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: 36356320 DOI: 10.1021/acs.jmedchem.2c01366 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.68 Å)

Structure validation