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Assay Detail

CHEMBL3998913

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

Functional
Trypanocidal activity against bloodstream trypomastigote stage of wild-type Trypanosoma brucei brucei Lister 427 assessed as inhibition of respiration in presence of glycerol
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion.
Fueyo González FJ, Ebiloma GU, Izquierdo García C, Bruggeman V, Sánchez Villamañán JM, Donachie A, Balogun EO, Inaoka DK, Shiba T, Harada S, Kita K, de Koning HP, Dardonville C.
J Med Chem (2017) 60 : 1509 -1522
PubMed 28112515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.39 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098620 1 9.10
CHEMBL4099534 1 8.92
CHEMBL4072631 1 8.70
CHEMBL55 PENTAMIDINE 4.0 1 8.40
CHEMBL4061239 1 8.30
CHEMBL4080586 1 8.30
CHEMBL35241 DIMINAZENE 2.0 1 7.20
CHEMBL4086675 1 7.11
CHEMBL4083110 1 7.08
CHEMBL4104576 1 7.05
CHEMBL4078575 1 6.80
CHEMBL4096176 1 6.64
CHEMBL309339 SALICYLHYDROXAMIC ACID 1 5.16
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098620 EC50 = 0.8 nM 9.10
CHEMBL4099534 EC50 = 1.2 nM 8.92
CHEMBL4072631 EC50 = 2.0 nM 8.70
CHEMBL55 PENTAMIDINE EC50 = 4.0 nM 8.40
CHEMBL4061239 EC50 = 5.0 nM 8.30
CHEMBL4080586 EC50 = 5.0 nM 8.30
CHEMBL35241 DIMINAZENE EC50 = 63.0 nM 7.20
CHEMBL4086675 EC50 = 78.0 nM 7.11
CHEMBL4083110 EC50 = 84.0 nM 7.08
CHEMBL4104576 EC50 = 89.0 nM 7.05
CHEMBL4078575 EC50 = 158.0 nM 6.80
CHEMBL4096176 EC50 = 230.0 nM 6.64
CHEMBL309339 SALICYLHYDROXAMIC ACID EC50 = 7000.0 nM 5.16
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID EC50 = 19000.0 nM 4.72