7DHL

Crystal structure of FGFR3 in complex with pyrimidine derivative

Summary for 7DHL

Entry DOI	10.2210/pdb7dhl/pdb
Descriptor	Fibroblast growth factor receptor 3, 5-[2-(3,5-dimethoxyphenyl)ethyl]-N-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidin-2-amine (3 entities in total)
Functional Keywords	protein kinase, signaling protein, transferase
Biological source	Homo sapiens (Human)
Total number of polymer chains	1
Total formula weight	36211.44
Authors	Echizen, Y.,Tateishi, Y.,Amano, Y. (deposition date: 2020-11-16, release date: 2021-02-03, Last modification date: 2023-11-29)
Primary citation	Kuriwaki, I.,Kameda, M.,Iikubo, K.,Hisamichi, H.,Kawamoto, Y.,Kikuchi, S.,Moritomo, H.,Kondoh, Y.,Terasaka, T.,Amano, Y.,Tateishi, Y.,Echizen, Y.,Iwai, Y.,Noda, A.,Tomiyama, H.,Nakazawa, T.,Hirano, M. Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency. Bioorg.Med.Chem., 33:116019-116019, 2021 Cited by PubMed: 33486159 DOI: 10.1016/j.bmc.2021.116019 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.57 Å)

Structure validation