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Assay Detail

CHEMBL1247359

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Binding
Inhibition of porcine erythrocyte calpain 1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calpain-1 catalytic subunit (CHEMBL4062)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.
Ovat A, Li ZZ, Hampton CY, Asress SA, Fernández FM, Glass JD, Powers JC.
J Med Chem (2010) 53 : 6326 -6336
PubMed 20690647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.76 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1240873 1 7.64
CHEMBL1240874 1 7.39
CHEMBL1242960 1 7.28
CHEMBL1240872 1 7.26
CHEMBL1242959 1 6.82
CHEMBL1242986 1 6.78
CHEMBL1242932 1 6.65
CHEMBL1240875 1 6.32
CHEMBL1242987 1 6.19
CHEMBL1242933 1 6.15
CHEMBL1240876 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1240873 Ki = 23.0 nM 7.64
CHEMBL1240874 Ki = 41.0 nM 7.39
CHEMBL1242960 Ki = 53.0 nM 7.28
CHEMBL1240872 Ki = 55.0 nM 7.26
CHEMBL1242959 Ki = 150.0 nM 6.82
CHEMBL1242986 Ki = 165.0 nM 6.78
CHEMBL1242932 Ki = 226.0 nM 6.65
CHEMBL1240875 Ki = 480.0 nM 6.32
CHEMBL1242987 Ki = 640.0 nM 6.19
CHEMBL1242933 Ki = 711.0 nM 6.15
CHEMBL1240876 Ki = 1370.0 nM 5.86