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
Summary for 5QTZ
Entry DOI | 10.2210/pdb5qtz/pdb |
Group deposition | Crystal Structures of TGF-beta receptor type 1 kinase domain (T204D) (G_1002109) |
Descriptor | TGF-beta receptor type-1, 6-[1-(2,2-difluoroethyl)-4-(6-methylpyridin-2-yl)-1H-imidazol-5-yl]imidazo[1,2-a]pyridine, GLYCEROL, ... (4 entities in total) |
Functional Keywords | alk5, sb431542, kinase domain, transferase-transferase inhibitor complex, transferase |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 1 |
Total formula weight | 35781.10 |
Authors | Sheriff, S. (deposition date: 2019-11-19, release date: 2020-02-05, Last modification date: 2024-05-22) |
Primary citation | Velaparthi, U.,Darne, C.P.,Warrier, J.,Liu, P.,Rahaman, H.,Augustine-Rauch, K.,Parrish, K.,Yang, Z.,Swanson, J.,Brown, J.,Dhar, G.,Anandam, A.,Holenarsipur, V.K.,Palanisamy, K.,Wautlet, B.S.,Fereshteh, M.P.,Lippy, J.,Tebben, A.J.,Sheriff, S.,Ruzanov, M.,Yan, C.,Gupta, A.,Gupta, A.K.,Vetrichelvan, M.,Mathur, A.,Gelman, M.,Singh, R.,Kinsella, T.,Murtaza, A.,Fargnoli, J.,Vite, G.,Borzilleri, R.M. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF beta R1 Inhibitor as an Immuno-oncology Agent. Acs Med.Chem.Lett., 11:172-178, 2020 Cited by PubMed: 32071685DOI: 10.1021/acsmedchemlett.9b00552 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.83 Å) |
Structure validation
Download full validation report