4MBI

Discovery of Pyrazolo[1,5a]pyrimidine-based Pim1 Inhibitors

Summary for 4MBI

• Entry DOI: 10.2210/pdb4mbi/pdb
• Related: 4MBL
• Descriptor: Serine/threonine-protein kinase pim-1, N,N-dimethyl-N'-[3-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-5-yl]ethane-1,2-diamine (3 entities in total)
• Functional Keywords: kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Isoform 2: Cytoplasm. Isoform 1: Cell membrane: P11309
• Total number of polymer chains: 1
• Total formula weight: 34117.67

Authors

Azevedo, R.,Fischmann, T.O. (deposition date: 2013-08-19, release date: 2013-09-18, Last modification date: 2024-02-28)

Primary citation

Dwyer, M.P.,Keertikar, K.,Paruch, K.,Alvarez, C.,Labroli, M.,Poker, C.,Fischmann, T.O.,Mayer-Ezell, R.,Bond, R.,Wang, Y.,Azevedo, R.,Guzi, T.J.
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: A template-based approach.
Bioorg.Med.Chem.Lett., 23:6178-6182, 2013

PubMed Abstract: The synthesis and hit-to-lead SAR development from a pyrazolo[1,5-a]pyrimidine-derived hit 5 to the identification of a series of potent, pan-Pim inhibitors such as 11j are described.

PubMed: 24091081
DOI: 10.1016/j.bmcl.2013.08.110

Experimental method

X-RAY DIFFRACTION (2.3 Å)