3R04
| The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors | Descriptor: | 5-{6-[(trans-4-aminocyclohexyl)amino]pyrazin-2-yl}-1-benzofuran-2-carboxylic acid, IMIDAZOLE, Proto-oncogene serine/threonine-protein kinase pim-1 | Authors: | Xiang, Y, Hirth, B, Asmussen, G, Biemann, H.-P, Good, A, Fitzgerald, M, Gladysheva, T, Jancsics, K, Liu, J, Metz, M, Papoulis, A, Skerlj, R, Stepp, D.J, Wei, R.R. | Deposit date: | 2011-03-07 | Release date: | 2011-05-11 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors. Bioorg.Med.Chem.Lett., 21, 2011
|
|
3R02
| The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors | Descriptor: | 7-[(cis-4-aminocyclohexyl)amino]-5-bromo-1-benzofuran-2-carboxylic acid, IMIDAZOLE, Proto-oncogene serine/threonine-protein kinase pim-1 | Authors: | Xiang, Y, Hirth, B, Asmussen, G, Biemann, H.-P, Good, A, Fitzgerald, M, Gladysheva, T, Jancsics, K, Liu, J, Metz, M, Papoulis, A, Skerlj, R, Stepp, D.J, Wei, R.R. | Deposit date: | 2011-03-07 | Release date: | 2011-05-11 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors. Bioorg.Med.Chem.Lett., 21, 2011
|
|
8W1L
| |
6V9C
| Crystal structure of FGFR4 kinase domain in complex with covalent inhibitor | Descriptor: | Fibroblast growth factor receptor 4, N-[(3R,4S)-4-{[6-(2,6-dichloro-3,5-dimethoxyphenyl)-8-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl]amino}oxolan-3-yl]prop-2-enamide, SULFATE ION | Authors: | Liu, J, Liu, H. | Deposit date: | 2019-12-13 | Release date: | 2020-03-25 | Last modified: | 2023-10-11 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma. Acs Med.Chem.Lett., 11, 2020
|
|
6WXJ
| CSF1R signaling is a regulator of pathogenesis in progressive MS | Descriptor: | 4-(3-{[(2S)-2-(6-methoxypyridin-3-yl)-2,3-dihydro-1,4-benzodioxin-6-yl]methyl}-3H-imidazo[4,5-b]pyridin-6-yl)-2-methylbut-3-yn-2-amine, Macrophage colony-stimulating factor 1 receptor | Authors: | Liu, J. | Deposit date: | 2020-05-10 | Release date: | 2021-02-10 | Last modified: | 2023-10-18 | Method: | X-RAY DIFFRACTION (2.62 Å) | Cite: | CSF1R signaling is a regulator of pathogenesis in progressive MS. Cell Death Dis, 11, 2020
|
|
8UH6
| Degrader-induced complex between PTPN2 and CRBN-DDB1 | Descriptor: | (5P)-3-(carboxymethoxy)-4-chloro-5-(3-{[(4S)-1-({3-[(4-{1-[(3R)-2,6-dioxopiperidin-3-yl]-3-methyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl}piperidine-1-carbonyl)amino]phenyl}methanesulfonyl)-2,2-dimethylpiperidin-4-yl]amino}phenyl)thiophene-2-carboxylic acid, DNA damage-binding protein 1, Protein cereblon, ... | Authors: | Catalano, C, Bratkowski, M, Scapin, G, Hao, Q. | Deposit date: | 2023-10-06 | Release date: | 2024-09-11 | Method: | ELECTRON MICROSCOPY (3.3 Å) | Cite: | Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex. Commun Chem, 7, 2024
|
|
8U0H
| Crystal structure of PTPN2 with a PROTAC | Descriptor: | (5P)-3-(carboxymethoxy)-4-chloro-5-(3-{[(4S)-1-({3-[2-(4-{3-[(3R)-2,6-dioxopiperidin-3-yl]-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl}piperidin-1-yl)acetamido]phenyl}methanesulfonyl)-2,2-dimethylpiperidin-4-yl]amino}phenyl)thiophene-2-carboxylic acid, ACETATE ION, PTPN2, ... | Authors: | Jain, R, Longenecker, K, Qiu, W. | Deposit date: | 2023-08-29 | Release date: | 2024-09-04 | Method: | X-RAY DIFFRACTION (1.93 Å) | Cite: | Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex. Commun Chem, 7, 2024
|
|
3C27
| Cyanofluorophenylacetamides as Orally Efficacious Thrombin Inhibitors | Descriptor: | Hirudin-3A, N-[2-(carbamimidamidooxy)ethyl]-2-{6-cyano-3-[(2,2-difluoro-2-pyridin-2-ylethyl)amino]-2-fluorophenyl}acetamide, Thrombin heavy chain, ... | Authors: | Spurlino, J.C, McMillan, M, Lewandowski, F, Milligan, C. | Deposit date: | 2008-01-24 | Release date: | 2009-02-17 | Last modified: | 2011-07-13 | Method: | X-RAY DIFFRACTION (2.182 Å) | Cite: | Cyanofluorophenylacetamides as Orally Efficacious Thrombin Inhibitors To be Published
|
|
7LGS
| |
3R00
| |
3R01
| The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors | Descriptor: | 5-bromo-7-methoxy-1-benzofuran-2-carboxylic acid, IMIDAZOLE, Proto-oncogene serine/threonine-protein kinase pim-1 | Authors: | Liu, J. | Deposit date: | 2011-03-07 | Release date: | 2011-05-11 | Last modified: | 2024-02-21 | Method: | X-RAY DIFFRACTION (2.6 Å) | Cite: | The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors. Bioorg.Med.Chem.Lett., 21, 2011
|
|
3VC4
| |
3VBX
| |
3VBT
| |
3VBQ
| |
3VBV
| |
3VBY
| |
3VBW
| |