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Assay Detail

CHEMBL4041122

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

Functional
Antiparasitic activity against bloodstream form of Trypanosoma brucei brucei 449 after 24 hrs by ATPlite assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei brucei
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).
Previti S, Ettari R, Cosconati S, Amendola G, Chouchene K, Wagner A, Hellmich UA, Ulrich K, Krauth-Siegel RL, Wich PR, Schmid I, Schirmeister T, Gut J, Rosenthal PJ, Grasso S, Zappalà M.
J Med Chem (2017) 60 : 6911 -6923
PubMed 28763614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.22 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL790 CHLORHEXIDINE 4.0 1 6.17
CHEMBL4083754 1 5.60
CHEMBL4078345 1 5.50
CHEMBL4096388 1 5.49
CHEMBL4072275 1 5.42
CHEMBL4081250 1 5.26
CHEMBL4101714 1 5.22
CHEMBL4062015 1 5.22
CHEMBL4082758 1 4.89
CHEMBL2402204 1 4.62
CHEMBL4093034 1 4.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL790 CHLORHEXIDINE EC50 = 670.0 nM 6.17
CHEMBL4083754 EC50 = 2500.0 nM 5.60
CHEMBL4078345 EC50 = 3180.0 nM 5.50
CHEMBL4096388 EC50 = 3230.0 nM 5.49
CHEMBL4072275 EC50 = 3850.0 nM 5.42
CHEMBL4081250 EC50 = 5480.0 nM 5.26
CHEMBL4101714 EC50 = 6080.0 nM 5.22
CHEMBL4062015 EC50 = 6050.0 nM 5.22
CHEMBL4082758 EC50 = 12900.0 nM 4.89
CHEMBL2402204 EC50 = 23700.0 nM 4.62
CHEMBL4093034 EC50 = 97200.0 nM 4.01