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Assay Detail

CHEMBL657758

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Binding
The calpain inhibitory activity(I 50) was measured as ability to enter the platelet to inhibit calpain after cell lysis(assay 2)
11
Total Activities
11
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 11 5.65 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL302897 1 6.52
CHEMBL61010 1 6.00
CHEMBL64174 1 5.70
CHEMBL63494 1 5.70
CHEMBL303315 1 5.70
CHEMBL418130 1 5.70
CHEMBL294046 1 5.52
CHEMBL63440 ALOXISTATIN 2.0 1 5.40
CHEMBL60482 1 5.40
CHEMBL302443 1 5.30
CHEMBL64647 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL302897 IC50 = 300.0 nM 6.52
CHEMBL61010 IC50 = 1000.0 nM 6.00
CHEMBL64174 IC50 = 2000.0 nM 5.70
CHEMBL63494 IC50 = 2000.0 nM 5.70
CHEMBL303315 IC50 = 2000.0 nM 5.70
CHEMBL418130 IC50 = 2000.0 nM 5.70
CHEMBL294046 IC50 = 3000.0 nM 5.52
CHEMBL63440 ALOXISTATIN IC50 = 4000.0 nM 5.40
CHEMBL60482 IC50 = 4000.0 nM 5.40
CHEMBL302443 IC50 = 5000.0 nM 5.30
CHEMBL64647 IC50 = 6000.0 nM 5.22