5FTA
| Crystal structure of the N-terminal BTB domain of human KCTD10 | Descriptor: | BTB/POZ DOMAIN-CONTAINING ADAPTER FOR CUL3-MEDIATED RHOA DEGRADATION PROTEIN 3, MERCURY (II) ION | Authors: | Pinkas, D.M, Sanvitale, C.E, Solcan, N, Goubin, S, Tallant, C, Newman, J.A, Kopec, J, Fitzpatrick, F, Talon, R, Collins, P, Krojer, T, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2016-01-12 | Release date: | 2016-02-17 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (2.64 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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5G6V
| Crystal structure of the PCTAIRE1 kinase in complex with inhibitor | Descriptor: | 1,2-ETHANEDIOL, 4-[4-({[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, CYCLIN-DEPENDENT KINASE 16 | Authors: | Dixon-Clarke, S.E, Galan Bartual, S, Elkins, J, Savitsky, P, Kopec, J, Mackenzie, A, Tallant, C, Heroven, C, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2016-08-16 | Release date: | 2016-11-23 | Last modified: | 2023-08-02 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16. Biochem.J., 474, 2017
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3BLH
| Crystal Structure of Human CDK9/cyclinT1 | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Cell division protein kinase 9, Cyclin-T1 | Authors: | Baumli, S, Lolli, G, Lowe, E.D, Johnson, L.N. | Deposit date: | 2007-12-11 | Release date: | 2008-07-01 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.48 Å) | Cite: | The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation Embo J., 27, 2008
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3BLR
| Crystal Structure of Human CDK9/cyclinT1 in complex with Flavopiridol | Descriptor: | 2-(2-CHLORO-PHENYL)-5,7-DIHYDROXY-8-(3-HYDROXY-1-METHYL-PIPERIDIN-4-YL)-4H-BENZOPYRAN-4-ONE, Cell division protein kinase 9, Cyclin-T1, ... | Authors: | Baumli, S, Lolli, G, Lowe, E.D, Johnson, L.N. | Deposit date: | 2007-12-11 | Release date: | 2008-07-01 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation Embo J., 27, 2008
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3H9R
| Crystal structure of the kinase domain of type I activin receptor (ACVR1) in complex with FKBP12 and dorsomorphin | Descriptor: | 6-[4-(2-piperidin-1-ylethoxy)phenyl]-3-pyridin-4-ylpyrazolo[1,5-a]pyrimidine, Activin receptor type-1, Peptidyl-prolyl cis-trans isomerase FKBP1A, ... | Authors: | Chaikuad, A, Alfano, I, Shrestha, B, Muniz, J.R.C, Petrie, K, Fedorov, O, Phillips, C, Bishop, S, Mahajan, P, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2009-04-30 | Release date: | 2009-06-02 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Structure of the Bone Morphogenetic Protein Receptor ALK2 and Implications for Fibrodysplasia Ossificans Progressiva. J.Biol.Chem., 287, 2012
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3II7
| Crystal structure of the kelch domain of human KLHL7 | Descriptor: | 1,2-ETHANEDIOL, Kelch-like protein 7 | Authors: | Chaikuad, A, Thangaratnarajah, C, Cooper, C.D.O, Ugochukwu, E, Muniz, J.R.C, Krojer, T, Sethi, R, Pike, A.C.W, Filippakopoulos, P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2009-07-31 | Release date: | 2009-08-25 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (1.63 Å) | Cite: | Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases. J.Biol.Chem., 288, 2013
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6YYE
| TREM2 extracellular domain (19-131) in complex with single-chain variable fragment (scFv-2) | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, TREM2 Single chain variable 2, Triggering receptor expressed on myeloid cells 2 | Authors: | Szykowska, A, Preger, C, Krojer, T, Mukhopadhyay, S.M.M, McKinley, G, Graslund, S, Wigren, E, Persson, H, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Di Daniel, E, Burgess-Brown, N, Bullock, A. | Deposit date: | 2020-05-04 | Release date: | 2021-02-17 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.36 Å) | Cite: | Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain. Structure, 29, 2021
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7OOV
| Crystal structure of PIM1 in complex with ARC-1411 | Descriptor: | 1,2-ETHANEDIOL, Inhibitor ARC-1411, SULFATE ION, ... | Authors: | Chaikuad, A, Dixon-Clarke, S.E, Nonga, O.E, Uri, A, Bullock, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2021-05-28 | Release date: | 2021-08-04 | Last modified: | 2024-04-10 | Method: | X-RAY DIFFRACTION (1.96 Å) | Cite: | Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules, 26, 2021
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7OOX
| Crystal structure of PIM1 in complex with ARC-3126 | Descriptor: | 1,2-ETHANEDIOL, Inhibitor ARC-3126, PHOSPHATE ION, ... | Authors: | Chaikuad, A, Dixon-Clarke, S.E, Nonga, O.E, Uri, A, Bullock, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2021-05-28 | Release date: | 2021-08-04 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (1.97 Å) | Cite: | Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules, 26, 2021
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7OOW
| Crystal structure of PIM1 in complex with ARC-1415 | Descriptor: | 1,2-ETHANEDIOL, INHIBITOR ARC-1415, MAGNESIUM ION, ... | Authors: | Chaikuad, A, Dixon-Clarke, S.E, Nonga, O.E, Uri, A, Bullock, A, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2021-05-28 | Release date: | 2021-08-04 | Last modified: | 2024-04-10 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules, 26, 2021
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5A6R
| Crystal structure of the BTB domain of human KCTD17 | Descriptor: | BTB/POZ DOMAIN-CONTAINING PROTEIN KCTD17 | Authors: | Pinkas, D.M, Sorrell, F, Sanvitale, C.E, Goubin, S, Williams, E, Newman, J.A, Pearce, N.M, Neshich, I, Pike, A.C.W, MacKenzie, A, Quigley, A, Faust, B, Carpenter, E.P, Tallant, C, Kopec, J, Chalk, R, Krojer, T, Burgess-Brown, N.A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2015-06-30 | Release date: | 2015-11-04 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.85 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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5A15
| Crystal structure of the BTB domain of human KCTD16 | Descriptor: | BTB/POZ DOMAIN-CONTAINING PROTEIN KCTD16 | Authors: | Pinkas, D.M, Sanvitale, C.E, Solcan, N, Goubin, S, Canning, P, Dixon Clarke, S.E, Talon, R, Wiggers, H.J, Fitzpatrick, F, Tallant, C, Kopec, J, Chalk, R, Doutch, J, Krojer, T, Burgess-Brown, N.A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2015-04-28 | Release date: | 2015-11-04 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (2.76 Å) | Cite: | Structural complexity in the KCTD family of Cullin3-dependent E3 ubiquitin ligases. Biochem. J., 474, 2017
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5ACB
| Crystal Structure of the Human Cdk12-Cyclink Complex | Descriptor: | CYCLIN-DEPENDENT KINASE 12, CYCLIN-K, N-[4-[(3R)-3-[[5-chloranyl-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]piperidin-1-yl]carbonylphenyl]-4-(dimethylamino)butanamide | Authors: | Dixon Clarke, S.E, Elkins, J.M, Pike, A.C.W, Mackenzie, A, Goubin, S, Strain-Damerell, C, Mahajan, P, Tallant, C, Chalk, R, Wiggers, H, Kopec, J, Fitzpatrick, F, Burgess-Brown, N, Carpenter, E.P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | Deposit date: | 2015-08-14 | Release date: | 2016-06-15 | Last modified: | 2016-10-05 | Method: | X-RAY DIFFRACTION (2.7 Å) | Cite: | Covalent Targeting of Remote Cysteine Residues to Develop Cdk12 and Cdk13 Inhibitors. Nat.Chem.Biol., 12, 2016
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6YMQ
| TREM2 extracellular domain (19-131) in complex with single-chain variable 4 (scFv-4) | Descriptor: | (4S)-2-METHYL-2,4-PENTANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, Single-chain variable 4, ... | Authors: | Szykowska, A, Preger, C, Scacioc, A, Mukhopadhyay, S.M.M, McKinley, G, Graslund, S, Wigren, E, Persson, H, von Delft, F, Arrowsmith, C.H, Edwards, A, Bountra, C, Di Daniel, E, Davis, J.B, Burgess-Brown, N, Bullock, A. | Deposit date: | 2020-04-09 | Release date: | 2021-02-17 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (3.07 Å) | Cite: | Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain. Structure, 29, 2021
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6Y6C
| TREM2 extracellular domain (19-174) in complex with single-chain variable fragment (scFv-4) | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Single chain variable, Triggering receptor expressed on myeloid cells 2 | Authors: | Szykowska, A, Preger, C, Williams, E, Mukhopadhyay, S.M.M, McKinley, G, Gruslund, S, Wigren, E, Persson, H, Arrowsmith, C.H, Edwards, A, von Delft, F, Bountra, C, Davis, J.B, Di Daniel, E, Burgess-Brown, N, Bullock, A. | Deposit date: | 2020-02-26 | Release date: | 2021-02-17 | Last modified: | 2024-01-31 | Method: | X-RAY DIFFRACTION (2.26 Å) | Cite: | Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain. Structure, 29, 2021
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3EMW
| Crystal Structure of human splA/ryanodine receptor domain and SOCS box containing 2 (SPSB2) in complex with a 20-residue VASA peptide | Descriptor: | 1,2-ETHANEDIOL, Peptide (VASA), SPRY domain-containing SOCS box protein 2 | Authors: | Filippakopoulos, P, Sharpe, T, Keates, T, Murray, J.W, Savitsky, P, Roos, A.K, Pike, A.C.W, Von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2008-09-25 | Release date: | 2008-10-28 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4. J.Mol.Biol., 401, 2010
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3CXW
| Crystal structure of human proto-oncogene serine threonine kinase (PIM1) in complex with a consensus peptide and a beta carboline ligand I | Descriptor: | (4R)-7,8-dichloro-1',9-dimethyl-1-oxo-1,2,4,9-tetrahydrospiro[beta-carboline-3,4'-piperidine]-4-carbonitrile, CHLORIDE ION, Pimtide peptide, ... | Authors: | Filippakopoulos, P, Bullock, A, Fedorov, O, Huber, K, Bracher, F, Pike, A.C.W, Roos, A, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2008-04-25 | Release date: | 2008-07-15 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.1 Å) | Cite: | 7,8-Dichloro-1-oxo-beta-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes J.Med.Chem., 55, 2012
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3F2O
| Crystal Structure of human splA/ryanodine receptor domain and SOCS box containing 1 (SPSB1) in complex with a 20-residue VASA peptide | Descriptor: | 20-mer peptide from ATP-dependent RNA helicase vasa, SPRY domain-containing SOCS box protein 1 | Authors: | Filippakopoulos, P, Sharpe, T, Keates, T, Murray, J.W, Savitsky, P, Roos, A, Pike, A.C.W, Von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2008-10-30 | Release date: | 2008-12-09 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.05 Å) | Cite: | Structural basis for Par-4 recognition by the SPRY domain- and SOCS box-containing proteins SPSB1, SPSB2, and SPSB4. J.Mol.Biol., 401, 2010
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3CY2
| Crystal structure of human proto-oncogene serine threonine kinase (PIM1) in complex with a consensus peptide and a beta carboline ligand II | Descriptor: | (4R)-7-chloro-9-methyl-1-oxo-1,2,4,9-tetrahydrospiro[beta-carboline-3,4'-piperidine]-4-carbonitrile, 1,2-ETHANEDIOL, CHLORIDE ION, ... | Authors: | Filippakopoulos, P, Bullock, A, Fedorov, O, Huber, K, Bracher, F, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2008-04-25 | Release date: | 2008-07-15 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.01 Å) | Cite: | 7,8-Dichloro-1-oxo-beta-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes J.Med.Chem., 55, 2012
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3G2F
| Crystal structure of the kinase domain of bone morphogenetic protein receptor type II (BMPR2) at 2.35 A resolution | Descriptor: | 1,2-ETHANEDIOL, ADENOSINE-5'-DIPHOSPHATE, Bone morphogenetic protein receptor type-2, ... | Authors: | Chaikuad, A, Thangaratnarajah, C, Roos, A.K, Filippakopoulos, P, Salah, E, Phillips, C, Keates, T, Fedorov, O, Chalk, R, Petrie, K, Pike, A.C.W, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2009-01-31 | Release date: | 2009-02-17 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.35 Å) | Cite: | Structural consequences of BMPR2 kinase domain mutations causing pulmonary arterial hypertension. Sci Rep, 9, 2019
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3MA3
| Crystal structure of human proto-oncogene serine threonine kinase (PIM1) in complex with a consensus peptide and a naphtho-difuran ligand | Descriptor: | Pimtide, Proto-oncogene serine/threonine-protein kinase pim-1, naphtho[2,1-b:7,6-b']difuran-2,8-dicarboxylic acid | Authors: | Filippakopoulos, P, Bullock, A, Fedorov, O, Vollmar, M, von Delft, F, Cochet, C, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2010-03-23 | Release date: | 2010-04-14 | Last modified: | 2023-09-06 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights. Faseb J., 24, 2010
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3MTL
| Crystal structure of the PCTAIRE1 kinase in complex with Indirubin E804 | Descriptor: | (2Z,3E)-2,3'-BIINDOLE-2',3(1H,1'H)-DIONE 3-{O-[(3R)-3,4-DIHYDROXYBUTYL]OXIME}, Cell division protein kinase 16 | Authors: | Krojer, T, Sharpe, T.D, Roos, A, Savitsky, P, Amos, A, Ayinampudi, V, Berridge, G, Fedorov, O, Keates, T, Phillips, C, Burgess-Brown, N, Zhang, Y, Pike, A.C.W, Muniz, J, Vollmar, M, Thangaratnarajah, C, Rellos, P, Ugochukwu, E, Filippakopoulos, P, Yue, W, Das, S, von Delft, F, Edwards, A, Arrowsmith, C.H, Weigelt, J, Bountra, C, Knapp, S, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2010-04-30 | Release date: | 2010-06-09 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16. Biochem.J., 474, 2017
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3MY0
| Crystal structure of the ACVRL1 (ALK1) kinase domain bound to LDN-193189 | Descriptor: | 4-[6-(4-piperazin-1-ylphenyl)pyrazolo[1,5-a]pyrimidin-3-yl]quinoline, Serine/threonine-protein kinase receptor R3 | Authors: | Chaikuad, A, Alfano, I, Cooper, C, Mahajan, P, Daga, N, Sanvitale, C, Fedorov, O, Petrie, K, Savitsky, P, Gileadi, O, Sethi, R, Krojer, T, Muniz, J.R.C, Pike, A.C.W, Vollmar, M, Carpenter, C.P, Ugochukwu, E, Knapp, S, von Delft, F, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2010-05-08 | Release date: | 2010-07-21 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.65 Å) | Cite: | A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis, 18, 2015
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3MTF
| Crystal structure of the ACVR1 kinase in complex with a 2-aminopyridine inhibitor | Descriptor: | 1,2-ETHANEDIOL, 3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol, Activin receptor type-1, ... | Authors: | Chaikuad, A, Sanvitale, C, Cooper, C, Mahajan, P, Daga, N, Petrie, K, Alfano, I, Canning, P, Krojer, T, Vollmar, M, Knapp, S, von Delft, F, Weigelt, J, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A, Structural Genomics Consortium (SGC) | Deposit date: | 2010-04-30 | Release date: | 2010-06-23 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.15 Å) | Cite: | A new class of small molecule inhibitor of BMP signaling. Plos One, 8, 2013
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2YPT
| Crystal structure of the human nuclear membrane zinc metalloprotease ZMPSTE24 mutant (E336A) in complex with a synthetic CSIM tetrapeptide from the C-terminus of prelamin A | Descriptor: | CAAX PRENYL PROTEASE 1 HOMOLOG, PRELAMIN-A/C, ZINC ION | Authors: | Pike, A.C.W, Dong, Y.Y, Quigley, A, Dong, L, Savitsky, P, Cooper, C.D.O, Chaikuad, A, Goubin, S, Shrestha, L, Li, Q, Mukhopadhyay, S, Yang, J, Xia, X, Shintre, C.A, Barr, A.J, Berridge, G, Chalk, R, Bray, J.E, von Delft, F, Bullock, A, Bountra, C, Arrowsmith, C.H, Edwards, A, Burgess-Brown, N, Carpenter, E.P. | Deposit date: | 2012-11-01 | Release date: | 2012-12-05 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (3.8 Å) | Cite: | The Structural Basis of Zmpste24-Dependent Laminopathies. Science, 339, 2013
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