3O23

Human unphosphorylated IGF1-R Kinase domain in complex with an hydantoin inhibitor

Summary for 3O23

• Entry DOI: 10.2210/pdb3o23/pdb
• Related: 3LVP
• Descriptor: Insulin-like growth factor 1 receptor, (5S)-5-methyl-1-(quinolin-4-ylmethyl)-3-{4-[(trifluoromethyl)sulfonyl]phenyl}imidazolidine-2,4-dione (3 entities in total)
• Functional Keywords: protein kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Membrane; Single-pass type I membrane protein: P08069
• Total number of polymer chains: 1
• Total formula weight: 35258.34

Authors

Maignan, S.,Guilloteau, J.P.,Dupuy, A. (deposition date: 2010-07-22, release date: 2011-05-04, Last modification date: 2023-11-01)

Primary citation

Lesuisse, D.,Mauger, J.,Nemecek, C.,Maignan, S.,Boiziau, J.,Harlow, G.,Hittinger, A.,Ruf, S.,Strobel, H.,Nair, A.,Ritter, K.,Malleron, J.L.,Dagallier, A.,El-Ahmad, Y.,Guilloteau, J.P.,Guizani, H.,Bouchard, H.,Venot, C.
Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: Advantages in comparison with competitive inhibitors
Bioorg.Med.Chem.Lett., 21:2224-2228, 2011

PubMed Abstract: A new series of IGF-1R inhibitors related to hydantoins were identified from a lead originating from HTS. Their noncompetitive property as well as their slow binding characteristics provided a series of compounds with unique selectivity and excellent cellular activities.

PubMed: 21441024
DOI: 10.1016/j.bmcl.2011.03.003

Experimental method

X-RAY DIFFRACTION (2.1 Å)