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Assay Detail

CHEMBL4718765

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 trypomastigotes incubated for 72 hrs by resazurin dye based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei rhodesiense (CHEMBL612348)
Type ORGANISM
Organism Trypanosoma brucei rhodesiense

Publication

Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides.
Russell S,Rahmani R,Jones AJ,Newson HL,Neilde K,Cotillo I,Rahmani Khajouei M,Ferrins L,Qureishi S,Nguyen N,Martinez-Martinez MS,Weaver DF,Kaiser M,Riley J,Thomas J,De Rycker M,Read KD,Flematti GR,Ryan E,Tanghe S,Rodriguez A,Charman SA,Kessler A,Avery VM,Baell JB,Piggott MJ
J Med Chem (2016) 59 : 9686 -9720
PubMed 27548560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.67 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3800137 1 7.34
CHEMBL1872842 1 7.11
CHEMBL3797262 1 6.68
CHEMBL4758947 1 6.66
CHEMBL1459740 1 6.38
CHEMBL2094559 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3800137 IC50 = 46.0 nM 7.34
CHEMBL1872842 IC50 = 78.0 nM 7.11
CHEMBL3797262 IC50 = 210.0 nM 6.68
CHEMBL4758947 IC50 = 220.0 nM 6.66
CHEMBL1459740 IC50 = 420.0 nM 6.38
CHEMBL2094559 IC50 = 1500.0 nM 5.82