8E1X
FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29)
Summary for 8E1X
Entry DOI | 10.2210/pdb8e1x/pdb |
Descriptor | Fibroblast growth factor receptor 2, (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 (3 entities in total) |
Functional Keywords | fgfr, inhibitor, kinase, gatekeeper, hyperphosphatemia, structural protein |
Biological source | Homo sapiens (human) |
Total number of polymer chains | 2 |
Total formula weight | 76539.42 |
Authors | Lei, H.-T.,Epling, L.B.,Deller, M.C. (deposition date: 2022-08-11, release date: 2022-11-23, Last modification date: 2023-11-15) |
Primary citation | 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. Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3. J.Med.Chem., 65:15433-15442, 2022 Cited by PubMed: 36356320DOI: 10.1021/acs.jmedchem.2c01366 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.68 Å) |
Structure validation
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