Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.
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Swahn BM, Xue Y, Arzel E, Kallin E, Magnus A, Plobeck N, Viklund J
Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3.
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1397-401. Epub 2005 Dec 5.
- PubMed ID
- 16337120 [ View in PubMed]
- Abstract
The design and synthesis of a new series of c-Jun N-terminal kinase-3 (JNK3) inhibitors with selectivity against JNK1 are reported. The novel series of substituted 2'-anilino-4,4'-bipyridines were designed based on a combination of hits from high throughput screening and X-ray crystal structure information of compounds crystallized into the JNK3 ATP binding active site.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) N-{2'-[(4-FLUOROPHENYL)AMINO]-4,4'-BIPYRIDIN-2-YL}-4-METHOXYCYCLOHEXANECARBOXAMIDE Mitogen-activated protein kinase 10 IC 50 (nM) 235 N/A N/A Details