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Assay Detail

CHEMBL785227

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

Functional
Inhibitory activity against the production of thromboxane B2 (TXB2) in glycogen-induced peritoneal cells of rat
17
Total Activities
17
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 (CHEMBL4028)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 17 6.29 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3216856 1 8.70
CHEMBL3215555 1 7.05
CHEMBL105139 1 7.05
CHEMBL3217077 1 7.00
CHEMBL3216618 1 6.96
CHEMBL3217065 1 6.75
CHEMBL104156 1 6.48
CHEMBL105587 1 6.19
CHEMBL3215528 1 5.89
CHEMBL322015 1 5.85
CHEMBL102243 1 5.70
CHEMBL105386 1 5.70
CHEMBL321358 1 5.40
CHEMBL320394 1 5.36
CHEMBL3216177 1 5.28
CHEMBL420281 1 5.26
CHEMBL3215733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3216856 IC50 = 2.0 nM 8.70
CHEMBL3215555 IC50 = 90.0 nM 7.05
CHEMBL105139 IC50 = 90.0 nM 7.05
CHEMBL3217077 IC50 = 100.0 nM 7.00
CHEMBL3216618 IC50 = 110.0 nM 6.96
CHEMBL3217065 IC50 = 180.0 nM 6.75
CHEMBL104156 IC50 = 330.0 nM 6.48
CHEMBL105587 IC50 = 650.0 nM 6.19
CHEMBL3215528 IC50 = 1300.0 nM 5.89
CHEMBL322015 IC50 = 1400.0 nM 5.85
CHEMBL102243 IC50 = 2000.0 nM 5.70
CHEMBL105386 IC50 = 2000.0 nM 5.70
CHEMBL321358 IC50 = 4000.0 nM 5.40
CHEMBL320394 IC50 = 4400.0 nM 5.36
CHEMBL3216177 IC50 = 5300.0 nM 5.28
CHEMBL420281 IC50 = 5500.0 nM 5.26
CHEMBL3215733 IC50 < 100.0 nM -