Discovery of novel imidazo[1,2-a]pyrazin-8-amines as Brk/PTK6 inhibitors.
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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.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Dasatinib Tyrosine-protein kinase Lck IC 50 (nM) 3 N/A N/A Details