8YHF
| The Crystal Structure of the Type I TGF beta receptor from Biortus. | Descriptor: | 2-fluoranyl-~{N}-[[5-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-1~{H}-imidazol-2-yl]methyl]aniline, TGF-beta receptor type-1 | Authors: | Wang, F, Cheng, W, Lv, Z, Meng, Q, Xu, Y. | Deposit date: | 2024-02-28 | Release date: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.4 Å) | Cite: | The Crystal Structure of the Type I TGF beta receptor from Biortus. To Be Published
|
|
5E8S
| TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (WT) | Descriptor: | TGF-beta receptor type-1 | Authors: | Sheriff, S. | Deposit date: | 2015-10-14 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.45 Å) | Cite: | Crystal structures of apo and inhibitor-bound TGF beta R2 kinase domain: insights into TGF beta R isoform selectivity. Acta Crystallogr D Struct Biol, 72, 2016
|
|
5E8X
| TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D,I211V,Y249F,S280T, Y282F,S287N,A350C,L352F) IN COMPLEX WITH STAUROSPORINE | Descriptor: | GLYCEROL, STAUROSPORINE, TGF-beta receptor type-1 | Authors: | Sheriff, S. | Deposit date: | 2015-10-14 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.45 Å) | Cite: | Crystal structures of apo and inhibitor-bound TGF beta R2 kinase domain: insights into TGF beta R isoform selectivity. Acta Crystallogr D Struct Biol, 72, 2016
|
|
8YHL
| The Crystal Structure of Tgf-Beta Type I Receptor (Alk5) from Biortus | Descriptor: | 1,2-ETHANEDIOL, 2-fluoranyl-~{N}-[[5-(6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-1~{H}-imidazol-2-yl]methyl]aniline, ACETATE ION, ... | Authors: | Wang, F, Cheng, W, Lv, Z, Meng, Q, Xu, Y. | Deposit date: | 2024-02-28 | Release date: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.47 Å) | Cite: | The Crystal Structure of Tgf-Beta Type I Receptor (Alk5) from Biortus To Be Published
|
|
4X2F
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 4-amino-8-(4-aminophenyl)pyrido[2,3-d]pyrimidin-5(8H)-one, SULFATE ION, TGF-beta receptor type-1 | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-26 | Release date: | 2015-10-28 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.49 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
|
|
4X2G
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 4-[(4-aminophenyl)amino]pyrido[2,3-d]pyrimidin-5(6H)-one, SULFATE ION, ... | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-26 | Release date: | 2015-08-12 | Last modified: | 2024-02-28 | Method: | X-RAY DIFFRACTION (1.51 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
|
|
5E8Z
| |
5QIK
| TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) IN COMPLEX WITH N-{4-[3-(6-fluoropyridin-3-yl)-4-oxo-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]pyridin-2-yl}acetamide | Descriptor: | GLYCEROL, N-{4-[3-(6-fluoropyridin-3-yl)-4-oxo-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl]pyridin-2-yl}acetamide, TGF-beta receptor type-1 | Authors: | Sheriff, S. | Deposit date: | 2018-08-05 | Release date: | 2018-10-31 | Last modified: | 2024-03-06 | Method: | X-RAY DIFFRACTION (1.58 Å) | Cite: | Discovery of 4-Azaindole Inhibitors of TGF beta RI as Immuno-oncology Agents. ACS Med Chem Lett, 9, 2018
|
|
6B8Y
| |
5QU0
| TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) IN COMPLEX WITH 6-[4-(3-CHLORO-4-FLUOROPHENYL)-1-(2-HYDROXYETHYL)-1H-IMIDAZOL-5-YL]IMIDAZO[1,2-B]PYRIDAZINE-3-CARBONITRILE | Descriptor: | 6-[4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl]imidazo[1,2-b]pyridazine-3-carbonitrile, GLYCEROL, TGF-beta receptor type-1 | Authors: | Sheriff, S. | Deposit date: | 2019-11-19 | Release date: | 2020-02-05 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (1.67 Å) | Cite: | Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF beta R1 Inhibitor as an Immuno-oncology Agent. Acs Med.Chem.Lett., 11, 2020
|
|
4X0M
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 4-aminopyrido[2,3-d]pyrimidin-5(8H)-one, SULFATE ION, TGF-beta receptor type-1 | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-21 | Release date: | 2014-12-24 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (1.68 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
|
|
4X2J
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 4-[(3-aminophenyl)amino]pyrido[2,3-d]pyrimidin-5(8H)-one, SULFATE ION, TGF-beta receptor type-1 | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-26 | Release date: | 2014-12-24 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.69 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
|
|
4X2K
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 4-[(3-aminophenyl)amino]pyrido[2,3-d]pyrimidin-5(6H)-one, SULFATE ION, TGF-beta receptor type-1 | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-26 | Release date: | 2014-12-24 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.69 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
|
|
5E8T
| TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) | Descriptor: | GLYCEROL, TGF-beta receptor type-1 | Authors: | Sheriff, S. | Deposit date: | 2015-10-14 | Release date: | 2016-05-11 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Crystal structures of apo and inhibitor-bound TGF beta R2 kinase domain: insights into TGF beta R isoform selectivity. Acta Crystallogr D Struct Biol, 72, 2016
|
|
3HMM
| Structure of Alk5 + GW855857 | Descriptor: | 2-(6-methylpyridin-2-yl)-N-pyridin-4-ylquinazolin-4-amine, TGF-beta receptor type-1 | Authors: | Smith, W, Janson, C. | Deposit date: | 2009-05-29 | Release date: | 2009-06-23 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors Bioorg.Med.Chem.Lett., 19, 2009
|
|
3TZM
| TGF-beta Receptor type 1 in complex with SB431542 | Descriptor: | 4-[5-(1,3-benzodioxol-5-yl)-4-(pyridin-2-yl)-1H-imidazol-2-yl]benzamide, TGF-beta receptor type-1 | Authors: | Ogunjimi, A.A, Zeqiraj, E, Ceccarelli, D.F, Sicheri, F. | Deposit date: | 2011-09-27 | Release date: | 2012-05-23 | Last modified: | 2023-09-13 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Structural Basis for Specificity of TGFbeta Family Receptor Small Molecule Inhibitors Cell Signal, 24, 2012
|
|
5QIM
| |
4X2N
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | SULFATE ION, TGF-beta receptor type-1 | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-26 | Release date: | 2014-12-24 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
|
|
3GXL
| ALK-5 kinase complex with GW857175 | Descriptor: | N-1H-indazol-5-yl-2-(6-methylpyridin-2-yl)quinazolin-4-amine, TGF-beta receptor type-1 | Authors: | Smith, W, Janson, C. | Deposit date: | 2009-04-02 | Release date: | 2009-04-21 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors Bioorg.Med.Chem.Lett., 19, 2009
|
|
5QTZ
| TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D) IN COMPLEX WITH 6-[1-(2,2-DIFLUOROETHYL)-4-(6-METHYLPYRIDIN-2-YL)-1H-IMIDAZOL-5-YL]IMIDAZO[1,2-A]PYRIDINE | Descriptor: | 6-[1-(2,2-difluoroethyl)-4-(6-methylpyridin-2-yl)-1H-imidazol-5-yl]imidazo[1,2-a]pyridine, GLYCEROL, TGF-beta receptor type-1 | Authors: | Sheriff, S. | Deposit date: | 2019-11-19 | Release date: | 2020-02-05 | Last modified: | 2024-05-22 | Method: | X-RAY DIFFRACTION (1.83 Å) | Cite: | Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF beta R1 Inhibitor as an Immuno-oncology Agent. Acs Med.Chem.Lett., 11, 2020
|
|
2WOT
| ALK5 IN COMPLEX WITH 4-((5,6-dimethyl-2-(2-pyridyl)-3-pyridyl)oxy)-N-(3,4,5-trimethoxyphenyl)pyridin-2-amine | Descriptor: | 1,2-ETHANEDIOL, 4-[(5,6-DIMETHYL-2,2'-BIPYRIDIN-3-YL)OXY]-N-(3,4,5-TRIMETHOXYPHENYL)PYRIDIN-2-AMINE, TGF-BETA RECEPTOR TYPE-1 | Authors: | Norman, R.A, Debreczeni, J.E, Goldberg, F.W, Ward, R.A, Finlay, R, Powell, S.J, Roberts, N.J, Dishington, A.P, Gingell, H.J, Wickson, K.F, Roberts, A.L. | Deposit date: | 2009-07-28 | Release date: | 2009-09-22 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.85 Å) | Cite: | Rapid Generation of a High Quality Lead for Transforming Growth Factor-Beta (Tgf-Beta) Type I Receptor (Alk5). J.Med.Chem., 52, 2009
|
|
5E8W
| |
5QIL
| |
5FRI
| ALK5 in complex witha an N-(4-anilino-2-pyridyl)acetamide inhibitor. | Descriptor: | 1,2-ETHANEDIOL, N-[4-[(6-chloro-[1,3]dioxolo[4,5-b]pyridin-7-yl)amino]-2-pyridyl]cyclopropanecarboxamide, TGF-BETA RECEPTOR TYPE-1 | Authors: | Goldberg, F.W, Daunt, P, Pearson, S.E, Greenwood, R, Debreczeni, J, Grist, M. | Deposit date: | 2015-12-17 | Release date: | 2016-07-27 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Identification and optimisation of a series of N-(4-anilino-2-pyridyl)acetamide activin receptor-like kinase 1 (ALK1) inhibitors Med. Chem. Commun., 7, 2016
|
|
1VJY
| Crystal Structure of a Naphthyridine Inhibitor of Human TGF-beta Type I Receptor | Descriptor: | 2-[5-(6-METHYLPYRIDIN-2-YL)-2,3-DIHYDRO-1H-PYRAZOL-4-YL]-1,5-NAPHTHYRIDINE, TGF-beta receptor type I | Authors: | Gellibert, F, Woolven, J, Fouchet, M.-H, Mathews, N, Goodland, H, Lovegrove, V, Laroze, A, Nguyen, V.-L, Sautet, S, Wang, R, Janson, C, Smith, W, Krysa, G, Boullay, V, de Gouville, A.-C, Huet, S, Hartley, D. | Deposit date: | 2004-04-07 | Release date: | 2004-08-31 | Last modified: | 2023-12-27 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Identification of 1,5-Naphthyridine Derivatives as a Novel Series of Potent and Selective TGF-beta Type I Receptor Inhibitors. J.Med.Chem., 47, 2004
|
|