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Assay Detail

CHEMBL4155548

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

Functional
Antileishmanial activity against amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as inhibition of parasite infection after 120 hrs by Giemsa staining-based microscopic method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania donovani
Confidence 1 — Organism
Curated By Intermediate

Target

Leishmania donovani (CHEMBL367)
Type ORGANISM
Organism Leishmania donovani

Publication

Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
Pedron J, Boudot C, Hutter S, Bourgeade-Delmas S, Stigliani JL, Sournia-Saquet A, Moreau A, Boutet-Robinet E, Paloque L, Mothes E, Laget M, Vendier L, Pratviel G, Wyllie S, Fairlamb A, Azas N, Courtioux B, Valentin A, Verhaeghe P.
Eur J Med Chem (2018) 155 : 135 -152
PubMed 29885575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.47 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267345 AMPHOTERICIN B 4.0 1 6.40
CHEMBL125 MILTEFOSINE 4.0 1 5.27
CHEMBL4170207 1 4.75
CHEMBL1631694 FEXINIDAZOLE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267345 AMPHOTERICIN B IC50 = 400.0 nM 6.40
CHEMBL125 MILTEFOSINE IC50 = 5400.0 nM 5.27
CHEMBL4170207 IC50 = 18000.0 nM 4.75
CHEMBL1631694 FEXINIDAZOLE IC50 > 50000.0 nM -