMBL159528 — — 1 7.52
CHEMBL348968 — — 1 7.50
CHEMBL159737 — — 1 7.47
CHEMBL352196 — — 1 7.44
CHEMBL423248 — — 1 7.43
CHEMBL159268 — — 1 7.43
CHEMBL161304 — — 1 7.41
CHEMBL159571 — — 1 7.41
CHEMBL160657 — — 1 7.40
CHEMBL350225 — — 1 7.40
CHEMBL159420 — — 1 7.40
CHEMBL159559 — — 1 7.40
CHEMBL159356 — — 1 7.40
CHEMBL352075 — — 1 7.39
CHEMBL422719 — — 1 7.38
CHEMBL355596 — — 1 7.38
CHEMBL161435 — — 1 7.36
CHEMBL159876 — — 1 7.35
CHEMBL350510 — — 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346590 — IC50 = 12.0 nM 7.92
CHEMBL161063 — IC50 = 15.0 nM 7.82
CHEMBL26820 (E)-ISBOGREL IC50 = 17.0 nM 7.77
CHEMBL352668 — IC50 = 19.0 nM 7.72
CHEMBL159243 — IC50 = 20.0 nM 7.70
CHEMBL159859 — IC50 = 22.0 nM 7.66
CHEMBL159778 — IC50 = 22.0 nM 7.66
CHEMBL159699 — IC50 = 24.0 nM 7.62
CHEMBL445644 — IC50 = 25.0 nM 7.60
CHEMBL435049 — IC50 = 26.0 nM 7.58
CHEMBL352668 — IC50 = 27.0 nM 7.57
CHEMBL161911 — IC50 = 29.0 nM 7.54
CHEMBL159528 — IC50 = 30.0 nM 7.52
CHEMBL348968 — IC50 = 32.0 nM 7.50
CHEMBL159737 — IC50 = 34.0 nM 7.47
CHEMBL352196 — IC50 = 36.0 nM 7.44
CHEMBL423248 — IC50 = 37.0 nM 7.43
CHEMBL159268 — IC50 = 37.0 nM 7.43
CHEMBL161304 — IC50 = 39.0 nM 7.41
CHEMBL159571 — IC50 = 39.0 nM 7.41
CHEMBL350225 — IC50 = 40.0 nM 7.40
CHEMBL160657 — IC50 = 40.0 nM 7.40
CHEMBL159356 — IC50 = 40.0 nM 7.40
CHEMBL159420 — IC50 = 40.0 nM 7.40
CHEMBL159559 — IC50 = 40.0 nM 7.40
CHEMBL352075 — IC50 = 41.0 nM 7.39
CHEMBL355596 — IC50 = 42.0 nM 7.38
CHEMBL422719 — IC50 = 42.0 nM 7.38
CHEMBL161435 — IC50 = 44.0 nM 7.36
CHEMBL353356 — IC50 = 45.0 nM 7.35
CHEMBL159876 — IC50 = 45.0 nM 7.35
CHEMBL350510 — IC50 = 45.0 nM 7.35
CHEMBL161608 — IC50 = 45.0 nM 7.35
CHEMBL161357 — IC50 = 46.0 nM 7.34
CHEMBL161105 — IC50 = 48.0 nM 7.32
CHEMBL350816 — IC50 = 50.0 nM 7.30
CHEMBL345572 — IC50 = 50.0 nM 7.30
CHEMBL445644 — IC50 = 50.0 nM 7.30
CHEMBL163278 — IC50 = 51.0 nM 7.29
CHEMBL159859 — IC50 = 51.0 nM 7.29
CHEMBL159196 — IC50 = 52.0 nM 7.28
CHEMBL161104 — IC50 = 54.0 nM 7.27
CHEMBL162032 — IC50 = 60.0 nM 7.22
CHEMBL159344 — IC50 = 66.0 nM 7.18
CHEMBL349160 — IC50 = 71.0 nM 7.15
CHEMBL158687 — IC50 = 90.0 nM 7.05
CHEMBL160467 — IC50 = 164.0 nM 6.79
CHEMBL422541 — IC50 = 220.0 nM 6.66
CHEMBL159510 — IC50 = 280.0 nM 6.55
CHEMBL350595 — IC50 = 360.0 nM 6.44