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Assay Detail

CHEMBL1018859

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

Functional
Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay
12
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type EOL1
Confidence 1 — Organism
Curated By Autocuration

Target

EOL1 (CHEMBL614489)
Type CELL-LINE
Organism Homo sapiens

Publication

Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.
Mahboobi S, Dove S, Sellmer A, Winkler M, Eichhorn E, Pongratz H, Ciossek T, Baer T, Maier T, Beckers T.
J Med Chem (2009) 52 : 2265 -2279
PubMed 19301902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL941 IMATINIB 4.0 2 9.70
CHEMBL473825 1 8.52
CHEMBL1080580 1 8.22
CHEMBL475820 1 8.15
CHEMBL514671 1 7.28
CHEMBL475796 2 7.00
CHEMBL514351 2 6.96
CHEMBL474863 1 6.92
CHEMBL98 VORINOSTAT 4.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL941 IMATINIB IC50 = 0.2 nM 9.70
CHEMBL941 IMATINIB IC50 = 0.1995 nM 9.70
CHEMBL473825 IC50 = 3.0 nM 8.52
CHEMBL1080580 IC50 = 6.0 nM 8.22
CHEMBL475820 IC50 = 7.0 nM 8.15
CHEMBL514671 IC50 = 53.0 nM 7.28
CHEMBL475796 IC50 = 100.0 nM 7.00
CHEMBL475796 IC50 = 100.0 nM 7.00
CHEMBL514351 IC50 = 110.0 nM 6.96
CHEMBL474863 IC50 = 120.0 nM 6.92
CHEMBL514351 IC50 = 125.89 nM 6.90
CHEMBL98 VORINOSTAT IC50 = 1000.0 nM 6.00