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Assay Detail

CHEMBL897089

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Functional
Antiproliferative activity against Trypanosoma brucei
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity.
Martyn DC, Jones DC, Fairlamb AH, Clardy J.
Bioorg Med Chem Lett (2007) 17 : 1280 -1283
PubMed 17197182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.01 6.82
IC50 1 8.34 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55 PENTAMIDINE 4.0 1 8.34
CHEMBL233348 1 6.82
CHEMBL535173 1 6.26
CHEMBL537483 1 6.17
CHEMBL233549 1 6.09
CHEMBL233339 1 6.02
CHEMBL392238 1 6.02
CHEMBL234180 1 6.01
CHEMBL536752 1 6.00
CHEMBL233347 1 6.00
CHEMBL231735 1 5.78
CHEMBL538585 1 5.52
CHEMBL395223 1 5.48
CHEMBL55756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55 PENTAMIDINE IC50 = 4.6 nM 8.34
CHEMBL233348 EC50 = 150.0 nM 6.82
CHEMBL535173 EC50 = 550.0 nM 6.26
CHEMBL537483 EC50 = 680.0 nM 6.17
CHEMBL233549 EC50 = 820.0 nM 6.09
CHEMBL233339 EC50 = 960.0 nM 6.02
CHEMBL392238 EC50 = 950.0 nM 6.02
CHEMBL234180 EC50 = 980.0 nM 6.01
CHEMBL536752 EC50 = 1000.0 nM 6.00
CHEMBL233347 EC50 = 1010.0 nM 6.00
CHEMBL231735 EC50 = 1650.0 nM 5.78
CHEMBL538585 EC50 = 3010.0 nM 5.52
CHEMBL395223 EC50 = 3300.0 nM 5.48
CHEMBL55756 EC50 > 50000.0 nM -