4AGW
Discovery of a small molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases
Summary for 4AGW
Entry DOI | 10.2210/pdb4agw/pdb |
Related | 1F1W 1F2F 1NLO 1NLP 1P13 1PRL 1PRM 1RLP 1RLQ 1SRL 1SRM 2PTK |
Descriptor | PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC, 3-{2-[(cyclopropylcarbonyl)amino][1,3]thiazolo[5,4-b]pyridin-5-yl}-N-{4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromet hyl)phenyl}benzamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... (5 entities in total) |
Functional Keywords | atp-binding, lipoprotein, myristate, phosphoprotein, sh2 domain, sh3 domain, transferase |
Biological source | GALLUS GALLUS |
Total number of polymer chains | 2 |
Total formula weight | 67153.21 |
Authors | Weisberg, E.,Choi, H.G.,Seeliger, M.,Gray, N.,Griffin, J.D. (deposition date: 2012-02-01, release date: 2012-02-15, Last modification date: 2024-05-08) |
Primary citation | Weisberg, E.,Choi, H.G.,Ray, A.,Barrett, R.,Zhang, J.,Sim, T.,Zhou, W.,Seeliger, M.,Cameron, M.,Azam, M.,Fletcher, J.A.,Debiec-Rychter, M.,Mayeda, M.,Moreno, D.,Kung, A.L.,Janne, P.A.,Khosravi-Far, R.,Melo, J.V.,Manley, P.W.,Adamia, S.,Wu, C.,Gray, N.,Griffin, J.D. Discovery of a Small-Molecule Type II Inhibitor of Wild-Type and Gatekeeper Mutants of Bcr-Abl, Pdgfralpha, Kit, and Src Kinases: Novel Type II Inhibitor of Gatekeeper Mutants. Blood, 115:4206-, 2010 Cited by PubMed: 20299508DOI: 10.1182/BLOOD-2009-11-251751 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.6 Å) |
Structure validation
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