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Assay Detail

CHEMBL805131

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

Binding
Inhibitory activity against Trypanosoma brucei rhodesiense cysteine protease rhodesain
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei rhodesiense
Confidence 9 — Direct single protein target
Curated By Expert

Target

Rhodesain (CHEMBL4188)
Type SINGLE PROTEIN
Organism Trypanosoma brucei rhodesiense

Publication

Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
Chiyanzu I, Hansell E, Gut J, Rosenthal PJ, McKerrow JH, Chibale K.
Bioorg Med Chem Lett (2003) 13 : 3527 -3530
PubMed 14505663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 4.99 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119370 1 6.00
CHEMBL118355 1 5.52
CHEMBL333137 1 5.46
CHEMBL119213 1 5.22
CHEMBL418861 1 5.16
CHEMBL119756 1 4.82
CHEMBL118210 1 4.82
CHEMBL119828 1 4.82
CHEMBL119345 1 4.82
CHEMBL120254 1 4.77
CHEMBL119515 1 4.52
CHEMBL118830 1 4.00
CHEMBL115581 1 -
CHEMBL118596 1 -
CHEMBL117515 1 -
CHEMBL326294 ISATIN 1 -
CHEMBL116649 1 -
CHEMBL120076 1 -
CHEMBL117767 1 -
CHEMBL118305 5-NITROISATIN 1 -
CHEMBL118638 1 -
CHEMBL336693 1 -
CHEMBL333067 1 -
CHEMBL326185 1 -
CHEMBL324722 1 -
CHEMBL118762 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119370 IC50 = 1000.0 nM 6.00
CHEMBL118355 IC50 = 3000.0 nM 5.52
CHEMBL333137 IC50 = 3500.0 nM 5.46
CHEMBL119213 IC50 = 6000.0 nM 5.22
CHEMBL418861 IC50 = 7000.0 nM 5.16
CHEMBL119756 IC50 = 15000.0 nM 4.82
CHEMBL118210 IC50 = 15000.0 nM 4.82
CHEMBL119828 IC50 = 15000.0 nM 4.82
CHEMBL119345 IC50 = 15000.0 nM 4.82
CHEMBL120254 IC50 = 17000.0 nM 4.77
CHEMBL119515 IC50 = 30000.0 nM 4.52
CHEMBL118830 IC50 = 100000.0 nM 4.00
CHEMBL115581 IC50 >> 10000.0 nM -
CHEMBL118596 IC50 >> 10000.0 nM -
CHEMBL117515 IC50 >> 10000.0 nM -
CHEMBL326294 ISATIN IC50 >> 10000.0 nM -
CHEMBL116649 IC50 >> 10000.0 nM -
CHEMBL120076 IC50 >> 10000.0 nM -
CHEMBL117767 IC50 >> 10000.0 nM -
CHEMBL118305 5-NITROISATIN IC50 >> 10000.0 nM -
CHEMBL118638 IC50 >> 10000.0 nM -
CHEMBL336693 IC50 >> 10000.0 nM -
CHEMBL333067 IC50 >> 10000.0 nM -
CHEMBL326185 IC50 >> 10000.0 nM -
CHEMBL324722 IC50 >> 10000.0 nM -
CHEMBL118762 IC50 >> 10000.0 nM -