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| Title | Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development. |
|---|---|
| Journal, issue, pages | J. Med. Chem., Vol. 59, Page 5650-5660, Year 2016 |
| Publish date | May 20, 2016 (structure data deposition date) |
Authors | Blake, J.F. / Burkard, M. / Chan, J. / Chen, H. / Chou, K.J. / Diaz, D. / Dudley, D.A. / Gaudino, J.J. / Gould, S.E. / Grina, J. ...Blake, J.F. / Burkard, M. / Chan, J. / Chen, H. / Chou, K.J. / Diaz, D. / Dudley, D.A. / Gaudino, J.J. / Gould, S.E. / Grina, J. / Hunsaker, T. / Liu, L. / Martinson, M. / Moreno, D. / Mueller, L. / Orr, C. / Pacheco, P. / Qin, A. / Rasor, K. / Ren, L. / Robarge, K. / Shahidi-Latham, S. / Stults, J. / Sullivan, F. / Wang, W. / Yin, J. / Zhou, A. / Belvin, M. / Merchant, M. / Moffat, J. / Schwarz, J.B. |
External links | J. Med. Chem. / PubMed:27227380 |
| Methods | X-ray diffraction |
| Resolution | 1.6 - 1.76 Å |
| Structure data | ![]() PDB-5k4i: ![]() PDB-5k4j: |
| Chemicals | ![]() ChemComp-6QB: ![]() ChemComp-EDO: ![]() ChemComp-HOH: |
| Source |
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Keywords | TRANSFERASE/TRANSFERASE INHIBITOR / protein Kinase / TRANSFERASE-TRANSFERASE INHIBITOR complex |
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homo sapiens (human)
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