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Assay Detail

CHEMBL1013486

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Binding
Inhibition of human erythrocytes mu-calpain
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calpain-1 catalytic subunit (CHEMBL3891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of 4-aryl-4-oxobutanoic acid amides as calpain inhibitors.
Zhang Y, Jung SY, Jin C, Kim ND, Gong P, Lee YS.
Bioorg Med Chem Lett (2009) 19 : 502 -507
PubMed 19041242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 5.76 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195728 1 7.40
CHEMBL423112 1 7.16
CHEMBL458859 1 6.47
CHEMBL467750 1 6.28
CHEMBL460813 1 6.27
CHEMBL459288 1 6.16
CHEMBL254142 1 6.15
CHEMBL462912 1 6.02
CHEMBL457768 1 5.93
CHEMBL465169 1 5.79
CHEMBL465173 1 5.73
CHEMBL461666 1 5.68
CHEMBL499571 1 5.67
CHEMBL464965 1 5.63
CHEMBL466551 1 5.50
CHEMBL518334 1 5.48
CHEMBL457993 1 5.42
CHEMBL464136 1 5.37
CHEMBL461669 1 5.37
CHEMBL457776 1 5.24
CHEMBL514112 1 5.21
CHEMBL466550 1 5.20
CHEMBL465172 1 5.10
CHEMBL503173 1 4.89
CHEMBL457767 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195728 IC50 = 40.0 nM 7.40
CHEMBL423112 IC50 = 70.0 nM 7.16
CHEMBL458859 IC50 = 340.0 nM 6.47
CHEMBL467750 IC50 = 520.0 nM 6.28
CHEMBL460813 IC50 = 540.0 nM 6.27
CHEMBL459288 IC50 = 700.0 nM 6.16
CHEMBL254142 IC50 = 710.0 nM 6.15
CHEMBL462912 IC50 = 950.0 nM 6.02
CHEMBL457768 IC50 = 1180.0 nM 5.93
CHEMBL465169 IC50 = 1640.0 nM 5.79
CHEMBL465173 IC50 = 1860.0 nM 5.73
CHEMBL461666 IC50 = 2090.0 nM 5.68
CHEMBL499571 IC50 = 2130.0 nM 5.67
CHEMBL464965 IC50 = 2350.0 nM 5.63
CHEMBL466551 IC50 = 3200.0 nM 5.50
CHEMBL518334 IC50 = 3330.0 nM 5.48
CHEMBL457993 IC50 = 3770.0 nM 5.42
CHEMBL464136 IC50 = 4250.0 nM 5.37
CHEMBL461669 IC50 = 4290.0 nM 5.37
CHEMBL457776 IC50 = 5730.0 nM 5.24
CHEMBL514112 IC50 = 6160.0 nM 5.21
CHEMBL466550 IC50 = 6250.0 nM 5.20
CHEMBL465172 IC50 = 8000.0 nM 5.10
CHEMBL503173 IC50 = 12990.0 nM 4.89
CHEMBL457767 IC50 = 13840.0 nM 4.86