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Assay Detail

CHEMBL2090696

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

Binding
Inhibition of Trypanosoma brucei CatB
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin B-like cysteine protease (CHEMBL5832)
Type SINGLE PROTEIN
Organism Trypanosoma brucei

Publication

Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives.
Lavrado J, Mackey Z, Hansell E, McKerrow JH, Paulo A, Moreira R.
Bioorg Med Chem Lett (2012) 22 : 6256 -6260
PubMed 22926067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.25 4.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1290380 1 4.58
CHEMBL1290489 1 4.58
CHEMBL253508 1 4.51
CHEMBL1290488 1 4.50
CHEMBL1289050 1 4.37
CHEMBL404321 1 4.37
CHEMBL1289827 1 4.26
CHEMBL1289049 1 4.23
CHEMBL1290717 1 4.23
CHEMBL1290599 1 4.23
CHEMBL404523 1 4.22
CHEMBL404522 1 4.21
CHEMBL253716 1 4.21
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE 1 4.19
CHEMBL1290718 1 4.19
CHEMBL1289828 1 4.12
CHEMBL439424 1 4.04
CHEMBL252504 1 4.02
CHEMBL253715 1 4.01
CHEMBL1290598 1 4.00
CHEMBL253717 1 -
CHEMBL267856 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1290380 IC50 = 26000.0 nM 4.58
CHEMBL1290489 IC50 = 26000.0 nM 4.58
CHEMBL253508 IC50 = 31000.0 nM 4.51
CHEMBL1290488 IC50 = 32000.0 nM 4.50
CHEMBL1289050 IC50 = 43000.0 nM 4.37
CHEMBL404321 IC50 = 43000.0 nM 4.37
CHEMBL1289827 IC50 = 55000.0 nM 4.26
CHEMBL1289049 IC50 = 59000.0 nM 4.23
CHEMBL1290717 IC50 = 59000.0 nM 4.23
CHEMBL1290599 IC50 = 59000.0 nM 4.23
CHEMBL404523 IC50 = 60000.0 nM 4.22
CHEMBL404522 IC50 = 62000.0 nM 4.21
CHEMBL253716 IC50 = 62000.0 nM 4.21
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE IC50 = 64000.0 nM 4.19
CHEMBL1290718 IC50 = 64000.0 nM 4.19
CHEMBL1289828 IC50 = 76000.0 nM 4.12
CHEMBL439424 IC50 = 91000.0 nM 4.04
CHEMBL252504 IC50 = 95000.0 nM 4.02
CHEMBL253715 IC50 = 97000.0 nM 4.01
CHEMBL1290598 IC50 = 99000.0 nM 4.00
CHEMBL253717 IC50 > 100000.0 nM -
CHEMBL267856 IC50 > 100000.0 nM -