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Assay Detail

CHEMBL827857

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Binding
Inhibitory concentration against human plasma mu-calpain
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors.
Lee KS, Seo SH, Lee YH, Kim HD, Son MH, Chung BY, Lee JY, Jin C, Lee YS.
Bioorg Med Chem Lett (2005) 15 : 2857 -2860
PubMed 15911268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.87 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL423112 1 6.70
CHEMBL195728 1 6.62
CHEMBL196671 1 6.35
CHEMBL382711 1 6.28
CHEMBL195992 1 6.14
CHEMBL382964 1 6.09
CHEMBL196113 1 5.61
CHEMBL196990 1 5.34
CHEMBL197415 1 5.25
CHEMBL197420 1 5.09
CHEMBL193345 1 5.06
CHEMBL196184 1 -
CHEMBL274229 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL423112 IC50 = 200.0 nM 6.70
CHEMBL195728 IC50 = 240.0 nM 6.62
CHEMBL196671 IC50 = 450.0 nM 6.35
CHEMBL382711 IC50 = 530.0 nM 6.28
CHEMBL195992 IC50 = 720.0 nM 6.14
CHEMBL382964 IC50 = 810.0 nM 6.09
CHEMBL196113 IC50 = 2480.0 nM 5.61
CHEMBL196990 IC50 = 4530.0 nM 5.34
CHEMBL197415 IC50 = 5690.0 nM 5.25
CHEMBL197420 IC50 = 8170.0 nM 5.09
CHEMBL193345 IC50 = 8730.0 nM 5.06
CHEMBL196184 IC50 > 20000.0 nM -
CHEMBL274229 IC50 > 20000.0 nM -