Structure of PDB 6ek3 Chain A

Receptor sequence
>6ek3A (length=194) Species: 9606 (Homo sapiens) [Search protein sequence]
LPEHWTDMNHQLFCMVQLEPGQSEYNTIKDKFTRTCSSYAIEKIERIQNA
FLWQSYQVKKRQMDIKNDHKNNERLLFHGTDADSVPYVNQHGFNRSCNAV
SYGKGTYFAVDASLSAKDTYSKPDSNGRKHMYVVRVLTGVFTKGRAGLVT
PPPKNPHNPTDLFDSVTNNTRSPKLFVVFFDNQAYPEYLITFTA
3D structure
PDB6ek3 4-(Phenoxy) and 4-(benzyloxy)benzamides as potent and selective inhibitors of mono-ADP-ribosyltransferase PARP10/ARTD10.
ChainA
Resolution1.6 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 2.4.2.-
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 OUL A H364 G365 Y396 F397 A398 S404 Y409 L464 H78 G79 Y107 F108 A109 S115 Y120 L175 PDBbind-CN: -logKd/Ki=6.48,IC50=330nM
BindingDB: IC50=>10000nM
Gene Ontology
Molecular Function
GO:0003950 NAD+-protein poly-ADP-ribosyltransferase activity

View graph for
Molecular Function
External links
PDB RCSB:6ek3, PDBe:6ek3, PDBj:6ek3
PDBsum6ek3
PubMed30006177
UniProtQ460N3|PAR15_HUMAN Protein mono-ADP-ribosyltransferase PARP15 (Gene Name=PARP15)

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