Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
GefitinibEpidermal growth factor receptorIC 50 (nM)23N/AN/ADetails