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Assay Detail

CHEMBL3377637

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

Binding
Inhibition of human recombinant caspase 1 using Ac-YVAD-AMC substrate assessed as accumulation of cleaved fluorogenic product
28
Total Activities
28
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-1 (CHEMBL4801)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis.
Limpachayaporn P, Wagner S, Kopka K, Schober O, Schäfers M, Haufe G.
J Med Chem (2014) 57 : 9383 -9395
PubMed 25358116 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.24 5.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3359200 1 5.59
CHEMBL3359203 1 5.13
CHEMBL3359202 1 5.00
CHEMBL3359201 1 -
CHEMBL3359199 1 -
CHEMBL3359198 1 -
CHEMBL3359197 1 -
CHEMBL3359196 1 -
CHEMBL3359195 1 -
CHEMBL3359194 1 -
CHEMBL3359193 1 -
CHEMBL3359192 1 -
CHEMBL3359191 1 -
CHEMBL3359190 1 -
CHEMBL3359189 1 -
CHEMBL3359188 1 -
CHEMBL3359187 1 -
CHEMBL3359186 1 -
CHEMBL3359185 1 -
CHEMBL3359184 1 -
CHEMBL3359183 1 -
CHEMBL3359182 1 -
CHEMBL494140 1 -
CHEMBL521840 1 -
CHEMBL493926 1 -
CHEMBL521839 1 -
CHEMBL216819 1 -
CHEMBL60190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3359200 IC50 = 2590.0 nM 5.59
CHEMBL3359203 IC50 = 7430.0 nM 5.13
CHEMBL3359202 IC50 = 9970.0 nM 5.00
CHEMBL3359201 IC50 = 500000.0 nM -
CHEMBL3359199 IC50 = 500000.0 nM -
CHEMBL3359198 IC50 = 500000.0 nM -
CHEMBL3359197 IC50 = 500000.0 nM -
CHEMBL3359196 IC50 - -
CHEMBL3359195 IC50 - -
CHEMBL3359194 IC50 - -
CHEMBL3359193 IC50 - -
CHEMBL3359192 IC50 - -
CHEMBL3359191 IC50 - -
CHEMBL3359190 IC50 - -
CHEMBL3359189 IC50 = 500000.0 nM -
CHEMBL3359188 IC50 = 500000.0 nM -
CHEMBL3359187 IC50 = 500000.0 nM -
CHEMBL3359186 IC50 = 500000.0 nM -
CHEMBL3359185 IC50 - -
CHEMBL3359184 IC50 - -
CHEMBL3359183 IC50 - -
CHEMBL3359182 IC50 - -
CHEMBL494140 IC50 - -
CHEMBL521840 IC50 - -
CHEMBL493926 IC50 - -
CHEMBL521839 IC50 - -
CHEMBL216819 IC50 - -
CHEMBL60190 IC50 = 500000.0 nM -