8EJB

Bruton's tyrosine kinase in complex with 3-{[4-(1-acetylpiperidin-4-yl)phenyl]amino}-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide

Summary for 8EJB

• Entry DOI: 10.2210/pdb8ejb/pdb
• Descriptor: Tyrosine-protein kinase BTK, 5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-3-[4-(piperidin-4-yl)anilino]pyrazine-2-carboxamide, 1,2-ETHANEDIOL, ... (6 entities in total)
• Functional Keywords: protein degradation, leukemia, transferase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 32255.81

Authors

Gajewski, S.,Clifton, M.C. (deposition date: 2022-09-16, release date: 2023-02-15, Last modification date: 2024-05-22)

• Primary citation: Zhang, D.,Harris, H.M.,Chen, J.,Judy, J.,James, G.,Kelly, A.,McIntosh, J.,Tenn-McClellan, A.,Ambing, E.,Tan, Y.S.,Lu, H.,Gajewski, S.,Clifton, M.C.,Yung, S.,Robbins, D.W.,Pirooznia, M.,Skanland, S.S.,Gaglione, E.,Mhibik, M.,Underbayev, C.,Ahn, I.E.,Sun, C.,Herman, S.E.M.,Noviski, M.,Wiestner, A.; NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts.; Blood, 141:1584-1596, 2023; PubMed: 36375120; DOI: 10.1182/blood.2022016934

Experimental method

X-RAY DIFFRACTION (1.58 Å)