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Assay Detail

CHEMBL972452

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Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense after 72 hrs by alamar blue assay
31
Total Activities
31
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

Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
Faist J, Seebacher W, Schlapper C, Kaiser M, Brun R, Saf R, Weis R.
Bioorg Med Chem (2009) 17 : 3595 -3603
PubMed 19395265 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.90 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.41
CHEMBL512069 1 6.89
CHEMBL466437 1 6.85
CHEMBL235333 1 6.68
CHEMBL511209 1 6.64
CHEMBL512241 1 6.57
CHEMBL237458 1 6.50
CHEMBL510747 1 6.46
CHEMBL237613 1 6.43
CHEMBL466095 1 6.39
CHEMBL392520 1 6.25
CHEMBL219073 1 6.22
CHEMBL235539 1 6.21
CHEMBL513643 1 6.16
CHEMBL392519 1 6.14
CHEMBL495021 1 6.07
CHEMBL466497 1 6.06
CHEMBL392729 1 6.06
CHEMBL466108 1 5.95
CHEMBL375182 1 5.94
CHEMBL466107 1 5.80
CHEMBL237612 1 5.70
CHEMBL522353 1 5.56
CHEMBL521525 1 5.38
CHEMBL414705 1 5.18
CHEMBL522683 1 4.55
CHEMBL494152 1 4.51
CHEMBL468130 1 4.50
CHEMBL493558 1 4.39
CHEMBL494024 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 3.9 nM 8.41
CHEMBL512069 IC50 = 130.0 nM 6.89
CHEMBL466437 IC50 = 140.0 nM 6.85
CHEMBL235333 IC50 = 210.0 nM 6.68
CHEMBL511209 IC50 = 230.0 nM 6.64
CHEMBL512241 IC50 = 270.0 nM 6.57
CHEMBL237458 IC50 = 320.0 nM 6.50
CHEMBL510747 IC50 = 350.0 nM 6.46
CHEMBL237613 IC50 = 370.0 nM 6.43
CHEMBL466095 IC50 = 410.0 nM 6.39
CHEMBL392520 IC50 = 560.0 nM 6.25
CHEMBL219073 IC50 = 600.0 nM 6.22
CHEMBL235539 IC50 = 610.0 nM 6.21
CHEMBL513643 IC50 = 690.0 nM 6.16
CHEMBL392519 IC50 = 720.0 nM 6.14
CHEMBL495021 IC50 = 860.0 nM 6.07
CHEMBL466497 IC50 = 870.0 nM 6.06
CHEMBL392729 IC50 = 870.0 nM 6.06
CHEMBL466108 IC50 = 1130.0 nM 5.95
CHEMBL375182 IC50 = 1160.0 nM 5.94
CHEMBL466107 IC50 = 1600.0 nM 5.80
CHEMBL237612 IC50 = 1990.0 nM 5.70
CHEMBL522353 IC50 = 2740.0 nM 5.56
CHEMBL521525 IC50 = 4150.0 nM 5.38
CHEMBL414705 IC50 = 6570.0 nM 5.18
CHEMBL522683 IC50 = 28250.0 nM 4.55
CHEMBL494152 IC50 = 30790.0 nM 4.51
CHEMBL468130 IC50 = 31930.0 nM 4.50
CHEMBL493558 IC50 = 41070.0 nM 4.39
CHEMBL494024 IC50 = 45800.0 nM 4.34
CHEMBL493963 IC50 = 92010.0 nM 4.04