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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 DOI10.2210/pdb5qtz/pdb
Group depositionCrystal Structures of TGF-beta receptor type 1 kinase domain (T204D) (G_1002109)
DescriptorTGF-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 Keywordsalk5, sb431542, kinase domain, transferase-transferase inhibitor complex, transferase
Biological sourceHomo sapiens (Human)
Total number of polymer chains1
Total formula weight35781.10
Authors
Sheriff, S. (deposition date: 2019-11-19, release date: 2020-02-05, Last modification date: 2021-11-17)
Primary citationVelaparthi, 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: 32071685
DOI: 10.1021/acsmedchemlett.9b00552
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.83 Å)
Structure validation

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