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Assay Detail

CHEMBL3707941

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

Binding
Fluorometric Enzymatic Assay: The inhibition of the activity of Caspase-1 to -10 by four different compounds (#53, #111, #123 & Z-DEVD-FMK used as a prodrug: z-D(OMe)E(OMe)VD(OMe)FMK (comparison control compound, SM Biochemicals LLC, Cat# SMFMK003)) and their respective IC50 values were determined using a fluorometric enzymatic assay (Active Recombinant Caspase Set IV (BioVision, Cat# K233-10-25) and Caspase Fluorometric Substrate Set II Plus (BioVision, Cat# K137-9-25)) on a Flexstation 3x (Molecular Devices). In brief, each compound was serially diluted for a final test concentration range of 0.1 nM to 3.3 uM (10-point titration). Each active recombinant Caspase (Active Recombinant Caspase Set IV (BioVision, Cat# K233-10-25)) was added to the respective wells of the 96-well High Efficiency plates (Molecular Devices, Cat#75-000-0005), followed by the addition of the diluted test compounds. DMSO (Final=1%) or Z-VAD-FMK (Caspase-Family Inhibitor, Z-VAD-FMK (BioVision, Cat#1010-100).
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Caspase-10 (CHEMBL5037)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective caspase inhibitors and uses thereof
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.70 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3678074 1 5.70
CHEMBL3673262 1 -
CHEMBL3678073 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3678074 IC50 = 2000.0 nM 5.70
CHEMBL3673262 IC50 > 3330.0 nM -
CHEMBL3678073 IC50 > 3330.0 nM -