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Assay Detail

CHEMBL1001821

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

Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900
21
Total Activities
21
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

Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives.
Ge JF, Arai C, Kaiser M, Wittlin S, Brun R, Ihara M.
J Med Chem (2008) 51 : 3654 -3658
PubMed 18476684 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.58 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.22
CHEMBL482930 1 7.85
CHEMBL485117 1 7.80
CHEMBL520624 1 7.66
CHEMBL484303 1 7.64
CHEMBL520012 1 7.04
CHEMBL482892 1 6.81
CHEMBL483707 1 6.80
CHEMBL485116 1 6.78
CHEMBL389921 1 6.64
CHEMBL482924 1 6.62
CHEMBL482921 1 6.61
CHEMBL482925 1 6.57
CHEMBL482920 1 6.07
CHEMBL482494 1 6.06
CHEMBL482719 1 5.82
CHEMBL482694 1 5.79
CHEMBL520124 1 5.59
CHEMBL482493 1 5.39
CHEMBL482495 1 5.26
CHEMBL484915 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 6.0 nM 8.22
CHEMBL482930 IC50 = 14.0 nM 7.85
CHEMBL485117 IC50 = 16.0 nM 7.80
CHEMBL520624 IC50 = 22.0 nM 7.66
CHEMBL484303 IC50 = 23.0 nM 7.64
CHEMBL520012 IC50 = 91.0 nM 7.04
CHEMBL482892 IC50 = 154.0 nM 6.81
CHEMBL483707 IC50 = 160.0 nM 6.80
CHEMBL485116 IC50 = 168.0 nM 6.78
CHEMBL389921 IC50 = 228.0 nM 6.64
CHEMBL482924 IC50 = 238.0 nM 6.62
CHEMBL482921 IC50 = 245.0 nM 6.61
CHEMBL482925 IC50 = 269.0 nM 6.57
CHEMBL482920 IC50 = 843.0 nM 6.07
CHEMBL482494 IC50 = 871.0 nM 6.06
CHEMBL482719 IC50 = 1510.0 nM 5.82
CHEMBL482694 IC50 = 1613.0 nM 5.79
CHEMBL520124 IC50 = 2594.0 nM 5.59
CHEMBL482493 IC50 = 4065.0 nM 5.39
CHEMBL482495 IC50 = 5471.0 nM 5.26
CHEMBL484915 IC50 = 8735.0 nM 5.06