Structure of PDB 3zcl Chain A

Receptor sequence

>3zclA (length=289) Species: 9606 (Homo sapiens)

HIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLKKI
HCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLV
VLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDL
AARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESL
QTQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQP
EYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTF

3D structure

• PDB: 3zcl Lessons from (S)-6-(1-(6-(1-Methyl-1H-Pyrazol-4-Yl)-[1,2, 4]Triazolo[4,3-B]Pyridazin-3-Yl)Ethyl)Quinoline (Pf-04254644), an Inhibitor of Receptor Tyrosine Kinase C-met with High Protein Kinase Selectivity But Broad Phosphodiesterase Family Inhibition Leading to Myocardial Degeneration in Rats.
• Chain: A
• Resolution: 1.4 Å

Enzymatic activity

• Catalytic site (original residue number in PDB): D1204 A1206 R1208 N1209 D1222 A1243
• Catalytic site (residue number reindexed from 1): D149 A151 R153 N154 D167 A188
• 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	5TF	A	I1084 A1108 L1157 M1160 M1211 A1221 D1222 Y1230 F1344	I33 A53 L102 M105 M156 A166 D167 Y175 F289	MOAD: Ki=0.0101uM PDBbind-CN: -logKd/Ki=8.00,Ki=10.1nM BindingDB: IC50=19nM,Ki=10nM

Gene Ontology

Molecular Function

• GO:0004672 protein kinase activity
• GO:0004713 protein tyrosine kinase activity
• GO:0005524 ATP binding

Biological Process

• GO:0006468 protein phosphorylation

External links

• PDB: RCSB:3zcl, PDBe:3zcl, PDBj:3zcl
• PDBsum: 3zcl
• PubMed: 23944843
• UniProt: P08581|MET_HUMAN Hepatocyte growth factor receptor (Gene Name=MET)