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Assay Detail

CHEMBL4362340

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

Functional
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-87MG ATCC
Confidence 1 — Organism
Curated By Autocuration

Target

U-87 MG (CHEMBL614247)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
Jovanović M, Zhukovsky D, Podolski-Renić A, Domračeva I, Žalubovskis R, Senćanski M, Glišić S, Sharoyko V, Tennikova T, Dar'in D, Pešić M, Krasavin M.
Eur J Med Chem (2019) 181 : 111580 -111580
PubMed 31400708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.54 6.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4577957 1 6.34
CHEMBL4562297 1 6.10
CHEMBL4451049 1 5.85
CHEMBL4589636 1 5.54
CHEMBL465843 PIPLARTINE 1 5.14
CHEMBL4459518 1 5.01
CHEMBL4452177 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4577957 IC50 = 460.0 nM 6.34
CHEMBL4562297 IC50 = 800.0 nM 6.10
CHEMBL4451049 IC50 = 1410.0 nM 5.85
CHEMBL4589636 IC50 = 2920.0 nM 5.54
CHEMBL465843 PIPLARTINE IC50 = 7180.0 nM 5.14
CHEMBL4459518 IC50 = 9700.0 nM 5.01
CHEMBL4452177 IC50 = 15190.0 nM 4.82