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Assay Detail

CHEMBL4812134

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Functional
Antileishmanial activity against amastigote form of Leishmania infantum MHOM/MA(BE)/67 infected in Swiss mouse peritoneal macrophages assessed as reduction in parasite growth treated at 2 hrs post-infection and measured after 5 days by Giemsa staining based microscopic analysis
80
Total Activities
80
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

Revisiting Pyrazolo[3,4-<i>d</i>]pyrimidine Nucleosides as Anti-<i>Trypanosoma cruzi</i> and Antileishmanial Agents.
Bouton J, Ferreira de Almeida Fiuza L, Cardoso Santos C, Mazzarella MA, Soeiro MNC, Maes L, Karalic I, Caljon G, Van Calenbergh S.
J Med Chem (2021) 64 : 4206 -4238
PubMed 33784107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 80 5.01 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846834 1 7.10
CHEMBL388593 1 6.75
CHEMBL4853515 1 6.60
CHEMBL4573679 1 5.97
CHEMBL4879324 1 5.70
CHEMBL1467 ALLOPURINOL 4.0 1 5.46
CHEMBL1688966 1 5.18
CHEMBL4866769 1 5.17
CHEMBL125 MILTEFOSINE 4.0 1 5.13
CHEMBL4857392 1 5.10
CHEMBL4850284 1 5.09
CHEMBL4854628 1 4.98
CHEMBL4849951 1 4.90
CHEMBL4866244 1 4.65
CHEMBL4867373 1 4.62
CHEMBL4441282 1 4.59
CHEMBL4851843 1 4.59
CHEMBL4849515 1 4.53
CHEMBL4850814 1 4.50
CHEMBL4872012 1 4.49
CHEMBL4854614 1 4.49
CHEMBL4867530 1 4.37
CHEMBL4848328 1 4.31
CHEMBL4847325 1 4.29
CHEMBL4862547 1 4.29
CHEMBL4863097 1 4.28
CHEMBL4858079 1 4.24
CHEMBL4862065 1 -
CHEMBL4861891 1 -
CHEMBL4870347 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846834 IC50 = 80.0 nM 7.10
CHEMBL388593 IC50 = 180.0 nM 6.75
CHEMBL4853515 IC50 = 250.0 nM 6.60
CHEMBL4573679 IC50 = 1060.0 nM 5.97
CHEMBL4879324 IC50 = 2000.0 nM 5.70
CHEMBL1467 ALLOPURINOL IC50 = 3510.0 nM 5.46
CHEMBL1688966 IC50 = 6660.0 nM 5.18
CHEMBL4866769 IC50 = 6820.0 nM 5.17
CHEMBL125 MILTEFOSINE IC50 = 7470.0 nM 5.13
CHEMBL4857392 IC50 = 8000.0 nM 5.10
CHEMBL4850284 IC50 = 8110.0 nM 5.09
CHEMBL4854628 IC50 = 10400.0 nM 4.98
CHEMBL4849951 IC50 = 12700.0 nM 4.90
CHEMBL4866244 IC50 = 22600.0 nM 4.65
CHEMBL4867373 IC50 = 24100.0 nM 4.62
CHEMBL4441282 IC50 = 25400.0 nM 4.59
CHEMBL4851843 IC50 = 25400.0 nM 4.59
CHEMBL4849515 IC50 = 29400.0 nM 4.53
CHEMBL4850814 IC50 = 32000.0 nM 4.50
CHEMBL4872012 IC50 = 32700.0 nM 4.49
CHEMBL4854614 IC50 = 32500.0 nM 4.49
CHEMBL4867530 IC50 = 43100.0 nM 4.37
CHEMBL4848328 IC50 = 49400.0 nM 4.31
CHEMBL4847325 IC50 = 50800.0 nM 4.29
CHEMBL4862547 IC50 = 50800.0 nM 4.29
CHEMBL4863097 IC50 = 52800.0 nM 4.28
CHEMBL4858079 IC50 = 57000.0 nM 4.24
CHEMBL4859043 IC50 > 64000.0 nM -
CHEMBL4860137 IC50 > 64000.0 nM -
CHEMBL4870178 IC50 > 64000.0 nM -
CHEMBL4848830 IC50 > 64000.0 nM -
CHEMBL4871690 IC50 > 64000.0 nM -
CHEMBL4872365 IC50 > 64000.0 nM -
CHEMBL4872889 IC50 > 64000.0 nM -
CHEMBL4869192 IC50 > 64000.0 nM -
CHEMBL4846810 IC50 > 64000.0 nM -
CHEMBL4850164 IC50 > 64000.0 nM -
CHEMBL4853064 IC50 > 64000.0 nM -
CHEMBL4866226 IC50 > 64000.0 nM -
CHEMBL4854372 IC50 > 64000.0 nM -
CHEMBL4847088 IC50 > 64000.0 nM -
CHEMBL4848164 IC50 > 64000.0 nM -
CHEMBL4865117 IC50 > 64000.0 nM -
CHEMBL4870841 IC50 > 64000.0 nM -
CHEMBL4879116 IC50 > 64000.0 nM -
CHEMBL4862443 IC50 > 64000.0 nM -
CHEMBL4859940 IC50 > 64000.0 nM -
CHEMBL4870347 IC50 > 64000.0 nM -
CHEMBL4861891 IC50 >= 50800.0 nM -
CHEMBL4862065 IC50 > 64000.0 nM -