6UIP
DYRK1A Kinase Domain in Complex with a 6-azaindole Derivative, GNF2133.
Summary for 6UIP
Entry DOI | 10.2210/pdb6uip/pdb |
Descriptor | Dual specificity tyrosine-phosphorylation-regulated kinase 1A, 4-ethyl-N-{4-[1-(oxan-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]pyridin-2-yl}piperazine-1-carboxamide (2 entities in total) |
Functional Keywords | kinase, inhibitor, transferase |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 3 |
Total formula weight | 127548.21 |
Authors | DiDonato, M.,Spraggon, G. (deposition date: 2019-10-01, release date: 2020-03-04, Last modification date: 2023-11-15) |
Primary citation | Liu, Y.A.,Jin, Q.,Zou, Y.,Ding, Q.,Yan, S.,Wang, Z.,Hao, X.,Nguyen, B.,Zhang, X.,Pan, J.,Mo, T.,Jacobsen, K.,Lam, T.,Wu, T.Y.,Petrassi, H.M.,Bursulaya, B.,DiDonato, M.,Gordon, W.P.,Liu, B.,Baaten, J.,Hill, R.,Nguyen-Tran, V.,Qiu, M.,Zhang, Y.Q.,Kamireddy, A.,Espinola, S.,Deaton, L.,Ha, S.,Harb, G.,Jia, Y.,Li, J.,Shen, W.,Schumacher, A.M.,Colman, K.,Glynne, R.,Pan, S.,McNamara, P.,Laffitte, B.,Meeusen, S.,Molteni, V.,Loren, J. Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133. J.Med.Chem., 63:2958-2973, 2020 Cited by PubMed: 32077280DOI: 10.1021/acs.jmedchem.9b01624 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (3.7 Å) |
Structure validation
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