Structure of PDB 3kcf Chain A

Receptor sequence
>3kcfA (length=328) Species: 9606 (Homo sapiens) [Search protein sequence]
ISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVW
RGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDN
GTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEI
VGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDINHR
VGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHE
DYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMR
ECWYANGAARLTALRIKKTLSQLSQQEG
3D structure
PDB3kcf Pyrazolone based TGFbetaR1 kinase inhibitors.
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) D333 K335 N338 D351 T375
Catalytic site (residue number reindexed from 1) D163 K165 N168 D181 T203
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 JZO A I211 A230 K232 L260 S280 Y282 H283 K337 L340 D351 I41 A60 K62 L90 S110 Y112 H113 K167 L170 D181 PDBbind-CN: -logKd/Ki=7.46,Ki=0.035uM
BindingDB: IC50=3690nM,Ki=35nM
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:3kcf, PDBe:3kcf, PDBj:3kcf
PDBsum3kcf
PubMed19914068
UniProtP36897|TGFR1_HUMAN TGF-beta receptor type-1 (Gene Name=TGFBR1)

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