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Assay Detail

CHEMBL808529

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

Binding
In vitro inhibition of thromboxane synthase (TSI) activity was determined by using human serum levels of TXB2
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Serum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives.
Takeuchi K, Kohn TJ, Mais DE, True TA, Wyss VL, Jakubowski JA.
Bioorg Med Chem Lett (1998) 8 : 1943 -1948
PubMed 9873463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.13 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293764 1 7.72
CHEMBL57359 1 7.64
CHEMBL57576 1 7.61
CHEMBL60710 1 7.60
CHEMBL291539 1 7.51
CHEMBL61306 1 7.42
CHEMBL26820 (E)-ISBOGREL 1 7.31
CHEMBL299467 2 7.26
CHEMBL56778 1 7.09
CHEMBL58332 1 7.09
CHEMBL56722 1 6.64
CHEMBL418323 1 5.50
CHEMBL59547 1 -
CHEMBL60516 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293764 IC50 = 19.0 nM 7.72
CHEMBL57359 IC50 = 23.0 nM 7.64
CHEMBL57576 IC50 = 24.7 nM 7.61
CHEMBL60710 IC50 = 25.0 nM 7.60
CHEMBL291539 IC50 = 31.2 nM 7.51
CHEMBL61306 IC50 = 38.0 nM 7.42
CHEMBL26820 (E)-ISBOGREL IC50 = 48.7 nM 7.31
CHEMBL299467 IC50 = 55.0 nM 7.26
CHEMBL56778 IC50 = 82.1 nM 7.09
CHEMBL58332 IC50 = 82.1 nM 7.09
CHEMBL56722 IC50 = 230.0 nM 6.64
CHEMBL299467 IC50 = 550.0 nM 6.26
CHEMBL418323 IC50 = 3167.0 nM 5.50
CHEMBL59547 IC50 > 10000.0 nM -
CHEMBL60516 IC50 > 10000.0 nM -