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Assay Detail

CHEMBL659382

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Binding
The ability of compound to inhibit calpain in a preparation of lysed platelets was measured with a caseinolytic assay(assay 1)
9
Total Activities
9
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

Ester and amide derivatives of E64c as inhibitors of platelet calpains.
Huang Z, McGowan EB, Detwiler TC.
J Med Chem (1992) 35 : 2048 -2054
PubMed 1597856 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.76 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418661 E-64C 1 7.40
CHEMBL294046 1 6.30
CHEMBL61010 1 6.16
CHEMBL63494 1 6.00
CHEMBL303315 1 5.70
CHEMBL302897 1 5.70
CHEMBL63440 ALOXISTATIN 2.0 1 5.40
CHEMBL60482 1 5.22
CHEMBL62988 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418661 E-64C IC50 = 40.0 nM 7.40
CHEMBL294046 IC50 = 500.0 nM 6.30
CHEMBL61010 IC50 = 700.0 nM 6.16
CHEMBL63494 IC50 = 1000.0 nM 6.00
CHEMBL303315 IC50 = 2000.0 nM 5.70
CHEMBL302897 IC50 = 2000.0 nM 5.70
CHEMBL63440 ALOXISTATIN IC50 = 4000.0 nM 5.40
CHEMBL60482 IC50 = 6000.0 nM 5.22
CHEMBL62988 IC50 = 100000.0 nM 4.00