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Assay Detail

CHEMBL3879206

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Binding
Antagonist activity at GP6 receptor in human platelet rich plasma assessed as inhibition of CRP-XL-induced platelet aggregation preincubated for 5 mins followed by CRP-XL addition measured after 5 mins by turbidimetric method
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Platelet glycoprotein VI (CHEMBL3308912)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Glycoprotein VI Antagonists as Antithrombotics: Synthesis, Biological Evaluation, and Molecular Modeling Studies on 2,3-Disubstituted Tetrahydropyrido(3,4-b)indoles.
Bhunia SS, Misra A, Khan IA, Gaur S, Jain M, Singh S, Saxena A, Hohlfield T, Dikshit M, Saxena AK.
J Med Chem (2017) 60 : 322 -337
PubMed 27996269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.70 5.12
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308493 1 5.12
CHEMBL3959435 2 4.27
CHEMBL191 LOSARTAN 4.0 1 -
CHEMBL2263356 1 -
CHEMBL2263357 S007-1558 (S) 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308493 IC50 = 7600.0 nM 5.12
CHEMBL3959435 IC50 = 53500.0 nM 4.27
CHEMBL3959435 Inhibition - % -
CHEMBL191 LOSARTAN IC50 = 158000.0 nM -
CHEMBL2263356 IC50 > 500000.0 nM -
CHEMBL2263357 S007-1558 (S) IC50 = 181400.0 nM -