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Assay Detail

CHEMBL2186432

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

Functional
Antitrypanosomal activity against trypomastigote form of Trypanosoma brucei rhodesiense STIB 900 assessed as growth inhibition after 72 hrs by microplate fluorometry
13
Total Activities
13
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

Conjugation of quinones with natural polyamines: toward an expanded antitrypanosomatid profile.
Lizzi F, Veronesi G, Belluti F, Bergamini C, López-Sánchez A, Kaiser M, Brun R, Krauth-Siegel RL, Hall DG, Rivas L, Bolognesi ML.
J Med Chem (2012) 55 : 10490 -10500
PubMed 23153330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.76 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.00
CHEMBL255731 1 7.30
CHEMBL2179000 1 7.16
CHEMBL256155 1 7.10
CHEMBL2178998 1 6.66
CHEMBL2179006 1 6.64
CHEMBL2179005 1 6.62
CHEMBL2178999 1 6.58
CHEMBL2179004 1 6.50
CHEMBL2177124 1 6.46
CHEMBL2179001 1 6.35
CHEMBL2179002 1 6.34
CHEMBL2179003 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 10.0 nM 8.00
CHEMBL255731 IC50 = 50.0 nM 7.30
CHEMBL2179000 IC50 = 70.0 nM 7.16
CHEMBL256155 IC50 = 80.0 nM 7.10
CHEMBL2178998 IC50 = 220.0 nM 6.66
CHEMBL2179006 IC50 = 230.0 nM 6.64
CHEMBL2179005 IC50 = 240.0 nM 6.62
CHEMBL2178999 IC50 = 260.0 nM 6.58
CHEMBL2179004 IC50 = 320.0 nM 6.50
CHEMBL2177124 IC50 = 350.0 nM 6.46
CHEMBL2179001 IC50 = 450.0 nM 6.35
CHEMBL2179002 IC50 = 460.0 nM 6.34
CHEMBL2179003 IC50 = 720.0 nM 6.14