Structure of PDB 4ctc Chain A

Receptor sequence
>4ctcA (length=288) Species: 9606 (Homo sapiens) [Search protein sequence]
PNYCFAGKTSSISDLKEVPRKNITLIRGLGGEVYEGQVPLQVAVKTLPEV
CSEQDELDFLMEALIISKFNHQNIVRCIGVSLQSLPRFILLELMAGGDLK
SFLRETRPRPSQPSSLAMLDLLHVARDIACGCQYLEENHFIHRDIAARNC
LLTCPGPGRVAKIGDFGMARDIGGCAMLPVKWMPPEAFMEGIFTSKTDTW
SFGVLLWEIFSLGYMPYPSKSNQEVLEFVTSGGRMDPPKNCPGPVYRIMT
QCWQHQPEDRPNFAIILERIEYCTQDPDVINTALPIEY
3D structure
PDB4ctc Discovery of (10R)-7-Amino-12-Fluoro-2,10,16-Trimethyl-15-Oxo-10,15,16,17-Tetrahydro-2H-8,4-(Metheno)Pyrazolo[4,3-H][2,5,11]Benzoxadiazacyclotetradecine-3-Carbonitrile (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant Mutations.
ChainA
Resolution2.03 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D1249 A1251 R1253 N1254 D1270
Catalytic site (residue number reindexed from 1) D144 A146 R148 N149 D165
Enzyme Commision number 2.7.10.1: receptor protein-tyrosine kinase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 J99 A L1122 V1130 A1148 E1197 M1199 A1200 N1254 L1256 G1269 D1270 Y1401 L29 V33 A43 E92 M94 A95 N149 L151 G164 D165 Y288 BindingDB: IC50=5.8nM,Ki=<0.100000nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0004714 transmembrane receptor protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007169 cell surface receptor protein tyrosine kinase signaling pathway
Cellular Component
GO:0016020 membrane

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Molecular Function
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Biological Process
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Cellular Component
External links
PDB RCSB:4ctc, PDBe:4ctc, PDBj:4ctc
PDBsum4ctc
PubMed24819116
UniProtQ9UM73|ALK_HUMAN ALK tyrosine kinase receptor (Gene Name=ALK)

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