Structure of PDB 6gip Chain A

Receptor sequence
>6gipA (length=296) Species: 9606 (Homo sapiens) [Search protein sequence]
VARDITLLECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETELYN
TVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTLDTV
SCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCCIA
DLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVD
IWAFGLVLWEVARRMVSNGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQ
RPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALRIKKTLTKID
3D structure
PDB6gip Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
ChainA
Resolution2.17 Å
3D
structure
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Enzymatic activity
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 EUN A V222 A233 K235 L263 L281 T283 Y285 H286 G289 L343 V19 A30 K32 L60 L78 T80 Y82 H83 G86 L140 MOAD: ic50=0.042uM
PDBbind-CN: -logKd/Ki=7.38,IC50=0.042uM
BindingDB: Kd=640nM,IC50=42nM
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:6gip, PDBe:6gip, PDBj:6gip
PDBsum6gip
PubMed30085668
UniProtQ04771|ACVR1_HUMAN Activin receptor type-1 (Gene Name=ACVR1)

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