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Assay Detail

CHEMBL4056310

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

Functional
Antiprotozoal activity against Giardia intestinalis IMSS:0696:1 (genotype A) trophozoites incubated for 48 hrs
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Giardia intestinalis
Confidence 1 — Organism
Curated By Autocuration

Target

Giardia intestinalis (CHEMBL612652)
Type ORGANISM
Organism Giardia intestinalis

Publication

Synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-NSAID chimeras displaying broad antiprotozoal spectrum.
Colín-Lozano B, León-Rivera I, Chan-Bacab MJ, Ortega-Morales BO, Moo-Puc R, López-Guerrero V, Hernández-Núñez E, Argüello-Garcia R, Scior T, Barbosa-Cabrera E, Navarrete-Vázquez G.
Bioorg Med Chem Lett (2017) 27 : 3490 -3494
PubMed 28645659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.84 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4084390 1 6.84
CHEMBL4100836 1 6.83
CHEMBL4062705 1 6.76
CHEMBL4092145 1 6.66
CHEMBL4071348 1 6.64
CHEMBL1401 NITAZOXANIDE 4.0 1 5.92
CHEMBL55 PENTAMIDINE 4.0 1 5.39
CHEMBL137 METRONIDAZOLE 4.0 1 5.27
CHEMBL125 MILTEFOSINE 4.0 1 4.70
CHEMBL110 BENZNIDAZOLE 4.0 1 4.65
CHEMBL4065457 1 4.53
CHEMBL290960 NIFURTIMOX 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4084390 IC50 = 145.0 nM 6.84
CHEMBL4100836 IC50 = 147.0 nM 6.83
CHEMBL4062705 IC50 = 172.0 nM 6.76
CHEMBL4092145 IC50 = 221.0 nM 6.66
CHEMBL4071348 IC50 = 227.0 nM 6.64
CHEMBL1401 NITAZOXANIDE IC50 = 1214.0 nM 5.92
CHEMBL55 PENTAMIDINE IC50 = 4079.0 nM 5.39
CHEMBL137 METRONIDAZOLE IC50 = 5360.0 nM 5.27
CHEMBL125 MILTEFOSINE IC50 = 20000.0 nM 4.70
CHEMBL110 BENZNIDAZOLE IC50 = 22580.0 nM 4.65
CHEMBL4065457 IC50 = 29571.0 nM 4.53
CHEMBL290960 NIFURTIMOX IC50 - -