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Assay Detail

CHEMBL816623

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

Binding
Tested for inhibitory activity against thromboxane A2 (TXA2) synthetase in microsome of human platelets
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Novel dual inhibitors of 5-lipoxygenase and thromboxane A2 synthetase: synthesis and structure-activity relationships of 3-pyridylmethyl-substituted 2-amino-6-hydroxybenzothiazole derivatives.
Hibi S, Okamoto Y, Tagami K, Numata H, Kobayashi N, Shinoda M, Kawahara T, Murakami M, Oketani K, Inoue T.
J Med Chem (1994) 37 : 3062 -3070
PubMed 7932529 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.14 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105139 1 8.05
CHEMBL3217077 1 8.00
CHEMBL105587 1 6.41
CHEMBL105386 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105139 IC50 = 9.0 nM 8.05
CHEMBL3217077 IC50 = 10.0 nM 8.00
CHEMBL105587 IC50 = 390.0 nM 6.41
CHEMBL105386 IC50 = 810.0 nM 6.09