3UGC
| Structural basis of Jak2 inhibition by the type II inhibtor NVP-BBT594 | Descriptor: | 5-{[6-(acetylamino)pyrimidin-4-yl]oxy}-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}-2,3-dihydro-1H-indole-1-carboxamide, MALONATE ION, Tyrosine-protein kinase JAK2 | Authors: | Scheufler, C, Tavares, G.A, Manley, P.W, Pissot-Soldermann, C, Kroemer, M. | Deposit date: | 2011-11-02 | Release date: | 2012-05-16 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.34 Å) | Cite: | Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent. Cancer Discov, 2, 2012
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3LPB
| Crystal structure of Jak2 complexed with a potent 2,8-diaryl-quinoxaline inhibitor | Descriptor: | N-methyl-4-[3-(3,4,5-trimethoxyphenyl)quinoxalin-5-yl]benzenesulfonamide, Tyrosine-protein kinase JAK2 | Authors: | Tavares, G.A, Pissot-Soldermann, C, Gerspacher, M, Furet, P, Kroemer, M. | Deposit date: | 2010-02-05 | Release date: | 2010-04-28 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors Bioorg.Med.Chem.Lett., 20, 2010
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