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Assay Detail

CHEMBL2382935

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

Binding
Inhibition of human recombinant caspase-7 assessed as Ac-DEVD-AMC conversion to 7-amino-4-methylcoumarin incubated for 10 mins prior to substrate addition measured after 10 mins by spectrophotometric analysis
9
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, 18F-radiolabeling, and in vivo biodistribution studies of N-fluorohydroxybutyl isatin sulfonamides using positron emission tomography.
Limpachayaporn P, Wagner S, Kopka K, Hermann S, Schäfers M, Haufe G.
J Med Chem (2013) 56 : 4509 -4520
PubMed 23656488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.15 9.02
Ki 2 7.05 7.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381343 1 9.02
CHEMBL2381345 1 7.57
CHEMBL293034 1 7.33
CHEMBL2381346 1 7.15
CHEMBL2381344 1 6.99
CHEMBL2381349 1 6.89
CHEMBL60190 2 6.77
CHEMBL2381348 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381343 IC50 = 0.951 nM 9.02
CHEMBL2381345 IC50 = 27.0 nM 7.57
CHEMBL293034 Ki = 47.0 nM 7.33
CHEMBL2381346 IC50 = 71.0 nM 7.15
CHEMBL2381344 IC50 = 103.0 nM 6.99
CHEMBL2381349 IC50 = 128.0 nM 6.89
CHEMBL60190 Ki = 170.0 nM 6.77
CHEMBL2381348 IC50 = 296.0 nM 6.53
CHEMBL60190 IC50 = 1290.0 nM 5.89