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Assay Detail

CHEMBL809674

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

Binding
Inhibitory activity against thromboxane B2 formation (TXA2 synthase) by incubating prostaglandin H2 (PGH-2) with horse platelet microsomes
74
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane-A synthase (CHEMBL1835)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thromboxane synthetase inhibitors (TXSI). Design, synthesis, and evaluation of a novel series of omega-pyridylalkenoic acids.
Kato K, Ohkawa S, Terao S, Terashita Z, Nishikawa K.
J Med Chem (1985) 28 : 287 -294
PubMed 4038746 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 74 7.12 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98477 1 7.75
CHEMBL320009 1 7.72
CHEMBL98715 1 7.70
CHEMBL432014 1 7.68
CHEMBL26820 (E)-ISBOGREL 1 7.58
CHEMBL98952 1 7.55
CHEMBL101841 1 7.55
CHEMBL319769 1 7.54
CHEMBL430495 1 7.54
CHEMBL101542 1 7.52
CHEMBL98443 1 7.52
CHEMBL98840 1 7.52
CHEMBL98439 1 7.51
CHEMBL98444 1 7.50
CHEMBL101813 1 7.50
CHEMBL329064 1 7.48
CHEMBL320158 1 7.47
CHEMBL28196 ISBOGREL 2.0 2 7.44
CHEMBL330592 1 7.43
CHEMBL328646 1 7.42
CHEMBL329965 1 7.39
CHEMBL97978 1 7.39
CHEMBL430678 1 7.39
CHEMBL98601 1 7.38
CHEMBL98901 1 7.38
CHEMBL419900 1 7.37
CHEMBL95554 1 7.35
CHEMBL97891 1 7.32
CHEMBL263019 1 7.30
CHEMBL330442 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98477 IC50 = 18.0 nM 7.75
CHEMBL320009 IC50 = 19.0 nM 7.72
CHEMBL98715 IC50 = 20.0 nM 7.70
CHEMBL432014 IC50 = 21.0 nM 7.68
CHEMBL26820 (E)-ISBOGREL IC50 = 26.0 nM 7.58
CHEMBL98952 IC50 = 28.0 nM 7.55
CHEMBL101841 IC50 = 28.0 nM 7.55
CHEMBL319769 IC50 = 29.0 nM 7.54
CHEMBL430495 IC50 = 29.0 nM 7.54
CHEMBL98840 IC50 = 30.0 nM 7.52
CHEMBL98443 IC50 = 30.0 nM 7.52
CHEMBL101542 IC50 = 30.0 nM 7.52
CHEMBL98439 IC50 = 31.0 nM 7.51
CHEMBL98444 IC50 = 32.0 nM 7.50
CHEMBL101813 IC50 = 32.0 nM 7.50
CHEMBL329064 IC50 = 33.0 nM 7.48
CHEMBL320158 IC50 = 34.0 nM 7.47
CHEMBL28196 ISBOGREL IC50 = 36.0 nM 7.44
CHEMBL330592 IC50 = 37.0 nM 7.43
CHEMBL328646 IC50 = 38.0 nM 7.42
CHEMBL329965 IC50 = 41.0 nM 7.39
CHEMBL430678 IC50 = 41.0 nM 7.39
CHEMBL97978 IC50 = 41.0 nM 7.39
CHEMBL98601 IC50 = 42.0 nM 7.38
CHEMBL98901 IC50 = 42.0 nM 7.38
CHEMBL419900 IC50 = 43.0 nM 7.37
CHEMBL95554 IC50 = 45.0 nM 7.35
CHEMBL97891 IC50 = 48.0 nM 7.32
CHEMBL330442 IC50 = 50.0 nM 7.30
CHEMBL263019 IC50 = 50.0 nM 7.30
CHEMBL28196 ISBOGREL IC50 = 51.0 nM 7.29
CHEMBL99223 IC50 = 52.0 nM 7.28
CHEMBL98282 IC50 = 54.0 nM 7.27
CHEMBL330187 IC50 = 55.0 nM 7.26
CHEMBL101812 IC50 = 55.0 nM 7.26
CHEMBL98690 IC50 = 56.0 nM 7.25
CHEMBL420086 IC50 = 58.0 nM 7.24
CHEMBL98845 IC50 = 60.0 nM 7.22
CHEMBL264871 IC50 = 60.0 nM 7.22
CHEMBL328191 IC50 = 62.0 nM 7.21
CHEMBL99319 IC50 = 63.0 nM 7.20
CHEMBL318048 IC50 = 65.0 nM 7.19
CHEMBL102200 IC50 = 65.0 nM 7.19
CHEMBL101098 IC50 = 65.0 nM 7.19
CHEMBL316848 IC50 = 70.0 nM 7.16
CHEMBL98941 IC50 = 71.0 nM 7.15
CHEMBL330440 IC50 = 73.0 nM 7.14
CHEMBL99551 IC50 = 75.0 nM 7.12
CHEMBL101785 IC50 = 80.0 nM 7.10
CHEMBL100755 IC50 = 82.0 nM 7.09