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Assay Detail

CHEMBL960159

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

Binding
Inhibition of human recombinant caspase 6 assessed as accumulation of fluorogenic product by fluorometric assay
22
Total Activities
22
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-6 (CHEMBL3308)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.
Chu W, Rothfuss J, Chu Y, Zhou D, Mach RH.
J Med Chem (2009) 52 : 2188 -2191
PubMed 19326941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.40 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478081 1 8.10
CHEMBL523131 1 6.82
CHEMBL516251 1 6.81
CHEMBL490850 1 6.73
CHEMBL476023 1 6.71
CHEMBL490851 1 6.64
CHEMBL477047 1 6.62
CHEMBL510809 1 6.55
CHEMBL519148 1 6.49
CHEMBL477659 1 6.45
CHEMBL492060 1 6.37
CHEMBL492061 1 6.34
CHEMBL478694 1 6.33
CHEMBL521801 1 6.26
CHEMBL492059 1 6.25
CHEMBL521972 1 6.23
CHEMBL226779 1 6.04
CHEMBL476022 1 5.01
CHEMBL482841 1 4.89
CHEMBL482634 1 -
CHEMBL484273 1 -
CHEMBL439753 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478081 IC50 = 8.0 nM 8.10
CHEMBL523131 IC50 = 151.0 nM 6.82
CHEMBL516251 IC50 = 156.0 nM 6.81
CHEMBL490850 IC50 = 188.0 nM 6.73
CHEMBL476023 IC50 = 197.0 nM 6.71
CHEMBL490851 IC50 = 230.0 nM 6.64
CHEMBL477047 IC50 = 241.0 nM 6.62
CHEMBL510809 IC50 = 280.0 nM 6.55
CHEMBL519148 IC50 = 325.0 nM 6.49
CHEMBL477659 IC50 = 358.0 nM 6.45
CHEMBL492060 IC50 = 425.0 nM 6.37
CHEMBL492061 IC50 = 453.0 nM 6.34
CHEMBL478694 IC50 = 468.0 nM 6.33
CHEMBL521801 IC50 = 545.0 nM 6.26
CHEMBL492059 IC50 = 568.0 nM 6.25
CHEMBL521972 IC50 = 591.7 nM 6.23
CHEMBL226779 IC50 = 918.0 nM 6.04
CHEMBL476022 IC50 = 9833.0 nM 5.01
CHEMBL482841 IC50 = 12833.0 nM 4.89
CHEMBL482634 IC50 > 15000.0 nM -
CHEMBL484273 IC50 > 20000.0 nM -
CHEMBL439753 IC50 > 5000.0 nM -