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Assay Detail

CHEMBL810395

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

Functional
Inhibitory activity against T.b. rhodesiense
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs.
Klenke B, Stewart M, Barrett MP, Brun R, Gilbert IH.
J Med Chem (2001) 44 : 3440 -3452
PubMed 11585449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.70 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL544580 1 6.75
CHEMBL553511 1 6.58
CHEMBL536324 1 6.58
CHEMBL541581 1 6.36
CHEMBL555240 1 6.24
CHEMBL538778 1 6.24
CHEMBL544335 1 6.09
CHEMBL541322 1 6.03
CHEMBL554895 1 6.03
CHEMBL542932 1 5.96
CHEMBL544116 1 5.92
CHEMBL545281 1 5.89
CHEMBL542698 1 5.64
CHEMBL544581 1 5.46
CHEMBL543884 1 5.40
CHEMBL539797 1 5.02
CHEMBL542936 1 5.01
CHEMBL117707 1 4.89
CHEMBL117655 1 4.85
CHEMBL553117 1 4.80
CHEMBL542204 1 4.80
CHEMBL542208 1 4.77
CHEMBL552613 1 -
CHEMBL538771 1 -
CHEMBL554860 1 -
CHEMBL543641 1 -
CHEMBL543639 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL544580 IC50 = 180.0 nM 6.75
CHEMBL553511 IC50 = 265.0 nM 6.58
CHEMBL536324 IC50 = 265.0 nM 6.58
CHEMBL541581 IC50 = 440.0 nM 6.36
CHEMBL555240 IC50 = 570.0 nM 6.24
CHEMBL538778 IC50 = 580.0 nM 6.24
CHEMBL544335 IC50 = 810.0 nM 6.09
CHEMBL541322 IC50 = 940.0 nM 6.03
CHEMBL554895 IC50 = 940.0 nM 6.03
CHEMBL542932 IC50 = 1100.0 nM 5.96
CHEMBL544116 IC50 = 1200.0 nM 5.92
CHEMBL545281 IC50 = 1300.0 nM 5.89
CHEMBL542698 IC50 = 2300.0 nM 5.64
CHEMBL544581 IC50 = 3500.0 nM 5.46
CHEMBL543884 IC50 = 4020.0 nM 5.40
CHEMBL539797 IC50 = 9600.0 nM 5.02
CHEMBL542936 IC50 = 9800.0 nM 5.01
CHEMBL117707 IC50 = 13000.0 nM 4.89
CHEMBL117655 IC50 = 14000.0 nM 4.85
CHEMBL553117 IC50 = 16000.0 nM 4.80
CHEMBL542204 IC50 = 16000.0 nM 4.80
CHEMBL542208 IC50 = 17000.0 nM 4.77
CHEMBL552613 IC50 > 152000.0 nM -
CHEMBL538771 IC50 > 152000.0 nM -
CHEMBL554860 IC50 > 163000.0 nM -
CHEMBL543641 IC50 = 128000.0 nM -
CHEMBL543639 IC50 = 160000.0 nM -