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Assay Detail

CHEMBL928702

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Binding
Inhibition of human mu-calpain
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of 4-quinolinone 2-carboxamides as calpain inhibitors.
Nam DH, Lee KS, Kim SH, Kim SM, Jung SY, Chung SH, Kim HJ, Kim ND, Jin C, Lee YS.
Bioorg Med Chem Lett (2008) 18 : 205 -209
PubMed 18024028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.67 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195728 1 7.40
CHEMBL423112 1 7.16
CHEMBL254142 1 6.15
CHEMBL253315 1 6.14
CHEMBL253112 1 5.75
CHEMBL401986 1 5.43
CHEMBL401985 1 5.42
CHEMBL253111 1 5.30
CHEMBL253113 1 5.25
CHEMBL253316 1 5.20
CHEMBL253314 1 5.11
CHEMBL254948 1 5.06
CHEMBL254949 1 4.40
CHEMBL402385 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195728 IC50 = 40.0 nM 7.40
CHEMBL423112 IC50 = 70.0 nM 7.16
CHEMBL254142 IC50 = 710.0 nM 6.15
CHEMBL253315 IC50 = 730.0 nM 6.14
CHEMBL253112 IC50 = 1780.0 nM 5.75
CHEMBL401986 IC50 = 3710.0 nM 5.43
CHEMBL401985 IC50 = 3810.0 nM 5.42
CHEMBL253111 IC50 = 5010.0 nM 5.30
CHEMBL253113 IC50 = 5630.0 nM 5.25
CHEMBL253316 IC50 = 6280.0 nM 5.20
CHEMBL253314 IC50 = 7720.0 nM 5.11
CHEMBL254948 IC50 = 8620.0 nM 5.06
CHEMBL254949 IC50 = 40170.0 nM 4.40
CHEMBL402385 IC50 > 50000.0 nM -