Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	-	578	4p16.3	GRK4	G protein-coupled receptor kinase 4
Mouse	-	574	5 17.91 cM	Grk4	G protein-coupled receptor kinase 4
Rat	-	575	14q21	Grk4	G protein-coupled receptor kinase 4

Previous and Unofficial Names

GPRK2L | G protein-coupled receptor kinase 2, groucho gene related | GPRK4

Database Links
Alphafold	P32298 (Hs), O70291 (Mm), P70507 (Rn)
BRENDA	2.7.11.16
ChEMBL Target	CHEMBL5861 (Hs)
Ensembl Gene	ENSG00000125388 (Hs), ENSMUSG00000052783 (Mm), ENSRNOG00000011847 (Rn)
Entrez Gene	2868 (Hs), 14772 (Mm), 59077 (Rn)
Human Protein Atlas	ENSG00000125388 (Hs)
KEGG Enzyme	2.7.11.16
KEGG Gene	hsa:2868 (Hs), mmu:14772 (Mm), rno:59077 (Rn)
OMIM	137026 (Hs)
Pharos	P32298 (Hs)
RefSeq Nucleotide	NM_001004056 (Hs), NM_001080743 (Mm), NM_019497 (Mm), NM_022928 (Rn)
RefSeq Protein	NP_001004056 (Hs), NP_001074212 (Mm), NP_062370 (Mm), NP_075217 (Rn)
UniProtKB	P32298 (Hs), O70291 (Mm), P70507 (Rn)
Wikipedia	GRK4 (Hs)

Enzyme Reaction
EC Number: 2.7.11.16

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols	View all chemical structures	Click column headers to sort
Ligand Sp. Action Value Parameter Reference balanol Hs Inhibition 6.6 pIC50 3 ⤷ pIC50 6.6 (IC50 2.6x10-7 M) [3] Description: Measuring inhibition of human GRK-4-mediated phosphorylation of bovine tubulin dimers.

DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform. http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan Reference: 2,4
Key to terms and symbols		Click column headers to sort
Target used in screen: GRK4
Ligand Sp. Type Action Value Parameter lestaurtinib Hs Inhibitor Inhibition 7.9 pKd staurosporine Hs Inhibitor Inhibition 7.4 pKd KW-2449 Hs Inhibitor Inhibition 7.2 pKd dovitinib Hs Inhibitor Inhibition 7.0 pKd midostaurin Hs Inhibitor Inhibition 7.0 pKd sunitinib Hs Inhibitor Inhibition 6.8 pKd fedratinib Hs Inhibitor Inhibition 6.8 pKd SU-14813 Hs Inhibitor Inhibition 6.4 pKd tozasertib Hs Inhibitor Inhibition 6.4 pKd PHA-665752 Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service. A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform. http://www.millipore.com/techpublications/tech1/pf3036 http://www.reactionbiology.com/webapps/main/pages/kinase.aspx Reference: ...1
Key to terms and symbols		Click column headers to sort
Target used in screen: nd/GRK4
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM staurosporine Hs Inhibitor Inhibition 20.5 Syk inhibitor Hs Inhibitor Inhibition 40.4 K-252a Hs Inhibitor Inhibition 44.1 PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 68.4 JAK inhibitor I Hs Inhibitor Inhibition 74.2 indirubin derivative E804 Hs Inhibitor Inhibition 74.7 Gö 6976 Hs Inhibitor Inhibition 75.1 sunitinib Hs Inhibitor Inhibition 75.8 Ro-32-0432 Hs Inhibitor Inhibition 76.4 SB 218078 Hs Inhibitor Inhibition 77.0
Displaying the top 10 most potent ligands  View all ligands in screen »

Immuno Process Associations

Immuno Process:  Antigen presentation