9GI9

Wildtype EGFR bound with (R)-3-((3-chloro-2-methoxyphenyl)amino)-2-(3-((tetrahydrofuran-2-yl)methoxy)pyridin-4-yl)-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one

This is a non-PDB format compatible entry.

Summary for 9GI9

• Entry DOI: 10.2210/pdb9gi9/pdb
• Related: 9FQP 9FQS 9FRD
• Descriptor: Epidermal growth factor receptor, 3-[(3-chloranyl-2-methoxy-phenyl)amino]-2-[3-[[(2~{R})-oxolan-2-yl]methoxy]pyridin-4-yl]-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one (2 entities in total)
• Functional Keywords: kinase, egfr wildtype, oncoprotein
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 38048.39

Authors

Pagliarini, R.A.,Henderson, J.A.,Borrelli, D.R.,Brooijmans, N.,Hilbert, B.J.,Huff, M.R.,Ito, T.,Kryukov, G.V.,Ladd, B.,Martin, B.R.,Milgram, B.C.,Motiwala, H.,OHearn, E.,Wang, W.,Hata, A.,Bellier, J.,Kuzmic, P.,Guzman-Perez, A.,Jackson, E.L.,Stuart, D.D. (deposition date: 2024-08-18, release date: 2025-05-14)

• Primary citation: Pagliarini, R.A.,Henderson, J.A.,Borrelli, D.R.,Brooijmans, N.,Hilbert, B.J.,Huff, M.R.,Ito, T.,Kryukov, G.V.,Ladd, B.,Martin, B.R.,Milgram, B.C.,Motiwala, H.,OHearn, E.,Wang, W.,Hata, A.,Bellier, J.,Kuzmic, P.,Guzman-Perez, A.,Jackson, E.L.,Stuart, D.D.; STX-721, a covalent EGFR/HER2 exon 20 inhibitor, takes advantage of exon 20 mutant dynamic protein states and achieves unique mutant-selectivity across human cancer models; To be published,

Experimental method

X-RAY DIFFRACTION (3.12 Å)