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Assay Detail

CHEMBL863672

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Binding
Inhibition of porcein kidney m calpain
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Kidney
Confidence 9 — Direct single protein target
Curated By Expert

Target

Calpain-2 catalytic subunit (CHEMBL4143)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Exploration of orally available calpain inhibitors 2: peptidyl hemiacetal derivatives.
Shirasaki Y, Nakamura M, Yamaguchi M, Miyashita H, Sakai O, Inoue J.
J Med Chem (2006) 49 : 3926 -3932
PubMed 16789748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.60 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL209457 1 7.68
CHEMBL288365 1 7.31
CHEMBL210347 1 6.92
CHEMBL378215 1 6.77
CHEMBL209274 1 6.77
CHEMBL211200 1 6.72
CHEMBL207440 1 6.72
CHEMBL378465 1 6.70
CHEMBL379402 1 6.62
CHEMBL209286 1 6.60
CHEMBL261953 1 6.47
CHEMBL208986 1 5.77
CHEMBL377197 1 5.72
CHEMBL209736 1 5.58
CHEMBL206737 1 -
CHEMBL288882 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL209457 IC50 = 21.0 nM 7.68
CHEMBL288365 IC50 = 49.0 nM 7.31
CHEMBL210347 IC50 = 120.0 nM 6.92
CHEMBL378215 IC50 = 170.0 nM 6.77
CHEMBL209274 IC50 = 170.0 nM 6.77
CHEMBL211200 IC50 = 190.0 nM 6.72
CHEMBL207440 IC50 = 190.0 nM 6.72
CHEMBL378465 IC50 = 200.0 nM 6.70
CHEMBL379402 IC50 = 240.0 nM 6.62
CHEMBL209286 IC50 = 250.0 nM 6.60
CHEMBL261953 IC50 = 340.0 nM 6.47
CHEMBL208986 IC50 = 1700.0 nM 5.77
CHEMBL377197 IC50 = 1900.0 nM 5.72
CHEMBL209736 IC50 = 2600.0 nM 5.58
CHEMBL206737 IC50 > 100000.0 nM -
CHEMBL288882 IC50 - -