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Assay Detail

CHEMBL4833900

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Functional
Antileishmanial activity against amastigote stage of Leishmania infantum MHOM/MA(BE)/67/ITMAP263 infected in mouse peritoneal macrophage assessed as reduction in parasite burden incubated for 5 days by Giemsa staining based microscopic analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Leishmania infantum (CHEMBL612848)
Type ORGANISM
Organism Leishmania infantum

Publication

DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Mowbray CE, Braillard S, Glossop PA, Whitlock GA, Jacobs RT, Speake J, Pandi B, Nare B, Maes L, Yardley V, Freund Y, Wall RJ, Carvalho S, Bello D, Van den Kerkhof M, Caljon G, Gilbert IH, Corpas-Lopez V, Lukac I, Patterson S, Zuccotto F, Wyllie S.
J Med Chem (2021) 64 : 16159 -16176
PubMed 34711050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 31 5.56 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4864912 1 6.30
CHEMBL4853379 1 6.30
CHEMBL4868645 1 6.23
CHEMBL4874617 1 6.22
CHEMBL4857581 1 6.19
CHEMBL4862187 1 6.10
CHEMBL4859733 1 5.89
CHEMBL4846846 1 5.89
CHEMBL4849214 1 5.85
CHEMBL4847520 1 5.80
CHEMBL4857278 1 5.80
CHEMBL4873099 1 5.77
CHEMBL4455345 1 5.77
CHEMBL4847418 1 5.75
CHEMBL4874673 1 5.75
CHEMBL4848737 1 5.70
CHEMBL4871287 1 5.68
CHEMBL4872513 1 5.66
CHEMBL2441392 1 5.57
CHEMBL4850767 1 5.52
CHEMBL4859032 1 5.51
CHEMBL4846571 1 5.24
CHEMBL4875612 1 5.24
CHEMBL4862021 1 5.19
CHEMBL125 MILTEFOSINE 4.0 1 5.00
CHEMBL4846529 1 4.85
CHEMBL4871532 1 4.80
CHEMBL4854414 1 4.47
CHEMBL4865994 1 4.43
CHEMBL4865151 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4864912 EC50 = 500.0 nM 6.30
CHEMBL4853379 EC50 = 500.0 nM 6.30
CHEMBL4868645 EC50 = 590.0 nM 6.23
CHEMBL4874617 EC50 = 600.0 nM 6.22
CHEMBL4857581 EC50 = 640.0 nM 6.19
CHEMBL4862187 EC50 = 800.0 nM 6.10
CHEMBL4859733 EC50 = 1300.0 nM 5.89
CHEMBL4846846 EC50 = 1300.0 nM 5.89
CHEMBL4849214 EC50 = 1400.0 nM 5.85
CHEMBL4847520 EC50 = 1600.0 nM 5.80
CHEMBL4857278 EC50 = 1600.0 nM 5.80
CHEMBL4873099 EC50 = 1700.0 nM 5.77
CHEMBL4455345 EC50 = 1700.0 nM 5.77
CHEMBL4847418 EC50 = 1800.0 nM 5.75
CHEMBL4874673 EC50 = 1800.0 nM 5.75
CHEMBL4848737 EC50 = 2000.0 nM 5.70
CHEMBL4871287 EC50 = 2100.0 nM 5.68
CHEMBL4872513 EC50 = 2200.0 nM 5.66
CHEMBL2441392 EC50 = 2700.0 nM 5.57
CHEMBL4850767 EC50 = 3000.0 nM 5.52
CHEMBL4859032 EC50 = 3100.0 nM 5.51
CHEMBL4846571 EC50 = 5700.0 nM 5.24
CHEMBL4875612 EC50 = 5700.0 nM 5.24
CHEMBL4862021 EC50 = 6400.0 nM 5.19
CHEMBL125 MILTEFOSINE EC50 = 10000.0 nM 5.00
CHEMBL4846529 EC50 = 14000.0 nM 4.85
CHEMBL4871532 EC50 = 16000.0 nM 4.80
CHEMBL4854414 EC50 = 34000.0 nM 4.47
CHEMBL4865994 EC50 = 37000.0 nM 4.43
CHEMBL4865151 EC50 = 38000.0 nM 4.42
CHEMBL2347704 ACOZIBOROLE EC50 > 64000.0 nM -