| Structural highlights
4px6 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: |
| | Activity: | Non-specific protein-tyrosine kinase, with EC number 2.7.10.2 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
We describe two series of Syk inhibitors which potently abrogate Syk kinase function in enzymatic assays, cellular assays and in primary cells in the presence of blood. Introduction of a 7-aminoindole substituent led to derivatives with good kinase selectivity and little or no hERG channel inhibition (3b, 10c).
Syk inhibitors with high potency in presence of blood.,Thoma G, Blanz J, Buhlmayer P, Druckes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H Bioorg Med Chem Lett. 2014 Apr 3. pii: S0960-894X(14)00302-3. doi:, 10.1016/j.bmcl.2014.03.075. PMID:24726806[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Thoma G, Blanz J, Buhlmayer P, Druckes P, Kittelmann M, Smith AB, van Eis M, Vangrevelinghe E, Zerwes HG, Che JJ, He X, Jin Y, Lee CC, Michellys PY, Uno T, Liu H. Syk inhibitors with high potency in presence of blood. Bioorg Med Chem Lett. 2014 Apr 3. pii: S0960-894X(14)00302-3. doi:, 10.1016/j.bmcl.2014.03.075. PMID:24726806 doi:http://dx.doi.org/10.1016/j.bmcl.2014.03.075
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