3EKN

Insulin receptor kinase complexed with an inhibitor

Summary for 3EKN

• Entry DOI: 10.2210/pdb3ekn/pdb
• Related: 3EKK 3ELJ
• Descriptor: Insulin receptor, 2-fluoro-6-{[2-({2-methoxy-4-[4-(1-methylethyl)piperazin-1-yl]phenyl}amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino}benzamide (3 entities in total)
• Functional Keywords: insulin, tyrosine kinase, atp-binding, carbohydrate metabolism, cleavage on pair of basic residues, diabetes mellitus, disease mutation, glycoprotein, kinase, membrane, nucleotide-binding, phosphoprotein, receptor, transferase, transmembrane, tyrosine-protein kinase
• Biological source: Homo sapiens (human)
• Cellular location: Membrane; Single-pass type I membrane protein: P06213
• Total number of polymer chains: 1
• Total formula weight: 35368.38

Authors

Chamberlain, S.,Atkins, C.,Deanda, F.,Dumble, M.,Gerding, R.,Groy, A.,Korenchuk, S.,Kumar, R.,Lei, H.,Mook, R.,Moorthy, G.,Redman, A.,Rowland, J.,Shewchuk, L. (deposition date: 2008-09-19, release date: 2008-12-30, Last modification date: 2023-08-30)

• Primary citation: Chamberlain, S.D.,Redman, A.M.,Wilson, J.W.,Deanda, F.,Shotwell, J.B.,Gerding, R.,Lei, H.,Yang, B.,Stevens, K.L.,Hassell, A.M.,Shewchuk, L.M.,Leesnitzer, M.A.,Smith, J.L.,Sabbatini, P.,Atkins, C.,Groy, A.,Rowand, J.L.,Kumar, R.,Mook, R.A.,Moorthy, G.,Patnaik, S.; Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.; Bioorg.Med.Chem.Lett., 19:360-364, 2009; PubMed: 19071018; DOI: 10.1016/j.bmcl.2008.11.077

Experimental method

X-RAY DIFFRACTION (2.2 Å)