Structure of PDB 3tt0 Chain A

Receptor sequence
>3tt0A (length=305) Species: 9606 (Homo sapiens) [Search protein sequence]
SEYELPEDPRWELPRDRLVLGKPLGEGAFGQVVLAEAIGLDKDKPNRVTK
VAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNIINLLGACTQDGPLYVI
VEYASKGNLREYLQARRPPGLEYSYNPSHNPEEQLSSKDLVSCAYQVARG
MEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG
RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELF
KLLKEGHRMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVAL
TSNQE
3D structure
PDB3tt0 Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
ChainA
Resolution2.8 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) T521 L525 L528 G567 R576 S588 Q606 D623 A625 R627 N628 V629 D641 G697
Catalytic site (residue number reindexed from 1) T61 L65 L68 G107 R116 S128 Q146 D163 A165 R167 N168 V169 D181 G237
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 07J A V492 A512 K514 E531 M535 I545 V561 Y563 A564 G567 L630 A640 D641 V32 A52 K54 E71 M75 I85 V101 Y103 A104 G107 L170 A180 D181 PDBbind-CN: -logKd/Ki=9.05,IC50=0.9nM
BindingDB: IC50=1.0nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005007 fibroblast growth factor receptor activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

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Molecular Function
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Biological Process
External links
PDB RCSB:3tt0, PDBe:3tt0, PDBj:3tt0
PDBsum3tt0
PubMed21936542
UniProtP11362|FGFR1_HUMAN Fibroblast growth factor receptor 1 (Gene Name=FGFR1)

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