Structure of PDB 3lcd Chain A

Receptor sequence
>3lcdA (length=290) Species: 9606 (Homo sapiens) [Search protein sequence]
GNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEATAFGLGKE
DAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGG
PVLVITEYCCYGDLLNFLRRKAEADLDPLELRDLLHFSSQVAQGMAFLAS
KNCIHRDVAARNVLLTNGHVAKIGDFGLARDIMSNYIVKGNARLPVKWMA
PESIFDCVYTVQSDVWSYGILLWEIFSLGLNPYPGILVNSKFYKLVKDGY
QMAQPAFAPKNIYSIMQACWALEPTHRPTFQQICSFLQEQ
3D structure
PDB3lcd Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode
ChainA
Resolution2.5 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D778 A780 R782 N783 D796 N814
Catalytic site (residue number reindexed from 1) D157 A159 R161 N162 D175 N191
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 BDY A L588 G589 A614 Y665 C666 G669 L785 L31 G32 A57 Y108 C109 G112 L164 MOAD: ic50=40nM
PDBbind-CN: -logKd/Ki=7.40,IC50=40nM
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

View graph for
Molecular Function

View graph for
Biological Process
External links
PDB RCSB:3lcd, PDBe:3lcd, PDBj:3lcd
PDBsum3lcd
PubMed20137931
UniProtP07333|CSF1R_HUMAN Macrophage colony-stimulating factor 1 receptor (Gene Name=CSF1R)

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