3VHK
| Crystal structure of the VEGFR2 kinase domain in complex with a back pocket binder | Descriptor: | 1,2-ETHANEDIOL, Vascular endothelial growth factor receptor 2, {3-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methoxy]phenyl}methanol | Authors: | Iwata, H, Oki, H, Okada, K, Takagi, T, Tawada, M, Miyazaki, Y, Imamura, S, Hori, A, Hixon, M.S, Kimura, H, Miki, H. | Deposit date: | 2011-08-25 | Release date: | 2012-09-05 | Last modified: | 2024-03-20 | Method: | X-RAY DIFFRACTION (2.49 Å) | Cite: | A Back-to-Front Fragment-Based Drug Design Search Strategy Targeting the DFG-Out Pocket of Protein Tyrosine Kinases. ACS MED.CHEM.LETT., 3, 2012
|
|
3VID
| Crystal structure of human VEGFR2 kinase domain with Compound A. | Descriptor: | 4,5,6,11-tetrahydro-1H-pyrazolo[4',3':6,7]cyclohepta[1,2-b]indole, Vascular endothelial growth factor receptor 2 | Authors: | Iwata, H, Oki, H, Okada, K, Takagi, T, Tawada, M, Miyazaki, Y, Imamura, S, Hori, A, Hixon, M.S, Kimura, H, Miki, H. | Deposit date: | 2011-09-29 | Release date: | 2012-08-15 | Last modified: | 2024-03-20 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | A Back-to-Front Fragment-Based Drug Design Search Strategy Targeting the DFG-Out Pocket of Protein Tyrosine Kinases. ACS MED.CHEM.LETT., 3, 2012
|
|
6UBW
| MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody | Descriptor: | CHLORIDE ION, Hepatocyte growth factor receptor, N-(6-{difluoro[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-a]pyridin-3-yl]methyl}imidazo[1,2-b]pyridazin-2-yl)cyclopropanecarboxamide | Authors: | Hoffman, I.D, Lawson, J.D. | Deposit date: | 2019-09-13 | Release date: | 2020-02-12 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody. Mol.Cancer Ther., 16, 2017
|
|
8SU8
| |
8T7V
| |
8T09
| |
4P58
| Crystal structure of mouse comt bound to an inhibitor | Descriptor: | 1',3'-dimethyl-1H,1'H-3,4'-bipyrazole, Catechol O-methyltransferase | Authors: | Lanier, M. | Deposit date: | 2014-03-15 | Release date: | 2014-06-25 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.06 Å) | Cite: | A fragment-based approach to identifying S-adenosyl-l-methionine -competitive inhibitors of catechol O-methyl transferase (COMT). J.Med.Chem., 57, 2014
|
|
5INH
| Crystal structure of Autotaxin/ENPP2 with a covalent fragment | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ACETATE ION, ... | Authors: | Klein, M.G, Tjhen, R. | Deposit date: | 2016-03-07 | Release date: | 2017-03-15 | Last modified: | 2020-07-29 | Method: | X-RAY DIFFRACTION (1.84 Å) | Cite: | Repurposing Suzuki Coupling Reagents as a Directed Fragment Library Targeting Serine Hydrolases and Related Enzymes. J. Med. Chem., 60, 2017
|
|
2IMA
| |
2ILP
| |
2IMC
| |
2IMB
| |
5UAB
| |
5UAD
| |
5USQ
| ALK-5 kinase inhibitor complex | Descriptor: | N-[2-(5-chloro-2-fluorophenyl)pyridin-4-yl]-2-[(piperidin-4-yl)methyl]-2H-pyrazolo[4,3-b]pyridin-7-amine, TGF-beta receptor type-1 | Authors: | Dougan, D.R, Lawson, J.D. | Deposit date: | 2017-02-13 | Release date: | 2017-04-12 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (2.55 Å) | Cite: | Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors. Bioorg. Med. Chem. Lett., 27, 2017
|
|