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Assay Detail

CHEMBL813724

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Functional
In vitro inhibition of TXB2 production by incubating prostaglandin H2 with human platelet microsomes.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Approach to dual-acting platelet activating factor (PAF) receptor antagonist/thromboxane synthase inhibitor (TxSI) based on the link of PAF antagonists and TxSIs.
Fujita M, Seki T, Inada H, Shimizu K, Takahama A, Sano T.
Bioorg Med Chem Lett (2002) 12 : 341 -344
PubMed 11814792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.93 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26820 (E)-ISBOGREL 1 9.05
CHEMBL117233 1 9.00
CHEMBL116975 1 8.92
CHEMBL117816 1 8.74
CHEMBL263227 1 8.44
CHEMBL117018 1 8.33
CHEMBL2111765 1 8.24
CHEMBL324533 1 7.92
CHEMBL116673 1 7.68
CHEMBL420137 1 7.68
CHEMBL11662 OZAGREL 4.0 1 7.62
CHEMBL539177 1 7.36
CHEMBL117889 1 7.28
CHEMBL323798 1 7.19
CHEMBL408135 1 7.14
CHEMBL324118 1 7.14
CHEMBL114843 1 7.06
CHEMBL114251 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26820 (E)-ISBOGREL IC50 = 0.89 nM 9.05
CHEMBL117233 IC50 = 1.0 nM 9.00
CHEMBL116975 IC50 = 1.2 nM 8.92
CHEMBL117816 IC50 = 1.8 nM 8.74
CHEMBL263227 IC50 = 3.6 nM 8.44
CHEMBL117018 IC50 = 4.7 nM 8.33
CHEMBL2111765 IC50 = 5.8 nM 8.24
CHEMBL324533 IC50 = 12.0 nM 7.92
CHEMBL116673 IC50 = 21.0 nM 7.68
CHEMBL420137 IC50 = 21.0 nM 7.68
CHEMBL11662 OZAGREL IC50 = 24.0 nM 7.62
CHEMBL539177 IC50 = 44.0 nM 7.36
CHEMBL117889 IC50 = 52.0 nM 7.28
CHEMBL323798 IC50 = 65.0 nM 7.19
CHEMBL408135 IC50 = 72.0 nM 7.14
CHEMBL324118 IC50 = 72.0 nM 7.14
CHEMBL114843 IC50 = 88.0 nM 7.06
CHEMBL114251 IC50 > 1000.0 nM -