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Assay Detail

CHEMBL903360

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

Binding
Inhibition of human recombinant caspase 7
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Caspase-7 (CHEMBL3468)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.
Isabel E, Aspiotis R, Black WC, Colucci J, Fortin R, Giroux A, Grimm EL, Han Y, Mellon C, Nicholson DW, Rasper DM, Renaud J, Roy S, Tam J, Tawa P, Vaillancourt JP, Xanthoudakis S, Zamboni RJ.
Bioorg Med Chem Lett (2007) 17 : 1671 -1674
PubMed 17251019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.61 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL248508 1 8.10
CHEMBL248310 1 7.19
CHEMBL180623 1 6.85
CHEMBL248309 1 6.55
CHEMBL246887 1 6.10
CHEMBL392245 1 6.04
CHEMBL396625 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL248508 IC50 = 8.0 nM 8.10
CHEMBL248310 IC50 = 64.7 nM 7.19
CHEMBL180623 IC50 = 140.0 nM 6.85
CHEMBL248309 IC50 = 280.0 nM 6.55
CHEMBL246887 IC50 = 800.0 nM 6.10
CHEMBL392245 IC50 = 920.0 nM 6.04
CHEMBL396625 IC50 = 3490.0 nM 5.46