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Assay Detail

CHEMBL4773767

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

Functional
Antileishmanial activity against Leishmania donovani MHOM/IN/00/DEVI promastigotes assessed as inhibition of parasitic metabolic activity measured after 72 hrs by MTT assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Leishmania donovani (CHEMBL367)
Type ORGANISM
Organism Leishmania donovani

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 23 5.72 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267345 AMPHOTERICIN B 4.0 1 7.16
CHEMBL4788930 1 6.30
CHEMBL4798187 1 6.16
CHEMBL4792432 1 6.10
CHEMBL4785404 1 6.05
CHEMBL1631694 FEXINIDAZOLE 4.0 1 5.92
CHEMBL4789978 1 5.92
CHEMBL4797467 1 5.72
CHEMBL4777198 1 5.72
CHEMBL4793961 1 5.60
CHEMBL4783344 1 5.58
CHEMBL125 MILTEFOSINE 4.0 1 5.51
CHEMBL4783634 1 5.40
CHEMBL4784988 1 5.25
CHEMBL4776584 1 5.24
CHEMBL4780635 1 5.21
CHEMBL4781188 1 5.13
CHEMBL4783616 1 5.03
CHEMBL4780577 1 -
CHEMBL4791191 1 -
CHEMBL4799356 1 -
CHEMBL4777308 1 -
CHEMBL4791331 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267345 AMPHOTERICIN B EC50 = 70.0 nM 7.16
CHEMBL4788930 EC50 = 500.0 nM 6.30
CHEMBL4798187 EC50 = 700.0 nM 6.16
CHEMBL4792432 EC50 = 800.0 nM 6.10
CHEMBL4785404 EC50 = 900.0 nM 6.05
CHEMBL1631694 FEXINIDAZOLE EC50 = 1200.0 nM 5.92
CHEMBL4789978 EC50 = 1200.0 nM 5.92
CHEMBL4797467 EC50 = 1900.0 nM 5.72
CHEMBL4777198 EC50 = 1900.0 nM 5.72
CHEMBL4793961 EC50 = 2500.0 nM 5.60
CHEMBL4783344 EC50 = 2600.0 nM 5.58
CHEMBL125 MILTEFOSINE EC50 = 3100.0 nM 5.51
CHEMBL4783634 EC50 = 4000.0 nM 5.40
CHEMBL4784988 EC50 = 5600.0 nM 5.25
CHEMBL4776584 EC50 = 5700.0 nM 5.24
CHEMBL4780635 EC50 = 6200.0 nM 5.21
CHEMBL4781188 EC50 = 7400.0 nM 5.13
CHEMBL4783616 EC50 = 9300.0 nM 5.03
CHEMBL4780577 EC50 > 12500.0 nM -
CHEMBL4791191 EC50 > 12500.0 nM -
CHEMBL4799356 EC50 > 12500.0 nM -
CHEMBL4777308 EC50 > 12500.0 nM -
CHEMBL4791331 EC50 > 12500.0 nM -