Uniprot accession / id : Q8VEB1  OR   Uniprot accession / id : P34947
 
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Entry Information
Entry status  (1)
REL
(10)
 
Experimental methods  (1)
X-ray diffraction
(10)
 
Authors  (20)
Chen Y
(7)
Gadi RK
(7)
Ghosh AK
(7)
Sonawane A
(7)
Tesmer JJG
(7)
Gamage SP
(5)
Tesmer JG
(5)
Benovic JL
(3)
Bhardwaj A
(3)
Komolov KE
(3)
Manda R
(2)
Chung KY
(1)
Dror RO
(1)
Duc NM
(1)
Laurinavichyute DK
(1)
Lou HJ
(1)
Sulon S
(1)
Sulon SM
(1)
Turk BE
(1)
van Keulen SC
(1)
 
Homo / hetero assembly  (2)
homo
(9)
hetero
(1)
 
Assembly composition  (2)
protein structure
(9)
protein/protein complex
(1)
 
Assembly polymer count  (2)
monomer
(9)
dimer
(1)
 
Resolution distribution
1.5 - 2
(2)
2.0 - 2.5
(2)
2.5 - 3
(5)
3.5 - 4
(1)
 
Release year distribution
2010 - 2015
(2)
2015 - 2020
(3)
2020 - 2025
(8)
2025 - 2030
(5)
 
Journal  (3)
Eur J Med Chem
(7)
J Biol Chem
(2)
Mol Cell
(1)
 
Macromolecules
Organism superkingdom  (1)
Eukaryota
(10)
 
Organism name  (1)
Homo sapiens
(10)
 
Molecule name  (2)
G protein-coupled receptor kinase 5
(10)
G protein-coupled receptor kinase GRK5
(10)
 
Molecule type  (1)
Protein
(10)
 
Gene names  (2)
GPRK5
(10)
GRK5
(10)
 
Interacting Molecules  (1)
EF-hand domain-containing protein
(1)
 
Interacting ligands  (9)
SGV : SANGIVAMYCIN
(2)
W3F : (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-[(4-{[(2S)-2-(furan-2-yl)-2-hydroxyacetyl]amino}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide
(2)
A1AQ6 : (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-({4-[(furan-2-carbonyl)amino]-3,5-dimethyl-1H-pyrrol-2-yl}methylidene)-2-oxo-3,7-dihydro-2H-indole-5-carboxamide
(1)
A1AQ7 : (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-({4-[(furan-3-carbonyl)amino]-3,5-dimethyl-1H-pyrrol-2-yl}methylidene)-2-oxo-3,7-dihydro-2H-indole-5-carboxamide
(1)
A1AQ8 : (3Z)-3-[(3,5-dimethyl-4-{[(2S)-5-oxooxolane-2-carbonyl]amino}-1H-pyrrol-2-yl)methylidene]-N-[(1R)-1-(4-fluorophenyl)ethyl]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide
(1)
A1AQ9 : (4S)-N-{5-[(Z)-(5-{[(1R)-1-(4-fluorophenyl)ethyl]carbamoyl}-2-oxo-2,7-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrol-3-yl}-2-methylimidazo[1,2-a]pyridine-3-carboxamide
(1)
ANP : PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER
(1)
MG : MAGNESIUM ION
(1)
W2T : (3Z)-3-{[4-(2-chloroacetamido)-3,5-dimethyl-1H-pyrrol-2-yl]methylidene}-N-[(1R)-1-(4-fluorophenyl)ethyl]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide
(1)
 
Function and Biology
EC number / name  (1)
2.7.11.16 : G-protein-coupled receptor kinase
(10)
 
Biological function  (12)
ATP binding
(10)
G protein-coupled receptor kinase activity
(10)
beta-adrenergic receptor kinase activity
(10)
kinase activity
(10)
lipid binding
(10)
nucleotide binding
(10)
phospholipid binding
(10)
protein binding
(10)
protein kinase C binding
(10)
protein kinase activity
(10)
protein serine/threonine kinase activity
(10)
transferase activity
(10)
 
Biological process  (14)
G protein-coupled receptor signaling pathway
(10)
Wnt signaling pathway
(10)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway
(10)
apoptotic process
(10)
fat cell differentiation
(10)
negative regulation of apoptotic process
(10)
positive regulation of cell population proliferation
(10)
protein autophosphorylation
(10)
regulation of G protein-coupled receptor signaling pathway
(10)
regulation of cell cycle
(10)
regulation of signal transduction
(10)
tachykinin receptor signaling pathway
(10)
protein phosphorylation
(5)
signal transduction
(5)
 
Biological cell component  (7)
cytoplasm
(10)
cytosol
(10)
membrane
(10)
nuclear membrane
(10)
nuclear speck
(10)
nucleus
(10)
plasma membrane
(10)
 
Sequence and Structure classification
CATH class  (2)
Alpha Beta
(2)
Mainly Alpha
(2)
 
CATH topology  (3)
Phosphorylase Kinase; domain 1
(2)
Regulator of G-protein Signalling 4; domain 2
(2)
Transferase(Phosphotransferase); domain 1
(2)
 
Pfam accession / name  (2)
PF00069 : Pkinase
(10)
PF00615 : RGS
(10)
 
Experimental Information
Diffraction protocol  (1)
Single wavelength
(10)
 
Diffraction radiation source type  (2)
Synchrotron
(9)
Rotating anode
(1)
 
Diffraction source  (6)
NSLS-II BEAMLINE 17-ID-2
(3)
NSLS BEAMLINE X6A
(2)
NSLS-II BEAMLINE 17-ID-1
(2)
APS BEAMLINE 23-ID-B
(1)
APS BEAMLINE 23-ID-D
(1)
RIGAKU MICROMAX-007 HF
(1)
 
Synchrotron site  (3)
NSLS-II
(5)
APS
(2)
NSLS
(2)
 
Diffraction detector type  (2)
Pixel
(8)
CCD
(2)
 
Refinement software  (1)
PHENIX
(10)
 
Representative Structures
Representative Structures
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Entries 1 to 10 of 10
Entries 1 to 10 of 10
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Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 D311N in Complex with CCG273441
Chen Y, Tesmer JJG
Eur J Med Chem (2023) [PMID: 38016297  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: W2T    W2T   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.5Å resolution
Released: 13 Dec 2023
Model geometry
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8uap
8uap
8uap
Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL019-21
Chen Y, Tesmer JJG
Eur J Med Chem (2025) [PMID: 39549325  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: W3F    W3F   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.8Å resolution
Released: 19 Feb 2025
Model geometry
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9bre
9bre
9bre
Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL093-22
Chen Y, Tesmer JJG
Eur J Med Chem (2025) [PMID: 39549325  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: A1AQ9    A1AQ9   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.8Å resolution
Released: 19 Feb 2025
Model geometry
Fit model/data
9brj
9brj
9brj
Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL055-22
Chen Y, Tesmer JJG
Eur J Med Chem (2025) [PMID: 39549325  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: A1AQ6    A1AQ6   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.7Å resolution
Released: 19 Feb 2025
Model geometry
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9brg
9brg
9brg
Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL064-22
Chen Y, Tesmer JJG
Eur J Med Chem (2025) [PMID: 39549325  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: A1AQ8    A1AQ8   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.9Å resolution
Released: 19 Feb 2025
Model geometry
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9bri
9bri
9bri
Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL056-21
Chen Y, Tesmer JJG
Eur J Med Chem (2025) [PMID: 39549325  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: A1AQ7    A1AQ7   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
3.69Å resolution
Released: 19 Feb 2025
Model geometry
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9brh
9brh
9brh
Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21
Chen Y, Tesmer JJG
Eur J Med Chem (2023) [PMID: 38016297  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: W3F    W3F   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.8Å resolution
Released: 13 Dec 2023
Model geometry
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8uaq
8uaq
8uaq
Crystal Structure of G Protein-Coupled Receptor Kinase 5 (GRK5) in Complex with Calmodulin (CaM)
Bhardwaj A, Komolov KE, Sulon S, Benovic JL
Mol Cell (2021) [PMID: 33321095  ]
Assembly composition: protein/protein complex
Bound ligands: CA    SGV    CA    SGV   
Modified residues: ACE    ACE   
Assembly name: G protein-coupled receptor kinase 5 and EF-hand domain-containing protein (Preferred)   search this complex
PDBe complex ID: PDB-CPX-100715 (Preferred)   search this ID
PDBe-KB: P34947    A0A094NJQ6   
X-ray diffraction
1.96Å resolution
Released: 9 Dec 2020
Model geometry
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6pjx
6pjx
6pjx
Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with AMP-PNP
Bhardwaj A, Komolov KE, Benovic JL
J Biol Chem (2015) [PMID: 26032409  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: ANP    MG    ANP    MG   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
1.802Å resolution
Released: 10 Jun 2015
Model geometry
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4tnd
4tnd
4tnd
Crystal Structure of G Protein-Coupled Receptor Kinase 5 in Complex with Sangivamycin
Bhardwaj A, Komolov KE, Benovic JL
J Biol Chem (2015) [PMID: 26032409  ]
Source organism: Homo sapiens  
Assembly composition: protein only structure
Bound ligands: SGV    SGV   
Assembly name: G protein-coupled receptor kinase 5 (Preferred)   search this complex
PDBe complex ID: PDB-CPX-152756 (Preferred)   search this ID
PDBe-KB: P34947   
X-ray diffraction
2.113Å resolution
Released: 10 Jun 2015
Model geometry
Fit model/data
4tnb
4tnb
4tnb
Entries 1 to 10 of 10
Entries 1 to 10 of 10