Summary for 9DF4
| Entry DOI | 10.2210/pdb9df4/pdb |
| Descriptor | Epidermal growth factor receptor, (2P)-3-(3-chloro-2-methoxyanilino)-2-[3-({(2R)-1-[(2E)-4-(dimethylamino)but-2-enoyl]-2-methylpyrrolidin-2-yl}ethynyl)pyridin-4-yl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one, CHLORIDE ION, ... (6 entities in total) |
| Functional Keywords | kinase, inhibitor, oncoprotein, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 1 |
| Total formula weight | 40073.15 |
| Authors | Hilbert, B.J.,Brooijmans, N.,Pagliarini, R.A.,Milgram, B.C. (deposition date: 2024-08-29, 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.,Ladd, B.,Martin, B.,Milgram, B.C.,Motiwala, H.,OHearn, E.,Wang, W.,Hata, A.,Bellier, J.,Kuzmic, P.,Guzman-Perez, A.,Jackson, E.L.,Stuart, 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 (1.78 Å) |
Structure validation
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