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Assay Detail

CHEMBL808536

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

Functional
In vitro inhibition of thromboxane synthase (TXA2) in human platelet microsomes [reduced formation of TXB2 from prostaglandin H2(PGH2)]
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel agents combining platelet activating factor (PAF) receptor antagonist with thromboxane synthase inhibitor (TxSI).
Fujita M, Seki T, Inada H, Shimizu K, Takahama A, Sano T.
Bioorg Med Chem Lett (2002) 12 : 771 -774
PubMed 11858999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.35 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28196 ISBOGREL 2.0 1 9.05
CHEMBL165575 1 9.00
CHEMBL352120 1 7.68
CHEMBL11662 OZAGREL 4.0 1 7.62
CHEMBL164665 1 7.62
CHEMBL165359 1 7.39
CHEMBL349982 1 7.24
CHEMBL350961 1 7.23
CHEMBL323798 1 7.19
CHEMBL423993 1 7.19
CHEMBL354662 1 7.17
CHEMBL166193 1 7.16
CHEMBL408135 1 7.14
CHEMBL349150 1 7.14
CHEMBL164123 1 7.10
CHEMBL164758 1 6.82
CHEMBL351562 1 6.33
CHEMBL351024 1 6.27
CHEMBL166208 1 -
CHEMBL351224 1 -
CHEMBL424160 1 -
CHEMBL29067 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28196 ISBOGREL IC50 = 0.9 nM 9.05
CHEMBL165575 IC50 = 1.0 nM 9.00
CHEMBL352120 IC50 = 21.0 nM 7.68
CHEMBL11662 OZAGREL IC50 = 24.0 nM 7.62
CHEMBL164665 IC50 = 24.0 nM 7.62
CHEMBL165359 IC50 = 41.0 nM 7.39
CHEMBL349982 IC50 = 58.0 nM 7.24
CHEMBL350961 IC50 = 59.0 nM 7.23
CHEMBL323798 IC50 = 65.0 nM 7.19
CHEMBL423993 IC50 = 65.0 nM 7.19
CHEMBL354662 IC50 = 68.0 nM 7.17
CHEMBL166193 IC50 = 69.0 nM 7.16
CHEMBL408135 IC50 = 72.0 nM 7.14
CHEMBL349150 IC50 = 72.0 nM 7.14
CHEMBL164123 IC50 = 80.0 nM 7.10
CHEMBL164758 IC50 = 151.0 nM 6.82
CHEMBL351562 IC50 = 465.0 nM 6.33
CHEMBL351024 IC50 = 540.0 nM 6.27
CHEMBL166208 IC50 > 1000.0 nM -
CHEMBL351224 IC50 > 1000.0 nM -
CHEMBL424160 IC50 > 1000.0 nM -
CHEMBL29067 IC50 - nM -