3KRJ

cFMS tyrosine kinase in complex with 4-Cyano-1H-imidazole-2-carboxylic acid (2-cyclohex-1-enyl-4-piperidin-4-yl-phenyl)-amide

Summary for 3KRJ

• Entry DOI: 10.2210/pdb3krj/pdb
• Related: 3KRL
• Descriptor: Macrophage colony-stimulating factor 1 receptor, Basic fibroblast growth factor receptor 1, ACETATE ION, 4-cyano-N-(2-cyclohex-1-en-1-yl-4-piperidin-4-ylphenyl)-1H-imidazole-2-carboxamide, ... (4 entities in total)
• Functional Keywords: kinase, inhibitor, chimera, atp-binding, disulfide bond, glycoprotein, immunoglobulin domain, membrane, nucleotide-binding, phosphoprotein, proto-oncogene, receptor, transferase, transmembrane, tyrosine-protein kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• Biological source: Homo sapiens (human); More
• Cellular location: Cell membrane; Single-pass type I membrane protein: P07333
• Total number of polymer chains: 1
• Total formula weight: 38498.99

Authors

Schubert, C. (deposition date: 2009-11-18, release date: 2010-12-01, Last modification date: 2023-09-06)

• Primary citation: Illig, C.R.,Manthey, C.L.,Wall, M.J.,Meegalla, S.K.,Chen, J.,Wilson, K.J.,Ballentine, S.K.,Desjarlais, R.L.,Schubert, C.,Crysler, C.S.,Chen, Y.,Molloy, C.J.,Chaikin, M.A.,Donatelli, R.R.,Yurkow, E.,Zhou, Z.,Player, M.R.,Tomczuk, B.E.; Optimization of a Potent Class of Arylamide Colony-Stimulating Factor-1 Receptor Inhibitors Leading to Anti-inflammatory Clinical Candidate 4-Cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).; J.Med.Chem., 54:7860-7883, 2011; PubMed: 22039836; DOI: 10.1021/jm200900q

Experimental method

X-RAY DIFFRACTION (2.1 Å)