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Assay Detail

CHEMBL3998916

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

Binding
Inhibition of recombinant MTS-deficient N-terminal His6-tagged and SUMO-tagged Trypanosoma alternative oxidase expressed in Escherichia coli FN102 using ubiquinol-1 as substrate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 7 5.65 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086675 1 5.87
CHEMBL4098620 1 5.84
CHEMBL309339 SALICYLHYDROXAMIC ACID 1 5.23
CHEMBL4080586 1 -
CHEMBL4096176 1 -
CHEMBL4104576 1 -
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086675 IC50 = 1360.0 nM 5.87
CHEMBL4098620 IC50 = 1460.0 nM 5.84
CHEMBL309339 SALICYLHYDROXAMIC ACID IC50 = 5930.0 nM 5.23
CHEMBL4080586 IC50 > 5000.0 nM -
CHEMBL4096176 IC50 > 5000.0 nM -
CHEMBL4104576 IC50 > 5000.0 nM -
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID IC50 = 116000.0 nM -