6MT0
Crystal structure of human Pim-1 kinase in complex with a quinazolinone-pyrrolodihydropyrrolone inhibitor
Summary for 6MT0
Entry DOI | 10.2210/pdb6mt0/pdb |
Descriptor | Serine/threonine-protein kinase pim-1, 3-(1-methylcyclopropyl)-2-[(1-methylcyclopropyl)amino]-8-[(6R)-6-methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4-b]pyrrol-2-yl]quinazolin-4(3H)-one, GLYCEROL, ... (4 entities in total) |
Functional Keywords | serine/threonine protein kinase, transferase |
Biological source | Homo sapiens (Human) |
Total number of polymer chains | 1 |
Total formula weight | 33652.09 |
Authors | Mohr, C. (deposition date: 2018-10-18, release date: 2019-01-16, Last modification date: 2024-03-13) |
Primary citation | Wang, H.L.,Andrews, K.L.,Booker, S.K.,Canon, J.,Cee, V.J.,Chavez Jr., F.,Chen, Y.,Eastwood, H.,Guerrero, N.,Herberich, B.,Hickman, D.,Lanman, B.A.,Laszlo 3rd., J.,Lee, M.R.,Lipford, J.R.,Mattson, B.,Mohr, C.,Nguyen, Y.,Norman, M.H.,Pettus, L.H.,Powers, D.,Reed, A.B.,Rex, K.,Sastri, C.,Tamayo, N.,Wang, P.,Winston, J.T.,Wu, B.,Wu, Q.,Wu, T.,Wurz, R.P.,Xu, Y.,Zhou, Y.,Tasker, A.S. Discovery of ( R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4- b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3 H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies. J. Med. Chem., 62:1523-1540, 2019 Cited by PubMed: 30624936DOI: 10.1021/acs.jmedchem.8b01733 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.2 Å) |
Structure validation
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