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Assay Detail

CHEMBL5148463

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

Functional
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei Lister 427 assessed as parasite growth inhibition incubated for 72 hrs by resazurin dye based analysis
7
Total Activities
7
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

Multitarget, Selective Compound Design Yields Potent Inhibitors of a Kinetoplastid Pteridine Reductase 1.
Pöhner I, Quotadamo A, Panecka-Hofman J, Luciani R, Santucci M, Linciano P, Landi G, Di Pisa F, Dello Iacono L, Pozzi C, Mangani S, Gul S, Witt G, Ellinger B, Kuzikov M, Santarem N, Cordeiro-da-Silva A, Costi MP, Venturelli A, Wade RC.
J Med Chem (2022) 65 : 9011 -9033
PubMed 35675511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.53 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.72
CHEMBL5201183 1 6.18
CHEMBL5184646 1 5.89
CHEMBL5193762 1 5.34
CHEMBL5188304 1 -
CHEMBL5200612 1 -
CHEMBL5199171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE EC50 = 1.9 nM 8.72
CHEMBL5201183 EC50 = 660.0 nM 6.18
CHEMBL5184646 EC50 = 1300.0 nM 5.89
CHEMBL5193762 EC50 = 4530.0 nM 5.34
CHEMBL5188304 EC50 - -
CHEMBL5200612 EC50 - -
CHEMBL5199171 EC50 - -