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Assay Detail

CHEMBL3376046

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

Functional
Antiprotozoan activity against Trypanosoma brucei rhodesiense STIB 900 trypomastigotes
10
Total Activities
10
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

Hydroxamic acid based histone deacetylase inhibitors with confirmed activity against the malaria parasite.
Giannini G, Battistuzzi G, Vignola D.
Bioorg Med Chem Lett (2015) 25 : 459 -461
PubMed 25563890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.63 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.22
CHEMBL3353928 1 5.62
CHEMBL3353926 1 5.60
CHEMBL98 VORINOSTAT 4.0 1 5.50
CHEMBL3353925 1 5.49
CHEMBL3098602 1 5.38
CHEMBL3353927 1 5.32
CHEMBL3098604 1 5.26
CHEMBL3098695 1 5.22
CHEMBL3098691 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 6.0 nM 8.22
CHEMBL3353928 IC50 = 2380.0 nM 5.62
CHEMBL3353926 IC50 = 2510.0 nM 5.60
CHEMBL98 VORINOSTAT IC50 = 3170.0 nM 5.50
CHEMBL3353925 IC50 = 3230.0 nM 5.49
CHEMBL3098602 IC50 = 4155.0 nM 5.38
CHEMBL3353927 IC50 = 4750.0 nM 5.32
CHEMBL3098604 IC50 = 5515.0 nM 5.26
CHEMBL3098695 IC50 = 6045.0 nM 5.22
CHEMBL3098691 IC50 = 19950.0 nM 4.70