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Assay Detail

CHEMBL3406372

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

Functional
Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as decrease infected macrophages after 120 hrs by microscopy
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania donovani
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

Leishmania donovani (CHEMBL367)
Type ORGANISM
Organism Leishmania donovani

Publication

Antileishmanial pharmacomodulation in 8-nitroquinolin-2(1H)-one series.
Kieffer C, Cohen A, Verhaeghe P, Paloque L, Hutter S, Castera-Ducros C, Laget M, Rault S, Valentin A, Rathelot P, Azas N, Vanelle P.
Bioorg Med Chem (2015) 23 : 2377 -2386
PubMed 25846065 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.94 7.22
EC50 1 5.55 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3400772 1 7.22
CHEMBL267345 AMPHOTERICIN B 4.0 1 6.80
CHEMBL57004 SITAMAQUINE 2.0 1 6.00
CHEMBL1631694 FEXINIDAZOLE 4.0 1 5.55
CHEMBL2441910 1 5.26
CHEMBL2042573 1 5.19
CHEMBL125 MILTEFOSINE 4.0 1 5.17
CHEMBL3400788 1 -
CHEMBL3400790 1 -
CHEMBL55 PENTAMIDINE 4.0 1 -
CHEMBL190951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3400772 IC50 = 60.0 nM 7.22
CHEMBL267345 AMPHOTERICIN B IC50 = 160.0 nM 6.80
CHEMBL57004 SITAMAQUINE IC50 = 1000.0 nM 6.00
CHEMBL1631694 FEXINIDAZOLE EC50 = 2800.0 nM 5.55
CHEMBL2441910 IC50 = 5500.0 nM 5.26
CHEMBL2042573 IC50 = 6500.0 nM 5.19
CHEMBL125 MILTEFOSINE IC50 = 6800.0 nM 5.17
CHEMBL3400788 IC50 > 20000.0 nM -
CHEMBL3400790 IC50 > 15600.0 nM -
CHEMBL55 PENTAMIDINE IC50 > 20000.0 nM -
CHEMBL190951 IC50 = 1220000.0 nM -