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Assay Detail

CHEMBL4340263

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi Y trypomastigotes infected in LLC-MK2-ATCC CCL7 cells assessed as reduction in parasite growth incubated for 24 hrs by Alamar blue dye based assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Structure-activity relationship study of antitrypanosomal chalcone derivatives using multivariate analysis.
Gomes KS, da Costa-Silva TA, Oliveira IH, Aguilar AM, Oliveira-Silva D, Uemi M, Silva WA, Melo LR, Andrade CKZ, Tempone AG, Tempone AG, Baldim JL, Lago JHG.
Bioorg Med Chem Lett (2019) 29 : 1459 -1462
PubMed 31000155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 37 4.63 5.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2237021 1 5.48
CHEMBL4460391 1 4.97
CHEMBL286151 1 4.86
CHEMBL110 BENZNIDAZOLE 4.0 1 4.78
CHEMBL61592 1 4.74
CHEMBL4544160 1 4.72
CHEMBL2282149 1 4.58
CHEMBL4556196 1 4.58
CHEMBL7976 CHALCONE 1 4.57
CHEMBL4585757 1 4.55
CHEMBL32147 2'-HYDROXYCHALCONE 1 4.54
CHEMBL4594015 1 4.54
CHEMBL227747 1 4.22
CHEMBL227400 1 4.21
CHEMBL390381 1 4.13
CHEMBL499801 1 -
CHEMBL244458 1 -
CHEMBL2237020 1 -
CHEMBL489719 1 -
CHEMBL455453 1 -
CHEMBL490143 DIHYDROCHALCONE 1 -
CHEMBL4443589 1 -
CHEMBL4436635 1 -
CHEMBL4435072 1 -
CHEMBL4546900 1 -
CHEMBL4521741 1 -
CHEMBL4589355 1 -
CHEMBL4576755 1 -
CHEMBL4522833 1 -
CHEMBL2012143 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2237021 EC50 = 3300.0 nM 5.48
CHEMBL4460391 EC50 = 10600.0 nM 4.97
CHEMBL286151 EC50 = 13900.0 nM 4.86
CHEMBL110 BENZNIDAZOLE EC50 = 16500.0 nM 4.78
CHEMBL61592 EC50 = 18400.0 nM 4.74
CHEMBL4544160 EC50 = 18900.0 nM 4.72
CHEMBL2282149 EC50 = 26000.0 nM 4.58
CHEMBL4556196 EC50 = 26500.0 nM 4.58
CHEMBL7976 CHALCONE EC50 = 26900.0 nM 4.57
CHEMBL4585757 EC50 = 28300.0 nM 4.55
CHEMBL4594015 EC50 = 28600.0 nM 4.54
CHEMBL32147 2'-HYDROXYCHALCONE EC50 = 28800.0 nM 4.54
CHEMBL227747 EC50 = 60000.0 nM 4.22
CHEMBL227400 EC50 = 60900.0 nM 4.21
CHEMBL390381 EC50 = 73200.0 nM 4.13
CHEMBL34398 4'-METHOXYCHALCONE EC50 > 100000.0 nM -
CHEMBL2237025 EC50 > 100000.0 nM -
CHEMBL142840 EC50 > 100000.0 nM -
CHEMBL242946 EC50 > 100000.0 nM -
CHEMBL2236854 EC50 > 100000.0 nM -
CHEMBL224690 EC50 > 100000.0 nM -
CHEMBL2237017 EC50 > 100000.0 nM -
CHEMBL499801 EC50 > 100000.0 nM -
CHEMBL244458 EC50 > 100000.0 nM -
CHEMBL2237020 EC50 > 100000.0 nM -
CHEMBL489719 EC50 > 100000.0 nM -
CHEMBL455453 EC50 > 100000.0 nM -
CHEMBL490143 DIHYDROCHALCONE EC50 > 100000.0 nM -
CHEMBL4443589 EC50 > 100000.0 nM -
CHEMBL4436635 EC50 > 100000.0 nM -
CHEMBL4435072 EC50 > 100000.0 nM -
CHEMBL4546900 EC50 > 100000.0 nM -
CHEMBL4521741 EC50 > 100000.0 nM -
CHEMBL4589355 EC50 > 100000.0 nM -
CHEMBL4576755 EC50 > 100000.0 nM -
CHEMBL4522833 EC50 > 100000.0 nM -
CHEMBL2012143 EC50 > 100000.0 nM -