4o6e

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine Inhibitors of Erk2Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine Inhibitors of Erk2

Structural highlights

4o6e is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:
Activity:	Mitogen-activated protein kinase, with EC number 2.7.11.24
Resources:	FirstGlance, OCA, RCSB, PDBsum

Publication Abstract from PubMed

The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.,Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068., Epub 2014 Apr 29. PMID:24813737^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB. Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068., Epub 2014 Apr 29. PMID:24813737 doi:http://dx.doi.org/10.1016/j.bmcl.2014.04.068

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

[1] Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB. Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068., Epub 2014 Apr 29. PMID:24813737 doi:http://dx.doi.org/10.1016/j.bmcl.2014.04.068

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