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Assay Detail

CHEMBL654080

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Functional
Inhibition of degradation of tyrosine kinase pp60src by Calpain 1 in human platelets
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Calpain-1 catalytic subunit (CHEMBL3891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.
Lubisch W, Beckenbach E, Bopp S, Hofmann HP, Kartal A, Kästel C, Lindner T, Metz-Garrecht M, Reeb J, Regner F, Vierling M, Möller A.
J Med Chem (2003) 46 : 2404 -2412
PubMed 12773044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.05 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423112 1 6.16
CHEMBL80605 1 6.16
CHEMBL77784 1 6.10
CHEMBL80933 1 6.00
CHEMBL310855 1 5.85
CHEMBL281874 1 -
CHEMBL26631 1 -
CHEMBL80903 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423112 IC50 = 700.0 nM 6.16
CHEMBL80605 IC50 = 700.0 nM 6.16
CHEMBL77784 IC50 = 800.0 nM 6.10
CHEMBL80933 IC50 = 1000.0 nM 6.00
CHEMBL310855 IC50 = 1400.0 nM 5.85
CHEMBL281874 IC50 = - nM -
CHEMBL26631 IC50 = - nM -
CHEMBL80903 IC50 = - nM -