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Assay Detail

CHEMBL1640696

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

Binding
Inhibition of PDGFRbeta by flash plate based radioactive enzyme assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Platelet-derived growth factor receptor beta (CHEMBL1913)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel chimeric histone deacetylase inhibitors: a series of lapatinib hybrides as potent inhibitors of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and histone deacetylase activity.
Mahboobi S, Sellmer A, Winkler M, Eichhorn E, Pongratz H, Ciossek T, Baer T, Maier T, Beckers T.
J Med Chem (2010) 53 : 8546 -8555
PubMed 21080629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.57 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630117 1 6.00
CHEMBL1630108 1 5.96
CHEMBL1630118 1 5.75
CHEMBL1630110 1 5.64
CHEMBL1630112 1 5.64
CHEMBL1630109 1 5.60
CHEMBL1630114 1 5.60
CHEMBL1630115 1 5.57
CHEMBL1630107 1 5.48
CHEMBL1630113 1 5.41
CHEMBL1630111 1 5.40
CHEMBL1630116 1 5.33
CHEMBL554 LAPATINIB 4.0 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630117 IC50 = 1000.0 nM 6.00
CHEMBL1630108 IC50 = 1100.0 nM 5.96
CHEMBL1630118 IC50 = 1800.0 nM 5.75
CHEMBL1630110 IC50 = 2300.0 nM 5.64
CHEMBL1630112 IC50 = 2300.0 nM 5.64
CHEMBL1630109 IC50 = 2500.0 nM 5.60
CHEMBL1630114 IC50 = 2500.0 nM 5.60
CHEMBL1630115 IC50 = 2700.0 nM 5.57
CHEMBL1630107 IC50 = 3300.0 nM 5.48
CHEMBL1630113 IC50 = 3900.0 nM 5.41
CHEMBL1630111 IC50 = 4000.0 nM 5.40
CHEMBL1630116 IC50 = 4700.0 nM 5.33
CHEMBL554 LAPATINIB IC50 = 8500.0 nM 5.07