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Assay Detail

CHEMBL4231091

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

Functional
Anti-parasitic activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 after 48 hrs by resazurin-based assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.
Ebiloma GU, Ayuga TD, Balogun EO, Gil LA, Donachie A, Kaiser M, Herraiz T, Inaoka DK, Shiba T, Harada S, Kita K, de Koning HP, Dardonville C.
Eur J Med Chem (2018) 150 : 385 -402
PubMed 29544150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 30 5.87 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4249714 1 9.24
CHEMBL477683 PHENYLARSINE OXIDE 1 8.96
CHEMBL4245918 1 8.80
CHEMBL4250711 1 8.62
CHEMBL55 PENTAMIDINE 4.0 1 8.48
CHEMBL4244022 1 7.50
CHEMBL35241 DIMINAZENE 2.0 1 7.19
CHEMBL4247258 1 6.88
CHEMBL4237349 1 6.68
CHEMBL4237238 1 5.76
CHEMBL4240979 1 5.42
CHEMBL4247810 1 5.39
CHEMBL4239171 1 4.92
CHEMBL4090897 1 4.84
CHEMBL4248268 1 4.84
CHEMBL4250174 1 4.84
CHEMBL4237659 1 4.83
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID 1 4.77
CHEMBL4251018 1 4.75
CHEMBL4237726 1 4.75
CHEMBL4244828 1 4.57
CHEMBL4068891 1 4.50
CHEMBL4241091 1 4.48
CHEMBL309339 SALICYLHYDROXAMIC ACID 1 4.41
CHEMBL4245303 1 4.38
CHEMBL4069905 1 4.34
CHEMBL4241528 1 4.31
CHEMBL4243481 1 -
CHEMBL4249095 1 -
CHEMBL4241625 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4249714 EC50 = 0.58 nM 9.24
CHEMBL477683 PHENYLARSINE OXIDE EC50 = 1.1 nM 8.96
CHEMBL4245918 EC50 = 1.6 nM 8.80
CHEMBL4250711 EC50 = 2.4 nM 8.62
CHEMBL55 PENTAMIDINE EC50 = 3.3 nM 8.48
CHEMBL4244022 EC50 = 32.0 nM 7.50
CHEMBL35241 DIMINAZENE EC50 = 65.0 nM 7.19
CHEMBL4247258 EC50 = 133.0 nM 6.88
CHEMBL4237349 EC50 = 210.0 nM 6.68
CHEMBL4237238 EC50 = 1750.0 nM 5.76
CHEMBL4240979 EC50 = 3800.0 nM 5.42
CHEMBL4247810 EC50 = 4100.0 nM 5.39
CHEMBL4239171 EC50 = 11900.0 nM 4.92
CHEMBL4090897 EC50 = 14500.0 nM 4.84
CHEMBL4248268 EC50 = 14400.0 nM 4.84
CHEMBL4250174 EC50 = 14600.0 nM 4.84
CHEMBL4237659 EC50 = 14700.0 nM 4.83
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID EC50 = 17100.0 nM 4.77
CHEMBL4251018 EC50 = 17700.0 nM 4.75
CHEMBL4237726 EC50 = 17600.0 nM 4.75
CHEMBL4244828 EC50 = 26700.0 nM 4.57
CHEMBL4068891 EC50 = 31800.0 nM 4.50
CHEMBL4241091 EC50 = 32900.0 nM 4.48
CHEMBL309339 SALICYLHYDROXAMIC ACID EC50 = 38700.0 nM 4.41
CHEMBL4245303 EC50 = 42100.0 nM 4.38
CHEMBL4069905 EC50 = 45700.0 nM 4.34
CHEMBL4241528 EC50 = 49000.0 nM 4.31
CHEMBL4243481 EC50 = 400000.0 nM -
CHEMBL4249095 EC50 = 400000.0 nM -
CHEMBL4241625 EC50 = 400000.0 nM -