8PYN
 
 | | Human IGF1R with inhibitor 56 | | Descriptor: | 5,5-dimethyl-1-(1H-pyrrolo[2,3-b]pyridin-4-ylmethyl)-3-[4-(trifluoromethylsulfonyl)phenyl]imidazolidine-2,4-dione, CADMIUM ION, Insulin-like growth factor 1 receptor beta chain, ... | | Authors: | Dreyer, M.K, Wang, J, Elkins, J.M. | | Deposit date: | 2023-07-25 | | Release date: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.71 Å) | | Cite: | Human IGF1R with inhibitor 56
To Be Published
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4UN0
 | | Crystal structure of the human CDK12-cyclinK complex | | Descriptor: | CYCLIN-DEPENDENT KINASE 12, CYCLIN-K | | Authors: | Dixon Clarke, S.E, Elkins, J.M, Pike, A.C.W, Chaikuad, A, Goubin, S, Krojer, T, Sorrell, F.J, Nowak, R, Williams, E, Kopec, J, Mahajan, R.P, Burgess-Brown, N, Carpenter, E.P, Knapp, S, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bullock, A. | | Deposit date: | 2014-05-22 | | Release date: | 2014-06-04 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (3.15 Å) | | Cite: | Structures of the Cdk12/Cyck Complex with AMP-Pnp Reveal a Flexible C-Terminal Kinase Extension Important for ATP Binding.
Sci.Rep., 5, 2015
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4W9X
 | | Crystal Structure of BMP-2-inducible kinase in complex with baricitinib | | Descriptor: | 1,2-ETHANEDIOL, BMP-2-inducible protein kinase, Baricitinib | | Authors: | Sorrell, F.J, Elkins, J.M, Krojer, T, Williams, E, Savitsky, P, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2014-08-28 | | Release date: | 2014-09-10 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.14 Å) | | Cite: | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.
Structure, 24, 2016
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4WSQ
 | | Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with small molecule inhibitor | | Descriptor: | 1,2-ETHANEDIOL, AP2-associated protein kinase 1, K-252A, ... | | Authors: | Sorrell, F.J, Elkins, J.M, Krojer, T, Williams, E, Abdul, K, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2014-10-28 | | Release date: | 2014-11-05 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases.
Structure, 24, 2016
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2A72
 | | Structure of the regulator of G-protein signaling domain of RGS7 | | Descriptor: | CHLORIDE ION, Regulator of G-protein signalling 7 | | Authors: | Schoch, G.A, Johansson, C, Phillips, C, Debreczeni, J, Smee, C, Elkins, J.M, Sundstrom, M, Edwards, A, Arrowsmith, C, von Delft, F, Gileadi, O, Doyle, D.A, Structural Genomics Consortium (SGC) | | Deposit date: | 2005-07-04 | | Release date: | 2005-07-12 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits.
Proc.Natl.Acad.Sci.Usa, 105, 2008
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2AF0
 | | Structure of the Regulator of G-Protein Signaling Domain of RGS2 | | Descriptor: | Regulator of G-protein signaling 2 | | Authors: | Papagrigoriou, E, Johannson, C, Phillips, C, Smee, C, Elkins, J.M, Weigelt, J, Arrowsmith, C, Edwards, A, Sundstrom, M, Von Delft, F, Doyle, D.A, Structural Genomics Consortium (SGC) | | Deposit date: | 2005-07-25 | | Release date: | 2005-08-02 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural diversity in the RGS domain and its interaction with heterotrimeric G protein alpha-subunits.
Proc.Natl.Acad.Sci.Usa, 105, 2008
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6I2Y
 | | Human STK10 bound to Foretinib | | Descriptor: | N-(3-fluoro-4-{[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Serine/threonine-protein kinase 10 | | Authors: | Sorrell, F.J, Berger, B.-T, Oerum, S, von Delft, F, Bountra, C, Arrowsmith, C, Edwards, A.M, Knapp, S, Elkins, J.M. | | Deposit date: | 2018-11-02 | | Release date: | 2018-12-12 | | Method: | X-RAY DIFFRACTION (2.56 Å) | | Cite: | Human STK10 bound to GW683134
To Be Published
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6HVD
 | | Human SLK bound to a maleimide inhibitor | | Descriptor: | 1,2-ETHANEDIOL, 3-(1,3-benzothiazol-2-ylamino)-4-(2-methoxyphenyl)pyrrole-2,5-dione, STE20-like serine/threonine-protein kinase, ... | | Authors: | Sorrell, F.J, Berger, B.T, Salah, E, Serafim, R.A.M, Savitsky, P.A, Krojer, T, Bailey, H.J, Pinkas, D, Burgess-Brown, N.A, von Delft, F, Knapp, S, Arrowsmith, C, Bountra, C, Edwards, A.M, Elkins, J.M. | | Deposit date: | 2018-10-10 | | Release date: | 2018-10-17 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.63 Å) | | Cite: | Human SLK bound to a maleimide inhibitor
To Be Published
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6HXF
 | | Human STK10 bound to a maleimide inhibitor | | Descriptor: | 1,2-ETHANEDIOL, 3-(2-methoxyphenyl)-4-[[4-(phenylcarbonyl)phenyl]amino]pyrrole-2,5-dione, CHLORIDE ION, ... | | Authors: | Sorrell, F.J, Salah, E, Serafim, R.A.M, Savitsky, P.A, Krojer, T, Bailey, H.J, Pinkas, D, Burgess-Brown, N.A, von Delft, F, Knapp, S, Arrowsmith, C, Bountra, C, Edwards, A.M, Elkins, J.M. | | Deposit date: | 2018-10-17 | | Release date: | 2018-10-31 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.09 Å) | | Cite: | Human STK10 bound to a maleimide inhibitor
To Be Published
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6BQP
 | | Crystal Structure of the Human CAMKK2B in complex with Crenolanib | | Descriptor: | 1,2-ETHANEDIOL, 1-(2-{5-[(3-Methyloxetan-3-yl)methoxy]-1H-benzimidazol-1-yl}quinolin-8-yl)piperidin-4-amine, Calcium/calmodulin-dependent protein kinase kinase 2 | | Authors: | Counago, R.M, de Souza, G.P, dos Reis, C.V, Ramos, P.Z, Drewry, D, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2017-11-28 | | Release date: | 2017-12-13 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Crystal Structure of the Human CAMKK2B in complex with Crenolanib
To Be Published
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6BU6
 | | Crystal Structure of the Human vaccinia-related kinase bound to a bis-difluorophenol-aminopyridine inhibitor | | Descriptor: | 4,4'-(2-aminopyridine-3,5-diyl)bis(2,6-difluorophenol), CHLORIDE ION, GLYCEROL, ... | | Authors: | Counago, R.M, dos Reis, C.V, de Souza, G.P, Santiago, A.S, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2017-12-08 | | Release date: | 2017-12-20 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a bis-difluorophenol-aminopyridine inhibitor
To Be Published
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6BLE
 | | Crystal Structure of the Human CAMKK2B in complex with CP673451 | | Descriptor: | 1-{2-[5-(2-methoxyethoxy)-1H-benzimidazol-1-yl]quinolin-8-yl}piperidin-4-amine, Calcium/calmodulin-dependent protein kinase kinase 2, GLYCEROL | | Authors: | Counago, R.M, dos Reis, C.V, de Souza, G.P, Ramos, P.Z, Drewry, D, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2017-11-10 | | Release date: | 2017-11-29 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystal Structure of the Human CAMKK2B in complex with CP673451
To Be Published
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6BRC
 | | Crystal Structure of the Human CAMKK2B in complex with AP26113-analog (ALK-IN-1) | | Descriptor: | 5-chloro-N~2~-{4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl}-N~4~-[2-(dimethylphosphoryl)phenyl]pyrimidine-2,4-diamine, Calcium/calmodulin-dependent protein kinase kinase 2, SODIUM ION | | Authors: | Counago, R.M, dos Reis, C.V, de Souza, G.P, Ramos, P.Z, Drewry, D, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2017-11-30 | | Release date: | 2017-12-13 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Crystal Structure of the Human CAMKK2B in complex with AP26113-analog (ALK-IN-1)
To Be Published
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6BRU
 | | Crystal Structure of the Human vaccinia-related kinase bound to a (S)-2-phenylaminopteridinone inhibitor | | Descriptor: | (7S)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7,8-trimethyl-7,8-dihydropteridin-6(5H)-one, 1,2-ETHANEDIOL, SULFATE ION, ... | | Authors: | Counago, R.M, dos Reis, C.V, de Souza, G.P, Aquino, B, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2017-12-01 | | Release date: | 2017-12-13 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a (S)-2-phenylaminopteridinone inhibitor
To Be Published
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5MXX
 | | Crystal structure of human SR protein kinase 1 (SRPK1) in complex with compound 1 | | Descriptor: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 5-methyl-~{N}-[2-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl]furan-2-carboxamide, ... | | Authors: | Tallant, C, Redondo, C, Batson, J, Toop, H.D, Babaebi-Jadidib, R, Savitsky, P, Elkins, J.M, Newman, J.A, Burgess-Brown, N, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Bates, D.O, Morris, J.C, Knapp, S, Structural Genomics Consortium (SGC) | | Deposit date: | 2017-01-25 | | Release date: | 2017-05-24 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease.
ACS Chem. Biol., 12, 2017
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6CFM
 | | Crystal Structure of the Human vaccinia-related kinase bound to a propynyl-pteridinone inhibitor | | Descriptor: | (7R)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7,8-dimethyl-5-(prop-2-yn-1-yl)-7,8-dihydropteridin-6(5H)-one, CHLORIDE ION, GLYCEROL, ... | | Authors: | Counago, R.M, dos Reis, C.V, de Souza, G.P, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-02-15 | | Release date: | 2018-03-07 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.45 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a propynyl-pteridinone inhibitor
To Be Published
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6CD6
 | | Crystal Structure of the Human CAMKK1A in complex with GSK650394 | | Descriptor: | 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid, CHLORIDE ION, Calcium/calmodulin-dependent protein kinase kinase 1 | | Authors: | Santiago, A.S, Counago, R.M, Righetto, G.L, Ramos, P.Z, Silva, P.N.B, Drewry, D, Elkins, J.M, Massirer, K.B, Arruda, P, Edwards, A.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-02-08 | | Release date: | 2018-03-07 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Crystal Structure of the Human CAMKK1A in complex with GSK650394
To be Published
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5NKS
 | | Human Dihydropyrimidinase-related Protein 4 (DPYSL4, CRMP3, ULIP-4) | | Descriptor: | Dihydropyrimidinase-related protein 4 | | Authors: | Mathea, S, Elkins, J.M, Strain-Damerell, C, Salah, E, Borkowska, O, Chalk, R, Burgess-Brown, N, Pinkas, D.M, von Delft, F, Krojer, T, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S. | | Deposit date: | 2017-03-31 | | Release date: | 2017-11-01 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Human Dihydropyrimidinase-related Protein 4 (DPYSL4, CRMP3, ULIP-4)
To Be Published
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6CNH
 | | Human PRPF4B in complex with Rebastinib | | Descriptor: | 4-[4-({[3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide, SULFATE ION, Serine/threonine-protein kinase PRP4 homolog | | Authors: | Godoi, P.H.C, Santiago, A.S, Ramos, P.Z, Fala, A.M, Salmazo, A.P.T, Counago, R.M, Righetto, G.L, Silva, P.N.B, Gileadi, O, Guimaraes, C.R.W, Massirer, K.B, Arruda, P, Elkins, J.M, Edwards, A.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-03-08 | | Release date: | 2018-03-28 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Crystal structure of the human PRPF4B in complex with Rebastinib
To be Published
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6CQH
 | | Crystal Structure of the Human vaccinia-related kinase bound to a N-propynyl-N-ethyl-dihydropteridine inhibitor | | Descriptor: | (7R)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-8-ethyl-7-methyl-5-(prop-2-yn-1-yl)-7,8-dihydropteridin-6(5H)-one, ACETATE ION, CHLORIDE ION, ... | | Authors: | dos Reis, C.V, de Souza, G.P, Counago, R.M, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-03-15 | | Release date: | 2018-03-28 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a N-propynyl-N-ethyl-dihydropteridine inhibitor
To Be Published
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6CPY
 | | Structure of apo GRMZM2G135359 pseudokinase | | Descriptor: | GRMZM2G135359 pseudokinase | | Authors: | Aquino, B, Counago, R.M, Godoi, P.H.C, Massirer, K.B, Elkins, J.M, Arruda, P, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-03-14 | | Release date: | 2018-04-04 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Structure of apo GRMZM2G135359 pseudokinase
To be Published
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6CSW
 | | Crystal Structure of the Human vaccinia-related kinase bound to a N-methyl-N-propyl-dihydropteridine inhibitor | | Descriptor: | (7R)-5-butyl-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7,8-dimethyl-7,8-dihydropteridin-6(5H)-one, ACETATE ION, CHLORIDE ION, ... | | Authors: | dos Reis, C.V, de Souza, G.P, Counago, R.M, Chiodi, C.G, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-03-21 | | Release date: | 2018-04-04 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a N-methyl-N-propyl-dihydropteridine inhibitor
To Be Published
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6CMM
 | | Crystal Structure of the Human vaccinia-related kinase bound to a N,N-dipropynyl-dihydropteridine inhibitor | | Descriptor: | (7R)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7-methyl-5,8-di(prop-2-yn-1-yl)-7,8-dihydropteridin-6(5H)-one, ACETATE ION, DI(HYDROXYETHYL)ETHER, ... | | Authors: | dos Reis, C.V, de Souza, G.P, Counago, R.M, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-03-05 | | Release date: | 2018-03-21 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a N,N-dipropynyl-dihydropteridine inhibitor
To Be Published
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6DD4
 | | Crystal Structure of the Human vaccinia-related kinase bound to a N,N-dipropyl-dihydropteridine inhibitor | | Descriptor: | (7R)-2-[(3,5-difluoro-4-hydroxyphenyl)amino]-7-methyl-5,8-dipropyl-7,8-dihydropteridin-6(5H)-one, ACETATE ION, CHLORIDE ION, ... | | Authors: | dos Reis, C.V, Santiago, A.S, de Souza, G.P, Counago, R.M, Azevedo, A, Guimaraes, C, Mascarello, A, Gama, F, Ferreira, M, Massirer, K.B, Arruda, P, Edwards, A.M, Elkins, J.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-05-09 | | Release date: | 2018-05-23 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Crystal Structure of the Human vaccinia-related kinase bound to a N,N-dipropyl-dihydropteridine inhibitor
To Be Published
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6CCF
 | | Crystal Structure of the Human CAMKK1A in complex with Hesperadin | | Descriptor: | 1,2-ETHANEDIOL, Calcium/calmodulin-dependent protein kinase kinase 1, N-[2-OXO-3-((E)-PHENYL{[4-(PIPERIDIN-1-YLMETHYL)PHENYL]IMINO}METHYL)-2,6-DIHYDRO-1H-INDOL-5-YL]ETHANESULFONAMIDE, ... | | Authors: | Santiago, A.S, Counago, R.M, dos Reis, C.V, Ramos, P.Z, Silva, P.N.B, Drewry, D, Elkins, J.M, Massirer, K.B, Arruda, P, Edwards, A.M, Structural Genomics Consortium (SGC) | | Deposit date: | 2018-02-07 | | Release date: | 2018-03-07 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Crystal Structure of the Human CAMKK1A in complex with Hesperadin
To be Published
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