Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3864985

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

Binding
Inhibition of human recombinant DTT-activated caspase-5 expressed in Escherichia coli using Ac-WEHD-AMC as substrate preincubated for 45 mins followed by substrate addition by fluorescence assay
1
Total Activities
1
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

Caspase-5 (CHEMBL3131)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Variation of the aryl substituent on the piperazine ring within the 4-(piperazin-1-yl)-2,6-di(pyrrolidin-1-yl)pyrimidine scaffold unveils potent, non-competitive inhibitors of the inflammatory caspases.
Kent CR, Bryja M, Gustafson HA, Kawarski MY, Lenti G, Pierce EN, Knopp RC, Ceja V, Pati B, Walters DE, Karver CE.
Bioorg Med Chem Lett (2016) 26 : 5476 -5480
PubMed 27777011 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.81 6.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3895496 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3895496 IC50 = 155.0 nM 6.81