Structure of PDB 3gxl Chain A

Receptor sequence
>3gxlA (length=285) Species: 9606 (Homo sapiens) [Search protein sequence]
IARTIVLQESIGKGRFGEVWRGKWEVAVKIFSSREERSWFREAEIYQTVM
LRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMI
KLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLG
LAVRHDSATDTIDRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVF
WEIARRCSIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRSCEA
LRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQ
3D structure
PDB3gxl Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors
ChainA
Resolution1.8 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D133 K135 N138 D151 T175
Catalytic site (residue number reindexed from 1) D130 K132 N135 D148 T167
Enzyme Commision number 2.7.11.30: receptor protein serine/threonine 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 QIG A I11 G14 A30 K32 L78 S80 Y82 H83 L140 D151 I11 G14 A27 K29 L75 S77 Y79 H80 L137 D148 MOAD: ic50=0.025uM
PDBbind-CN: -logKd/Ki=7.60,IC50=0.025uM
BindingDB: IC50=>10000nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004675 transmembrane receptor protein serine/threonine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007178 cell surface receptor protein serine/threonine 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:3gxl, PDBe:3gxl, PDBj:3gxl
PDBsum3gxl
PubMed19285388
UniProtP36897|TGFR1_HUMAN TGF-beta receptor type-1 (Gene Name=TGFBR1)

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