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Assay Detail

CHEMBL2350002

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

Functional
Inhibition of thrombin-induced rabbit platelet aggregation compound pre-incubated in rabbit liver microsomal suspension
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Liver
Cell Type Platelet
Subcellular Microsome
Confidence 1 — Organism
Curated By Autocuration

Target

Platelet (CHEMBL4296519)
Type CELL-LINE

Publication

Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate.
Yang XZ, Diao XJ, Yang WH, Li F, He GW, Gong GQ, Xu YG.
Bioorg Med Chem Lett (2013) 23 : 2089 -2092
PubMed 23466230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.33 6.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2347120 1 6.69
CHEMBL2347117 1 6.54
CHEMBL539697 DABIGATRAN ETEXILATE 4.0 1 6.47
CHEMBL2347118 1 6.34
CHEMBL2347116 1 6.22
CHEMBL2347119 1 6.16
CHEMBL2347121 1 6.11
CHEMBL2347122 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2347120 IC50 = 206.0 nM 6.69
CHEMBL2347117 IC50 = 290.0 nM 6.54
CHEMBL539697 DABIGATRAN ETEXILATE IC50 = 337.0 nM 6.47
CHEMBL2347118 IC50 = 453.0 nM 6.34
CHEMBL2347116 IC50 = 607.0 nM 6.22
CHEMBL2347119 IC50 = 687.0 nM 6.16
CHEMBL2347121 IC50 = 784.0 nM 6.11
CHEMBL2347122 IC50 = 841.0 nM 6.08