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Assay Detail

CHEMBL4057142

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

Binding
Inhibition of Trypanosoma brucei rhodesiense rhodesain using Cbz-Phe-Arg-AMC as substrate measured for 10 mins by spectrofluorometric analysis
12
Total Activities
12
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 Autocuration

Target

Rhodesain (CHEMBL4188)
Type SINGLE PROTEIN
Organism Trypanosoma brucei rhodesiense

Publication

Bistacrines as potential antitrypanosomal agents.
Schmidt I, Göllner S, Fuß A, Stich A, Kucharski A, Schirmeister T, Katzowitsch E, Bruhn H, Miliu A, Krauth-Siegel RL, Holzgrabe U.
Bioorg Med Chem (2017) 25 : 4526 -4531
PubMed 28698054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.83 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3814557 1 5.24
CHEMBL73160 1 5.13
CHEMBL3814548 1 4.88
CHEMBL75274 1 4.77
CHEMBL3815015 1 4.74
CHEMBL424707 1 4.71
CHEMBL3813885 1 4.58
CHEMBL4103108 1 4.58
CHEMBL179732 1 -
CHEMBL73800 1 -
CHEMBL32823 1 -
CHEMBL4078832 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3814557 IC50 = 5800.0 nM 5.24
CHEMBL73160 IC50 = 7400.0 nM 5.13
CHEMBL3814548 IC50 = 13300.0 nM 4.88
CHEMBL75274 IC50 = 16900.0 nM 4.77
CHEMBL3815015 IC50 = 18100.0 nM 4.74
CHEMBL424707 IC50 = 19400.0 nM 4.71
CHEMBL3813885 IC50 = 26600.0 nM 4.58
CHEMBL4103108 IC50 = 26600.0 nM 4.58
CHEMBL179732 IC50 - -
CHEMBL73800 IC50 - -
CHEMBL32823 IC50 - -
CHEMBL4078832 IC50 - -