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Assay Detail

CHEMBL744607

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Suc-Leu-Tyr-AMC binding to human mu-calpain from erythrocytes
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 novel piperidine carboxamide derived calpain inhibitors.
Lubisch W, Hofmann HP, Treiber HJ, Möller A.
Bioorg Med Chem Lett (2000) 10 : 2187 -2191
PubMed 11012026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.25 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL407974 1 8.05
CHEMBL423112 1 7.82
CHEMBL69715 1 7.52
CHEMBL73171 1 6.80
CHEMBL307829 1 6.35
CHEMBL70044 1 6.34
CHEMBL409426 1 6.25
CHEMBL304400 1 6.17
CHEMBL69254 1 6.09
CHEMBL69466 1 6.02
CHEMBL303024 1 5.87
CHEMBL306220 1 4.87
CHEMBL68143 1 4.87
CHEMBL69332 1 4.48
CHEMBL68874 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL407974 Ki = 9.0 nM 8.05
CHEMBL423112 Ki = 15.0 nM 7.82
CHEMBL69715 Ki = 30.0 nM 7.52
CHEMBL73171 Ki = 160.0 nM 6.80
CHEMBL307829 Ki = 450.0 nM 6.35
CHEMBL70044 Ki = 460.0 nM 6.34
CHEMBL409426 Ki = 560.0 nM 6.25
CHEMBL304400 Ki = 670.0 nM 6.17
CHEMBL69254 Ki = 810.0 nM 6.09
CHEMBL69466 Ki = 960.0 nM 6.02
CHEMBL303024 Ki = 1350.0 nM 5.87
CHEMBL306220 Ki = 13500.0 nM 4.87
CHEMBL68143 Ki = 13600.0 nM 4.87
CHEMBL69332 Ki = 33000.0 nM 4.48
CHEMBL68874 Ki = 800000.0 nM -