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Assay Detail

CHEMBL4623091

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

Binding
Inhibition of mu-calpain in porcine erythrocyte using Suc-Leu-Tyr-AMC as substrate by microtiter plate assay based Dixon plot analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Cell Type Erythrocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Calpain-1 catalytic subunit (CHEMBL4062)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.
Donkor IO, Xu J, Liu J, Cameron K.
Bioorg Med Chem (2020) 28 : 115433 -115433
PubMed 32199690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.67 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4647187 1 8.05
CHEMBL286722 1 8.00
CHEMBL4642092 1 7.85
CHEMBL4646991 1 7.80
CHEMBL4642290 1 7.75
CHEMBL4640485 1 6.56
CHEMBL428647 PACLITAXEL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4647187 Ki = 9.0 nM 8.05
CHEMBL286722 Ki = 10.0 nM 8.00
CHEMBL4642092 Ki = 14.0 nM 7.85
CHEMBL4646991 Ki = 16.0 nM 7.80
CHEMBL4642290 Ki = 18.0 nM 7.75
CHEMBL4640485 Ki = 273.0 nM 6.56
CHEMBL428647 PACLITAXEL Ki - -