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Assay Detail

CHEMBL2090300

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

Functional
Antiplatelet activity against rabbit platelets assessed as inhibition of thrombin-induced platelet aggregation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Cell Type Platelet
Confidence 1 — Organism
Curated By Autocuration

Publication

Synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing a cleavable moiety with anti-platelet activity.
Yang XZ, Yang WH, Xu YG, Diao XJ, He GW, Gong GQ.
Eur J Med Chem (2012) 57 : 21 -28
PubMed 23043765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.98 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2087701 1 8.50
CHEMBL2087702 1 7.42
CHEMBL2087705 1 7.14
CHEMBL2087703 1 6.66
CHEMBL2087704 1 6.54
CHEMBL2087707 1 6.54
CHEMBL2087706 1 6.53
CHEMBL539697 DABIGATRAN ETEXILATE 4.0 1 6.49
CHEMBL63331 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2087701 IC50 = 3.13 nM 8.50
CHEMBL2087702 IC50 = 38.1 nM 7.42
CHEMBL2087705 IC50 = 72.8 nM 7.14
CHEMBL2087703 IC50 = 218.0 nM 6.66
CHEMBL2087704 IC50 = 292.0 nM 6.54
CHEMBL2087707 IC50 = 287.0 nM 6.54
CHEMBL2087706 IC50 = 295.0 nM 6.53
CHEMBL539697 DABIGATRAN ETEXILATE IC50 = 326.0 nM 6.49
CHEMBL63331 IC50 = 8410000.0 nM -