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Title | Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, Part I: Transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors. |
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Journal, issue, pages | Bioorg. Med. Chem. Lett., Vol. 23, Page 3438-3442, Year 2013 |
Publish date | Mar 5, 2013 (structure data deposition date) |
Authors | Plummer, M.S. / Cornicelli, J. / Roark, H. / Skalitzky, D.J. / Stankovic, C.J. / Bove, S. / Pandit, J. / Goodman, A. / Hicks, J. / Shahripour, A. ...Plummer, M.S. / Cornicelli, J. / Roark, H. / Skalitzky, D.J. / Stankovic, C.J. / Bove, S. / Pandit, J. / Goodman, A. / Hicks, J. / Shahripour, A. / Beidler, D. / Lu, X.K. / Sanchez, B. / Whitehead, C. / Sarver, R. / Braden, T. / Gowan, R. / Shen, X.Q. / Welch, K. / Ogden, A. / Sadagopan, N. / Baum, H. / Miller, H. / Banotai, C. / Spessard, C. / Lightle, S. |
External links | Bioorg. Med. Chem. Lett. / PubMed:23582272 |
Methods | X-ray diffraction |
Resolution | 1.72 Å |
Structure data | PDB-4jib: |
Chemicals | ChemComp-ZN: ChemComp-MG: ChemComp-1L6: ChemComp-HOH: |
Source |
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Keywords | HYDROLASE/HYDROLASE INHIBITOR / HYDROLASE-HYDROLASE INHIBITOR complex |