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Assay Detail

CHEMBL3871901

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

Binding
Inhibition of rabbit thrombin-induced platelet aggregation in rabbit platelet-rich plasma preincubated with rabbit liver microsomes for 4 hrs followed by addition to platelet
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thrombin (CHEMBL2040703)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Design, synthesis and antithrombotic evaluation of novel non-peptide thrombin inhibitors.
Chen D, Shi J, Liu J, Zhang X, Deng X, Yang Y, Cui S, Zhu Q, Gong G, Xu Y.
Bioorg Med Chem (2017) 25 : 458 -470
PubMed 27884512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.83 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539697 DABIGATRAN ETEXILATE 4.0 1 6.26
CHEMBL3935798 1 5.71
CHEMBL3960020 1 5.09
CHEMBL3909953 1 4.60
CHEMBL3979276 1 4.05
CHEMBL3971094 1 4.04
CHEMBL3899919 1 4.04
CHEMBL3908646 1 -
CHEMBL3889895 1 -
CHEMBL3961893 1 -
CHEMBL3890936 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539697 DABIGATRAN ETEXILATE IC50 = 554.0 nM 6.26
CHEMBL3935798 IC50 = 1950.0 nM 5.71
CHEMBL3960020 IC50 = 8160.0 nM 5.09
CHEMBL3909953 IC50 = 25300.0 nM 4.60
CHEMBL3979276 IC50 = 88200.0 nM 4.05
CHEMBL3971094 IC50 = 91200.0 nM 4.04
CHEMBL3899919 IC50 = 91500.0 nM 4.04
CHEMBL3908646 IC50 > 1000000.0 nM -
CHEMBL3889895 IC50 = 164000.0 nM -
CHEMBL3961893 IC50 > 1000000.0 nM -
CHEMBL3890936 IC50 > 1000000.0 nM -