6Z4B
 
 | | Crystal Structure of EGFR-T790M/V948R in Complex with Osimertinib and EAI045 | | Descriptor: | (2R)-2-(5-fluoro-2-hydroxyphenyl)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, SULFATE ION, ... | | Authors: | Niggenaber, J, Mueller, M.P, Rauh, D. | | Deposit date: | 2020-05-25 | | Release date: | 2020-11-11 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands.
Acs Med.Chem.Lett., 11, 2020
|
|
6Z4D
 | | Crystal Structure of EGFR-T790M/V948R in Complex with Mavelertinib and EAI001 | | Descriptor: | (2R)-2-(1-oxo-1,3-dihydro-2H-isoindol-2-yl)-2-phenyl-N-(1,3-thiazol-2-yl)acetamide, Epidermal growth factor receptor, N-[(3R,4R)-4-fluoro-1-{6-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-9-methyl-9H-purin-2-yl}pyrrolidin-3-yl]propanamide, ... | | Authors: | Niggenaber, J, Mueller, M.P, Rauh, D. | | Deposit date: | 2020-05-25 | | Release date: | 2020-11-11 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands.
Acs Med.Chem.Lett., 11, 2020
|
|
8W5C
 | | Crystal structure of FGFR4 kinase domain in complex with 8K | | Descriptor: | Fibroblast growth factor receptor 4, N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-5-methanoyl-6-[(4-methylpiperazin-1-yl)methyl]-1-propan-2-yl-pyrrolo[3,2-b]pyridine-3-carboxamide | | Authors: | Zhang, Z.M, Huang, H.S. | | Deposit date: | 2023-08-26 | | Release date: | 2024-07-31 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J.Med.Chem., 67, 2024
|
|
7CQE
 | |
8XLQ
 | |
8XLO
 | |
8YGX
 | |
8YGZ
 | | The Crystal Structure of TGF beta R2 kinase domain from Biortus. | | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, TGF-beta receptor type-2 | | Authors: | Wang, F, Cheng, W, Lv, Z, Ju, C, Wang, J. | | Deposit date: | 2024-02-27 | | Release date: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | The Crystal Structure of TGF beta R2 kinase domain from Biortus.
To Be Published
|
|
6YVY
 | |
6YVS
 | | FOCAL ADHESION KINASE CATALYTIC DOMAIN IN COMPLEX WITH 5-{4-[(Pyridin-3-ylmethyl)-amino]-5-trifluoromethyl-pyrimidin-2-ylamino}-1,3-dihydro-indol-2-one | | Descriptor: | 5-[[4-(pyridin-3-ylmethylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]-1,3-dihydroindol-2-one, Focal adhesion kinase 1, SULFATE ION | | Authors: | Musil, D, Heinrich, T, Amaral, M. | | Deposit date: | 2020-04-28 | | Release date: | 2021-02-10 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.81 Å) | | Cite: | Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Cell Chem Biol, 28, 2021
|
|
7CC2
 | |
6ZCU
 | | syk in complex with 57262_SYKB-AZ13344324-2 | | Descriptor: | 6-chloro-2-(2-fluoro-4,5-dimethoxyphenyl)-N-(piperidin-4-ylmethyl)-3H-imidazo[4,5-b]pyridin-7-amine, Tyrosine-protein kinase SYK | | Authors: | Read, J.A, Patel, J. | | Deposit date: | 2020-06-12 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.73 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 2b
To Be Published
|
|
8YVV
 | | The Crystal Structure of BTK from Biortus | | Descriptor: | 1,2-ETHANEDIOL, CHLORIDE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | Wang, F, Cheng, W, Yuan, Z, Lin, D, Pan, W. | | Deposit date: | 2024-03-29 | | Release date: | 2024-07-03 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | The Crystal Structure of BTK from Biortus.
To Be Published
|
|
6ZCP
 | | SYK Kinase domain in complex with azabenzimidazole inhibitor 2b | | Descriptor: | 7-[[4-[4-[(dimethylamino)methyl]pyrazol-1-yl]pyrimidin-2-yl]amino]-~{N},3-dimethyl-imidazo[1,5-a]pyridine-1-carboxamide, Tyrosine-protein kinase SYK | | Authors: | Read, J.A. | | Deposit date: | 2020-06-11 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 4
To Be Published
|
|
6ZCS
 | | SYK Kinase domain in complex with azabenzimidazole inhibitor 3 | | Descriptor: | (3~{R},4~{R})-~{N}4-[1-[2-(1-methylindol-4-yl)-3~{H}-imidazo[4,5-b]pyridin-7-yl]pyrazol-4-yl]oxane-3,4-diamine, Tyrosine-protein kinase SYK | | Authors: | Read, J.A. | | Deposit date: | 2020-06-12 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.47 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 3
To Be Published
|
|
6ZCX
 | | SYK Kinase domain in complex with azabenzimidazole inhibitor 18 | | Descriptor: | Tyrosine-protein kinase SYK, ~{N},1-dimethyl-5-[[4-[3-methyl-4-[[(3~{R})-piperidin-3-yl]amino]pyrazol-1-yl]pyrimidin-2-yl]amino]indazole-3-carboxamide | | Authors: | Read, J.A. | | Deposit date: | 2020-06-12 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.66 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 18
To Be Published
|
|
6ZC0
 | | SYK Kinase domain in complex with azabenzimidazole inhibitor 2b | | Descriptor: | Tyrosine-protein kinase SYK, ~{N},~{N}-dimethyl-1-[1-[2-(1-methylindol-4-yl)-3~{H}-imidazo[4,5-b]pyridin-7-yl]pyrazol-4-yl]methanamine | | Authors: | Read, J.A. | | Deposit date: | 2020-06-09 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.97 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 2b
To Be Published
|
|
6ZCQ
 | | SYK Kinase domain in complex with diamine inhibitor 5 | | Descriptor: | 7-[[4-[4-[[(3~{R},4~{R})-3-azanyloxan-4-yl]amino]pyrazol-1-yl]pyrimidin-2-yl]amino]-~{N},3-dimethyl-imidazo[1,5-a]pyridine-1-carboxamide, Tyrosine-protein kinase SYK | | Authors: | Read, J.A. | | Deposit date: | 2020-06-11 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.32 Å) | | Cite: | SYK Kinase domain in complex with diamine inhibitor 5
To Be Published
|
|
6ZCY
 | | SYK Kinase domain in complex with diamine inhibitor 16 | | Descriptor: | Tyrosine-protein kinase SYK, ~{N},1-dimethyl-5-[[4-[3-methyl-4-[[(3~{R})-pyrrolidin-3-yl]amino]pyrazol-1-yl]pyrimidin-2-yl]amino]indazole-3-carboxamide | | Authors: | Read, J.A. | | Deposit date: | 2020-06-12 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.81 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 16
To Be Published
|
|
6ZCR
 | | SYK Kinase domain in complex with azabenzimidazole inhibitor 7 | | Descriptor: | 6-chloro-2-(2-fluoro-4,5-dimethoxyphenyl)-N-(piperidin-4-ylmethyl)-3H-imidazo[4,5-b]pyridin-7-amine, Tyrosine-protein kinase SYK | | Authors: | Read, J.A, Patel, J. | | Deposit date: | 2020-06-12 | | Release date: | 2021-06-23 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.73 Å) | | Cite: | SYK Kinase domain in complex with azabenzimidazole inhibitor 7
To Be Published
|
|
8YKI
 | | FGFR-1 in complex with ligand tasurgratinib | | Descriptor: | CHLORIDE ION, Fibroblast growth factor receptor 1, Tasurgratinib | | Authors: | Ikemori-Kawada, M, Watanabe Miyano, S. | | Deposit date: | 2024-03-05 | | Release date: | 2024-06-12 | | Method: | X-RAY DIFFRACTION (2.79 Å) | | Cite: | Antitumor Activity of Tasurgratinib as an Orally Available FGFR1-3 Inhibitor in Cholangiocarcinoma Models With FGFR2-fusion.
Anticancer Res., 44, 2024
|
|
7DHL
 | | Crystal structure of FGFR3 in complex with pyrimidine derivative | | Descriptor: | 5-[2-(3,5-dimethoxyphenyl)ethyl]-N-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidin-2-amine, Fibroblast growth factor receptor 3 | | Authors: | Echizen, Y, Tateishi, Y, Amano, Y. | | Deposit date: | 2020-11-16 | | Release date: | 2021-02-03 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.57 Å) | | Cite: | Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.
Bioorg.Med.Chem., 33, 2021
|
|
8Y22
 | | FGFR1 kinase domain with a covalent inhibitor 9g | | Descriptor: | Fibroblast growth factor receptor 1, SULFATE ION, ~{N}-[4-[[4-azanyl-3-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]propanamide | | Authors: | Chen, X.J, Chen, Y.H. | | Deposit date: | 2024-01-25 | | Release date: | 2024-06-26 | | Method: | X-RAY DIFFRACTION (2.792 Å) | | Cite: | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
|
|
8XZ7
 | | FGFR1 kinase domain with a covalent inhibitor 10h | | Descriptor: | 5-azanyl-3-[2-[4,6-bis(fluoranyl)-2-methyl-3~{H}-benzimidazol-5-yl]ethynyl]-1-[[3-(prop-2-enoylamino)phenyl]methyl]pyrazole-4-carboxamide, Fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Chen, X.J, Chen, Y.H. | | Deposit date: | 2024-01-20 | | Release date: | 2024-06-26 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
|
|
8ZKD
 | | The Crystal Structure of the RON from Biortus. | | Descriptor: | 1,2-ETHANEDIOL, MAGNESIUM ION, Macrophage-stimulating protein receptor beta chain, ... | | Authors: | Wang, F, Cheng, W, Yuan, Z, Qi, J, Pan, W. | | Deposit date: | 2024-05-16 | | Release date: | 2024-06-26 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | The Crystal Structure of the RON from Biortus.
To Be Published
|
|
