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Assay Detail

CHEMBL4384229

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

Functional
Antiparasitic activity against Entamoeba histolytica HM-1:IMSS trophozoites after 24 to 48 hrs by CellTiter-Glo luminescent cell viability assay
77
Total Activities
50
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Entamoeba histolytica
Confidence 1 — Organism
Curated By Autocuration

Target

Entamoeba histolytica (CHEMBL612853)
Type ORGANISM
Organism Entamoeba histolytica

Publication

Design, Synthesis, and Biological Evaluation of 2-Nitroimidazopyrazin-one/-es with Antitubercular and Antiparasitic Activity.
Jarrad AM, Ang CW, Debnath A, Hahn HJ, Woods K, Tan L, Sykes ML, Jones AJ, Pelingon R, Butler MS, Avery VM, West NP, Karoli T, Blaskovich MAT, Cooper MA.
J Med Chem (2018) 61 : 11349 -11371
PubMed 30468386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 75 4.98 5.66
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3983955 1 5.66
CHEMBL4460588 1 5.66
CHEMBL3940020 1 5.66
CHEMBL4435915 1 5.66
CHEMBL3956327 1 5.66
CHEMBL137 METRONIDAZOLE 4.0 2 5.40
CHEMBL512244 2 5.30
CHEMBL4565179 1 5.11
CHEMBL4530876 2 5.04
CHEMBL227875 PRETOMANID 4.0 2 5.03
CHEMBL4459697 2 5.02
CHEMBL3956589 1 5.00
CHEMBL4580469 2 5.00
CHEMBL4579641 2 5.00
CHEMBL3920140 1 5.00
CHEMBL3957229 1 5.00
CHEMBL3985906 1 5.00
CHEMBL3947931 1 5.00
CHEMBL4469243 2 4.82
CHEMBL4563622 2 4.80
CHEMBL4447641 2 4.80
CHEMBL4453745 2 4.75
CHEMBL4516883 2 4.60
CHEMBL4453184 2 4.52
CHEMBL4453153 2 4.50
CHEMBL4435234 2 4.50
CHEMBL4548055 1 -
CHEMBL4562001 2 -
CHEMBL4557266 2 -
CHEMBL4468508 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3983955 IC50 = 2200.0 nM 5.66
CHEMBL3956327 IC50 = 2200.0 nM 5.66
CHEMBL4435915 IC50 = 2200.0 nM 5.66
CHEMBL4460588 IC50 = 2200.0 nM 5.66
CHEMBL3940020 IC50 = 2200.0 nM 5.66
CHEMBL137 METRONIDAZOLE IC50 = 3981.07 nM 5.40
CHEMBL137 METRONIDAZOLE IC50 = 4300.0 nM 5.37
CHEMBL512244 IC50 = 5011.87 nM 5.30
CHEMBL512244 IC50 = 5300.0 nM 5.28
CHEMBL4565179 IC50 = 7800.0 nM 5.11
CHEMBL4530876 IC50 = 9100.0 nM 5.04
CHEMBL227875 PRETOMANID IC50 = 9300.0 nM 5.03
CHEMBL4459697 IC50 = 9500.0 nM 5.02
CHEMBL4580469 IC50 = 10000.0 nM 5.00
CHEMBL3957229 IC50 = 10000.0 nM 5.00
CHEMBL3985906 IC50 = 10000.0 nM 5.00
CHEMBL3947931 IC50 = 10000.0 nM 5.00
CHEMBL3920140 IC50 = 10000.0 nM 5.00
CHEMBL3956589 IC50 = 10000.0 nM 5.00
CHEMBL4579641 IC50 = 10000.0 nM 5.00
CHEMBL4579641 IC50 = 10000.0 nM 5.00
CHEMBL4530876 IC50 = 10000.0 nM 5.00
CHEMBL227875 PRETOMANID IC50 = 10000.0 nM 5.00
CHEMBL4580469 IC50 = 10000.0 nM 5.00
CHEMBL4459697 IC50 = 10000.0 nM 5.00
CHEMBL4469243 IC50 = 15000.0 nM 4.82
CHEMBL4563622 IC50 = 15848.93 nM 4.80
CHEMBL4447641 IC50 = 15848.93 nM 4.80
CHEMBL4469243 IC50 = 15848.93 nM 4.80
CHEMBL4563622 IC50 = 16000.0 nM 4.80
CHEMBL4447641 IC50 = 17000.0 nM 4.77
CHEMBL4453745 IC50 = 18000.0 nM 4.75
CHEMBL4453745 IC50 = 19952.62 nM 4.70
CHEMBL4516883 IC50 = 25118.86 nM 4.60
CHEMBL4516883 IC50 = 27000.0 nM 4.57
CHEMBL4453184 IC50 = 30000.0 nM 4.52
CHEMBL4453153 IC50 = 31622.78 nM 4.50
CHEMBL4435234 IC50 = 31622.78 nM 4.50
CHEMBL4453184 IC50 = 31622.78 nM 4.50
CHEMBL4435234 IC50 = 33000.0 nM 4.48
CHEMBL4453153 IC50 = 34000.0 nM 4.47
CHEMBL4460422 Activity - -
CHEMBL3912869 IC50 > 25000.0 nM -
CHEMBL4473101 IC50 > 50000.0 nM -
CHEMBL4565041 Activity - -
CHEMBL4527225 IC50 > 50000.0 nM -
CHEMBL4527225 IC50 > 50118.72 nM -
CHEMBL4453399 IC50 > 50000.0 nM -
CHEMBL4467771 IC50 > 25000.0 nM -
CHEMBL4580019 IC50 > 50000.0 nM -