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Assay Detail

CHEMBL656202

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Binding
Inhibitory activity against human Calpain 1 isolated from erythrocytes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 8 7.47 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310855 1 8.08
CHEMBL77784 1 7.88
CHEMBL80903 1 7.82
CHEMBL423112 1 7.81
CHEMBL80933 1 7.74
CHEMBL80605 1 7.57
CHEMBL26631 1 6.85
CHEMBL281874 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310855 Ki = 8.4 nM 8.08
CHEMBL77784 Ki = 13.3 nM 7.88
CHEMBL80903 Ki = 15.0 nM 7.82
CHEMBL423112 Ki = 15.5 nM 7.81
CHEMBL80933 Ki = 18.3 nM 7.74
CHEMBL80605 Ki = 27.0 nM 7.57
CHEMBL26631 Ki = 140.0 nM 6.85
CHEMBL281874 Ki = 1080.0 nM 5.97