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TitleDiscovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Journal, issue, pagesJ. Med. Chem., Vol. 65, Page 15433-15442, Year 2022
Publish dateAug 11, 2022 (structure data deposition date)
AuthorsShvartsbart, A. / Roach, J.J. / Witten, M.R. / Koblish, H. / Harris, J.J. / Covington, M. / Hess, R. / Lin, L. / Frascella, M. / Truong, L. ...Shvartsbart, A. / Roach, J.J. / Witten, M.R. / Koblish, H. / Harris, J.J. / Covington, M. / Hess, R. / Lin, L. / Frascella, M. / Truong, L. / Leffet, L. / Conlen, P. / Beshad, E. / Klabe, R. / Katiyar, K. / Kaldon, L. / Young-Sciame, R. / He, X. / Petusky, S. / Chen, K.J. / Horsey, A. / Lei, H.T. / Epling, L.B. / Deller, M.C. / Vechorkin, O. / Yao, W.
External linksJ. Med. Chem. / PubMed:36356320
MethodsX-ray diffraction
Resolution2.68 Å
Structure data

PDB-8e1x:
FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29)
Method: X-RAY DIFFRACTION / Resolution: 2.68 Å

Chemicals

ChemComp-U9P:
(5M)-N-methyl-5-{(6M,8S)-5-{[(3S)-oxolan-3-yl]amino}-6-[1-(propan-2-yl)-1H-pyrazol-3-yl]pyrazolo[1,5-a]pyrimidin-3-yl}pyridine-3-carboxamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsSTRUCTURAL PROTEIN / FGFR / inhibitor / kinase / gatekeeper / hyperphosphatemia

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