9TFA

PDGFRA-G680R mutant kinase domain in complex with a 6,7-dimethoxyquinazoline-based compound (43)

This is a non-PDB format compatible entry.

Summary for 9TFA

• Entry DOI: 10.2210/pdb9tfa/pdb
• Descriptor: Platelet-derived growth factor receptor alpha, (1~{S})-1-[2-[4-(6,7-dimethoxyquinazolin-4-yl)piperazin-1-yl]pyrimidin-5-yl]-1-(4-fluorophenyl)ethanamine (3 entities in total)
• Functional Keywords: pdgfra protein kinase, inhibitor, tyrosine kinase, transmembrane receptor, platelet-derived growth factor receptor alpha, pdgf, platelet-derived growth factor, gist, gastrointestinal stromal tumors, solvent-front mutant, p16234, transferase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 41075.30

Authors

Scrima, A.,Mueller, M.P.,Rauh, D. (deposition date: 2025-11-27, release date: 2026-07-15)

• Primary citation: Schulz, T.,Beerbaum, M.,Scrima, A.,Jantzen, H.,Teuber, A.,Muehlenberg, T.,Garcia-Fossa, F.,Weisner, J.,Mueller, M.P.,Sievers, S.,Bauer, S.,Rauh, D.; Structure-based Scaffold Hopping Reveals Strategies to Overcome Oncogenic KIT and PDGFRA Mutation-Driven Drug-Resistance in GIST; To Be Published,

Experimental method

X-RAY DIFFRACTION (2.2 Å)