Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.

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Citation

Zeng H, Belanger DB, Curran PJ, Shipps GW Jr, Miao H, Bracken JB, Arshad Siddiqui M, Malkowski M, Wang Y

Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5870-5. doi: 10.1016/j.bmcl.2011.07.101. Epub 2011 Aug 3.

PubMed ID
21855335 [ View in PubMed
]
Abstract

A series of substituted imidazo[1,2-a]pyrazin-8-amines were discovered as novel breast tumor kinase (Brk)/protein tyrosine kinase 6 (PTK6) inhibitors. Tool compounds with low-nanomolar Brk inhibition activity, high selectivity towards other kinases and desirable DMPK properties were achieved to enable the exploration of Brk as an oncology target.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DasatinibTyrosine-protein kinase LckIC 50 (nM)3N/AN/ADetails