Brand  (β version)

PDB ID: 6MEP

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Ligands
Code Name Style Show Link
9VS Cis-4-[(2-[(4-{[4-(1,3-dioxolan-2-yl)pyridin-2-yl]ethynyl}phenyl)amino]-5-{4-[(4-methylpiperazin-1-yl)methyl]phenyl}pyrimidin-4-yl)amino]cyclohexan-1-ol PoSSuM
CL Chloride ion PoSSuM
MG Magnesium ion PoSSuM
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Structure summary

Code : 6MEP   PDBj   RCSB PDB   PDBe
Header : Transferase/Transferase Inhibitor
Title : Crystal structure of the catalytic domain of the proto-oncogene tyrosine-protein kinase MER in complex with inhibitor UNC3437
Release Data : 2019-09-11
Compound :
mol_id molecule chains synonym
1 Tyrosine-protein kinase Mer A,B Proto-oncogene c-Mer,Receptor tyrosine kinase MerTK
ec: 2.7.10.1
fragment: catalytic domain
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: MERTK, MER
Authors : Da, C., Zhang, D., Stashko, M.A., Cheng, A., Hunter, D., Norris-Drouin, J., Graves, L., Machius, M., Miley, M.J., DeRyckere, D., Earp, H.S., Graham, D.K., Frye, S.V., Wang, X., Kireev, D.
Keywords : Macrocyclic, Drug Design, Fibrinolytic Agents, Humans, Models, Molecular, Protein Kinase Inhibitors, Proto-Oncogene Proteins, Pyrimidines, Receptor Protein-Tyrosine Kinases, Structure-Activity Relationship, Thrombosis, Transferase-Transferase Inhibitor complex
Exp. method : X-RAY DIFFRACTION ( 2.8930 Å )
Citation :

Data-Driven Construction of Antitumor Agents with Controlled Polypharmacology.

Da, C.,Zhang, D.,Stashko, M.  et al.
(2019)  J.Am.Chem.Soc.  141 : 15700 - 15709

PubMed: 31497954
DOI: 10.1021/jacs.9b08660

Reaction

Chain : A, B
UniProt : Q12866 (MERTK_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.1 PROSITE-ProRule:PRU10028
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