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

CHEMBL659708

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

Binding
Inhibitory activity against caspase-8
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Caspase-8 (CHEMBL3776)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Han Y, Giroux A, Grimm EL, Aspiotis R, Francoeur S, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt JP, Rasper DM, Tam J, Tawa P, Thornberry NA, Paterson EP, Garcia-Calvo M, Becker JW, Rotonda J, Nicholson DW, Zamboni RJ.
Bioorg Med Chem Lett (2004) 14 : 805 -808
PubMed 14741294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.47 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417149 1 6.89
CHEMBL166754 1 6.31
CHEMBL167882 1 6.09
CHEMBL352426 1 5.82
CHEMBL353919 1 5.70
CHEMBL82932 1 5.64
CHEMBL167670 1 5.62
CHEMBL167071 1 5.54
CHEMBL168816 1 5.48
CHEMBL81038 1 5.42
CHEMBL168065 1 5.20
CHEMBL166513 1 5.18
CHEMBL354612 1 5.11
CHEMBL166992 1 5.06
CHEMBL352554 1 5.03
CHEMBL168847 1 4.85
CHEMBL166472 1 4.81
CHEMBL354345 1 4.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL417149 IC50 = 130.0 nM 6.89
CHEMBL166754 IC50 = 490.0 nM 6.31
CHEMBL167882 IC50 = 810.0 nM 6.09
CHEMBL352426 IC50 = 1500.0 nM 5.82
CHEMBL353919 IC50 = 2000.0 nM 5.70
CHEMBL82932 IC50 = 2300.0 nM 5.64
CHEMBL167670 IC50 = 2400.0 nM 5.62
CHEMBL167071 IC50 = 2900.0 nM 5.54
CHEMBL168816 IC50 = 3300.0 nM 5.48
CHEMBL81038 IC50 = 3850.0 nM 5.42
CHEMBL168065 IC50 = 6300.0 nM 5.20
CHEMBL166513 IC50 = 6600.0 nM 5.18
CHEMBL354612 IC50 = 7800.0 nM 5.11
CHEMBL166992 IC50 = 8700.0 nM 5.06
CHEMBL352554 IC50 = 9300.0 nM 5.03
CHEMBL168847 IC50 = 14000.0 nM 4.85
CHEMBL166472 IC50 = 15500.0 nM 4.81
CHEMBL354345 IC50 = 22500.0 nM 4.65