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Assay Detail

CHEMBL4773769

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Functional
Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP-263 axenic amastigotes assessed as inhibition of parasitic metabolic activity incubated for 48 hrs by steady Glow reagent based luminescence assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania infantum
Confidence 1 — Organism
Curated By Autocuration

Target

Leishmania infantum (CHEMBL612848)
Type ORGANISM
Organism Leishmania infantum

Publication

Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties.
Fersing C,Boudot C,Paoli-Lombardo R,Primas N,Pinault E,Hutter S,Castera-Ducros C,Kabri Y,Pedron J,Bourgeade-Delmas S,Sournia-Saquet A,Stigliani JL,Valentin A,Azqueta A,Muruzabal D,Destere A,Wyllie S,Fairlamb AH,Corvaisier S,Since M,Malzert-Fréon A,Di Giorgio C,Rathelot P,Azas N,Courtioux B,Vanelle P,Verhaeghe P
Eur J Med Chem (2020) 206 : 112668 -112668
PubMed 32795774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.33 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267345 AMPHOTERICIN B 4.0 1 7.22
CHEMBL125 MILTEFOSINE 4.0 1 6.10
CHEMBL4788930 1 6.10
CHEMBL4798187 1 6.05
CHEMBL4777198 1 5.80
CHEMBL1631694 FEXINIDAZOLE 4.0 1 5.47
CHEMBL4783344 1 5.30
CHEMBL4783634 1 5.10
CHEMBL4789978 1 4.99
CHEMBL4783616 1 4.80
CHEMBL4791191 1 4.75
CHEMBL4777308 1 4.49
CHEMBL4799356 1 4.33
CHEMBL4792432 1 4.11
CHEMBL4791331 1 -
CHEMBL4784988 1 -
CHEMBL4785404 1 -
CHEMBL4776584 1 -
CHEMBL4780635 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267345 AMPHOTERICIN B EC50 = 60.0 nM 7.22
CHEMBL125 MILTEFOSINE EC50 = 800.0 nM 6.10
CHEMBL4788930 EC50 = 800.0 nM 6.10
CHEMBL4798187 EC50 = 900.0 nM 6.05
CHEMBL4777198 EC50 = 1600.0 nM 5.80
CHEMBL1631694 FEXINIDAZOLE EC50 = 3400.0 nM 5.47
CHEMBL4783344 EC50 = 5000.0 nM 5.30
CHEMBL4783634 EC50 = 7900.0 nM 5.10
CHEMBL4789978 EC50 = 10300.0 nM 4.99
CHEMBL4783616 EC50 = 15900.0 nM 4.80
CHEMBL4791191 EC50 = 17800.0 nM 4.75
CHEMBL4777308 EC50 = 32100.0 nM 4.49
CHEMBL4799356 EC50 = 46300.0 nM 4.33
CHEMBL4792432 EC50 = 77800.0 nM 4.11
CHEMBL4791331 EC50 > 100000.0 nM -
CHEMBL4784988 EC50 > 3100.0 nM -
CHEMBL4785404 EC50 > 100000.0 nM -
CHEMBL4776584 EC50 > 25000.0 nM -
CHEMBL4780635 EC50 > 3100.0 nM -