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Assay Detail

CHEMBL719973

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

Functional
In vitro inhibitory concentration against mice infected with Trypanosoma brucei pentamidine-sensitive strain (EATRO Lab 110).
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Trypanocidal activity of conformationally restricted pentamidine congeners.
Donkor IO, Huang TL, Tao B, Rattendi D, Lane S, Vargas M, Goldberg B, Bacchi C.
J Med Chem (2003) 46 : 1041 -1048
PubMed 12620080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.35 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 9.10
CHEMBL269032 1 8.67
CHEMBL25526 1 8.03
CHEMBL8892 1 7.73
CHEMBL9185 1 7.56
CHEMBL9126 1 7.24
CHEMBL9391 1 7.16
CHEMBL267154 1 7.15
CHEMBL9516 1 7.07
CHEMBL9479 1 6.77
CHEMBL9053 1 6.75
CHEMBL276449 1 6.27
CHEMBL9025 1 6.06
CHEMBL2311124 1 -
CHEMBL9121 1 -
CHEMBL9531 1 -
CHEMBL266808 1 -
CHEMBL9490 1 -
CHEMBL9341 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 0.8 nM 9.10
CHEMBL269032 IC50 = 2.15 nM 8.67
CHEMBL25526 IC50 = 9.4 nM 8.03
CHEMBL8892 IC50 = 18.5 nM 7.73
CHEMBL9185 IC50 = 27.5 nM 7.56
CHEMBL9126 IC50 = 58.0 nM 7.24
CHEMBL9391 IC50 = 70.0 nM 7.16
CHEMBL267154 IC50 = 71.0 nM 7.15
CHEMBL9516 IC50 = 86.0 nM 7.07
CHEMBL9479 IC50 = 169.0 nM 6.77
CHEMBL9053 IC50 = 180.0 nM 6.75
CHEMBL276449 IC50 = 540.0 nM 6.27
CHEMBL9025 IC50 = 870.0 nM 6.06
CHEMBL2311124 IC50 > 1000.0 nM -
CHEMBL9121 IC50 > 1000.0 nM -
CHEMBL9531 IC50 > 1000.0 nM -
CHEMBL266808 IC50 > 1000.0 nM -
CHEMBL9490 IC50 > 1000.0 nM -
CHEMBL9341 IC50 > 1000.0 nM -