Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Article Details
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Ballard P, Bradbury RH, Harris CS, Hennequin LF, Hickinson M, Kettle JG, Kendrew J, Klinowska T, Ogilvie DJ, Pearson SE, Williams EJ, Wilson I
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Bioorg Med Chem Lett. 2006 Sep 15;16(18):4908-12. Epub 2006 Jun 27.
- PubMed ID
- 16806916 [ View in PubMed]
- Abstract
The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated. Strategies to lower volume of distribution and shorten half-life through structure and pKa modulation are discussed.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Gefitinib Epidermal growth factor receptor IC 50 (nM) 23 N/A N/A Details