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Assay Detail

CHEMBL816595

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

Functional
Inhibition of Thromboxane B2 formation in collagen-stimulated human platelets in platelet rich plasma.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids.
Manley PW, Tuffin DP, Allanson NM, Buckle PE, Lad N, Lai SM, Lunt DO, Porter RA, Wade PJ.
J Med Chem (1987) 30 : 1812 -1818
PubMed 3656356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.03 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51802 1 7.44
CHEMBL54268 1 6.92
CHEMBL301609 1 6.92
CHEMBL53703 1 6.41
CHEMBL51367 1 6.38
CHEMBL41908 1 6.27
CHEMBL299321 1 6.25
CHEMBL301189 1 6.14
CHEMBL53487 1 6.12
CHEMBL412442 1 6.00
CHEMBL267473 DAZOXIBEN 2.0 1 5.89
CHEMBL53700 1 5.84
CHEMBL52858 1 5.72
CHEMBL53656 1 5.40
CHEMBL53480 1 5.08
CHEMBL53881 1 5.00
CHEMBL296611 1 4.75
CHEMBL52568 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51802 IC50 = 36.0 nM 7.44
CHEMBL54268 IC50 = 120.0 nM 6.92
CHEMBL301609 IC50 = 120.0 nM 6.92
CHEMBL53703 IC50 = 390.0 nM 6.41
CHEMBL51367 IC50 = 420.0 nM 6.38
CHEMBL41908 IC50 = 540.0 nM 6.27
CHEMBL299321 IC50 = 560.0 nM 6.25
CHEMBL301189 IC50 = 730.0 nM 6.14
CHEMBL53487 IC50 = 750.0 nM 6.12
CHEMBL412442 IC50 = 1000.0 nM 6.00
CHEMBL267473 DAZOXIBEN IC50 = 1290.0 nM 5.89
CHEMBL53700 IC50 = 1430.0 nM 5.84
CHEMBL52858 IC50 = 1890.0 nM 5.72
CHEMBL53656 IC50 = 4000.0 nM 5.40
CHEMBL53480 IC50 = 8330.0 nM 5.08
CHEMBL53881 IC50 = 10000.0 nM 5.00
CHEMBL296611 IC50 = 17600.0 nM 4.75
CHEMBL52568 IC50 > 20000.0 nM -