5E8U
 
 | | TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D,I211V,Y249F,S280T, Y282F,S287N,A350C,L352F) | | 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 (2.03 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
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5E90
 | | TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D,I211V,Y249F, S280T,Y282F,S287N,A350C,L352F) IN COMPLEX WITH 3-AMINO-6- [4-(2-HYDROXYETHYL)PHENYL]-N-[4-(MORPHOLIN-4-YL)PYRIDIN-3-YL]PYRAZINE-2-CARBOXAMIDE | | Descriptor: | 3-amino-6-[4-(2-hydroxyethyl)phenyl]-N-[4-(morpholin-4-yl)pyridin-3-yl]pyrazine-2-carboxamide, 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 (2.05 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
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2WOU
 | | ALK5 IN COMPLEX WITH 4-((4-((2,6-dimethyl-3-pyridyl)oxy)-2-pyridyl) amino)benzenesulfonamide | | Descriptor: | 1,2-ETHANEDIOL, 4-({4-[(2,6-DIMETHYLPYRIDIN-3-YL)OXY]PYRIDIN-2-YL}AMINO)BENZENESULFONAMIDE, TGF-BETA RECEPTOR TYPE-1 | | Authors: | Debreczeni, J.E, Norman, R.A, 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 (2.3 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
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1PY5
 | | Crystal Structure of TGF-beta receptor I kinase with inhibitor | | Descriptor: | 4-(3-PYRIDIN-2-YL-1H-PYRAZOL-4-YL)QUINOLINE, SULFATE ION, TGF-beta receptor type I | | Authors: | Zhang, F, Sawyer, J.S. | | Deposit date: | 2003-07-08 | | Release date: | 2004-07-13 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Bioorg.Med.Chem.Lett., 14, 2004
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6MAC
 | | Ternary structure of GDF11 bound to ActRIIB-ECD and Alk5-ECD | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Activin receptor type-2B, Growth/differentiation factor 11, ... | | Authors: | Goebel, E.J, Thompson, T.B. | | Deposit date: | 2018-08-27 | | Release date: | 2019-07-17 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.34 Å) | | Cite: | Structural characterization of an activin class ternary receptor complex reveals a third paradigm for receptor specificity.
Proc.Natl.Acad.Sci.USA, 116, 2019
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1RW8
 | | Crystal Structure of TGF-beta receptor I kinase with ATP site inhibitor | | Descriptor: | 3-(4-FLUOROPHENYL)-2-(6-METHYLPYRIDIN-2-YL)-5,6-DIHYDRO-4H-PYRROLO[1,2-B]PYRAZOLE, TGF-beta receptor type I | | Authors: | Zhang, F, Sawyer, J.S. | | Deposit date: | 2003-12-16 | | Release date: | 2005-02-01 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Bioorg.Med.Chem.Lett., 14, 2004
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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
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1B6C
 | | CRYSTAL STRUCTURE OF THE CYTOPLASMIC DOMAIN OF THE TYPE I TGF-BETA RECEPTOR IN COMPLEX WITH FKBP12 | | Descriptor: | FK506-BINDING PROTEIN, SULFATE ION, TGF-B SUPERFAMILY RECEPTOR TYPE I | | Authors: | Huse, M, Chen, Y.-G, Massague, J, Kuriyan, J. | | Deposit date: | 1999-01-13 | | Release date: | 1999-06-15 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Crystal structure of the cytoplasmic domain of the type I TGF beta receptor in complex with FKBP12.
Cell(Cambridge,Mass.), 96, 1999
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3KCF
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1IAS
 | | CYTOPLASMIC DOMAIN OF UNPHOSPHORYLATED TYPE I TGF-BETA RECEPTOR CRYSTALLIZED WITHOUT FKBP12 | | Descriptor: | SULFATE ION, TGF-BETA RECEPTOR TYPE I | | Authors: | Huse, M, Muir, T.W, Chen, Y.-G, Kuriyan, J, Massague, J. | | Deposit date: | 2001-03-23 | | Release date: | 2001-10-03 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | The TGF beta receptor activation process: an inhibitor- to substrate-binding switch.
Mol.Cell, 8, 2001
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3KFD
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2PJY
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3FAA
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2X7O
 | | Crystal structure of TGFbRI complexed with an indolinone inhibitor | | Descriptor: | (3Z)-N-ETHYL-N-METHYL-2-OXO-3-(PHENYL{[4-(PIPERIDIN-1-YLMETHYL)PHENYL]AMINO}METHYLIDENE)-2,3-DIHYDRO-1H-INDOLE-6-CARBOXAMIDE, TGF-BETA RECEPTOR TYPE I | | Authors: | Roth, G.J, Heckel, A, Brandl, T, Grauert, M, Hoerer, S, Kley, J.T, Schnapp, G, Baum, P, Mennerich, D, Schnapp, A, Park, J.E. | | Deposit date: | 2010-03-03 | | Release date: | 2010-10-20 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (3.7 Å) | | Cite: | Design, Synthesis and Evaluation of Indolinones as Inhibitors of the Transforming Growth Factor Beta Receptor I (Tgfbri)
J.Med.Chem., 53, 2010
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2L5S
 | | Solution structure of the extracellular domain of the TGF-beta type I receptor | | Descriptor: | TGF-beta receptor type-1 | | Authors: | Zuniga, J.E, Ilangovan, U, Pardeep, M, Hinck, C, Huang, T. | | Deposit date: | 2010-11-04 | | Release date: | 2011-10-26 | | Method: | SOLUTION NMR | | Cite: | The TbetaR-I Pre-Helix Extension Is Structurally Ordered in the Unbound Form and Its Flanking Prolines Are Essential for Binding
J.Mol.Biol., 412, 2011
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