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Assay Detail

CHEMBL5350294

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

Functional
Antiparasitic activity against 1-(4-Amino-2-((3,4-difluorophenyl)amino)thiazol-5-yl)-3-hydroxy-3-methylbutan-1-one-resistant wild type Tb927.8.6290 overexpressing Trypanosoma brucei in presence of 5% Co2 at incubated for 24 hrs
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static-Cidal Screening of Analogues.
Cleghorn LAT, Wall RJ, Albrecht S, MacGowan SA, Norval S, De Rycker M, Woodland A, Spinks D, Thompson S, Patterson S, Corpas Lopez V, Dey G, Collie IT, Hallyburton I, Kime R, Simeons FRC, Stojanovski L, Frearson JA, Wyatt PG, Read KD, Gilbert IH, Wyllie S.
J Med Chem (2023) 66 : 8896 -8916
PubMed 37343180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.59 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399411 1 6.77
CHEMBL5430949 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399411 EC50 = 170.0 nM 6.77
CHEMBL5430949 EC50 = 400.0 nM 6.40