Structure of PDB 6gi6 Chain A

Receptor sequence
>6gi6A (length=298) Species: 9606 (Homo sapiens) [Search protein sequence]
RTVARDITLLECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETEL
YNTVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTLD
TVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCC
IADLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKR
VDIWAFGLVLWEVARRMVSNGIVEDYKPPFYDVVPNDPSFEDMRKVVCVD
QQRPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALRIKKTLTKID
3D structure
PDB6gi6 Novel Quinazolinone Inhibitors of ALK2 Flip between Alternate Binding Modes: Structure-Activity Relationship, Structural Characterization, Kinase Profiling, and Cellular Proof of Concept.
ChainA
Resolution1.98 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 EZB A V222 K235 L263 T283 Y285 H286 L343 A353 V21 K34 L62 T82 Y84 H85 L142 A152 MOAD: ic50=0.194uM
PDBbind-CN: -logKd/Ki=6.71,IC50=0.194uM
BindingDB: IC50=194nM
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:6gi6, PDBe:6gi6, PDBj:6gi6
PDBsum6gi6
PubMed30085668
UniProtQ04771|ACVR1_HUMAN Activin receptor type-1 (Gene Name=ACVR1)

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