GRK7

Summary

GRK7 (G protein-coupled receptor kinase 7, HGNC:17031) is a protein-coding gene on chromosome 3q23, encoding Rhodopsin kinase GRK7 (Q8WTQ7). Retina-specific kinase involved in the shutoff of the photoresponse and adaptation to changing light conditions via cone opsin phosphorylation, including rhodopsin (RHO).

This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. It is specifically expressed in the retina and the encoded protein has been shown to phosphorylate cone opsins and initiate their deactivation.

Source: NCBI Gene 131890 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 88 total
• Druggable target: yes — 19 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_139209

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17031
Approved symbol	GRK7
Name	G protein-coupled receptor kinase 7
Location	3q23
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000114124
Ensembl biotype	protein_coding
OMIM	606987
Entrez	131890

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000264952, ENST00000682958

RefSeq mRNA: 1 — MANE Select: NM_139209 NM_139209

CCDS: CCDS3120

Canonical transcript exons

ENST00000682958 — 6 exons

Exon	Start	End
ENSE00000779066	141780374	141780811
ENSE00001077552	141807645	141807919
ENSE00003916660	141816714	141819352
ENSE00003918335	141763408	141765738
ENSE00003921589	141774580	141774680
ENSE00003922459	141778172	141778896

Expression profiles

Bgee: expression breadth broad, 28 present calls, max score 72.95.

Top tissues by expression

195 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
buccal mucosa cell	CL:0002336	72.95	silver quality
granulocyte	CL:0000094	47.67	silver quality
gastrocnemius	UBERON:0001388	46.42	gold quality
muscle of leg	UBERON:0001383	45.97	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	44.32	silver quality
hindlimb stylopod muscle	UBERON:0004252	43.97	silver quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	43.37	gold quality
cortical plate	UBERON:0005343	43.36	gold quality
colonic epithelium	UBERON:0000397	42.81	gold quality
secondary oocyte	CL:0000655	42.57	gold quality
islet of Langerhans	UBERON:0000006	42.56	silver quality
oviduct epithelium	UBERON:0004804	41.52	gold quality
sural nerve	UBERON:0015488	41.43	gold quality
vastus lateralis	UBERON:0001379	41.41	gold quality
quadriceps femoris	UBERON:0001377	41.37	gold quality
superficial temporal artery	UBERON:0001614	41.33	gold quality
monocyte	CL:0000576	41.16	gold quality
subthalamic nucleus	UBERON:0001906	41.11	gold quality
palpebral conjunctiva	UBERON:0001812	41.10	gold quality
mucosa of paranasal sinus	UBERON:0005030	40.98	gold quality
amniotic fluid	UBERON:0000173	40.69	gold quality
ganglionic eminence	UBERON:0004023	40.63	gold quality
jejunal mucosa	UBERON:0000399	40.59	gold quality
biceps brachii	UBERON:0001507	40.57	gold quality
epithelium of nasopharynx	UBERON:0001951	40.45	gold quality
myocardium	UBERON:0002349	40.45	gold quality
gingival epithelium	UBERON:0001949	40.43	gold quality
germinal epithelium of ovary	UBERON:0001304	40.33	gold quality
esophagus squamous epithelium	UBERON:0006920	40.29	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	40.27	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-MTAB-7316	yes	25.42
E-ANND-3	yes	2.78
E-CURD-10	no	98.33

Regulation

Is transcription factor: no

Literature-anchored findings (GeneRIF, showing 3)

• Phosphorylation of GRK1 and GRK7 by PKA occurs in the dark, when cAMP levels in photoreceptor cells are elevated. (PMID:15946941)
• synthesis of 29 of GRK1 or GRK7 partial peptides that cover the entire sequence of GRK1/GRK7, to see which interacts with recoverin. (PMID:18266817)
• Defects in GRK1 or GRK7 cause patients to suffer from an inability to properly deactivate rhodopsin leading to problems with recovery and dark adaptation. (PMID:22183412)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
danio_rerio	grk7a	ENSDARG00000020602
danio_rerio	grk7b	ENSDARG00000055534

Paralogs (7): GRK3 (ENSG00000100077), GRK4 (ENSG00000125388), RSKR (ENSG00000167524), GRK2 (ENSG00000173020), GRK1 (ENSG00000185974), GRK6 (ENSG00000198055), GRK5 (ENSG00000198873)

Protein

Protein identifiers

Rhodopsin kinase GRK7 — Q8WTQ7 (reviewed: Q8WTQ7)

Alternative names: G protein-coupled receptor kinase 7, G protein-coupled receptor kinase GRK7

All UniProt accessions (1): Q8WTQ7

UniProt curated annotations — full annotation on UniProt →

Function. Retina-specific kinase involved in the shutoff of the photoresponse and adaptation to changing light conditions via cone opsin phosphorylation, including rhodopsin (RHO).

Subunit / interactions. Interacts (when prenylated) with PDE6D; this promotes release from membranes.

Subcellular location. Membrane.

Tissue specificity. Retinal cones, outer and inner segments.

Post-translational modifications. Autophosphorylated in vitro at Ser-490. Phosphorylation at Ser-36 is regulated by light and activated by cAMP.

Activity regulation. Inhibited by phosphorylation of Ser-36.

Miscellaneous. Although the protein is present in a diversity of vertebrates ranging from bony fish to mammals, the mouse and rat orthologous proteins do not exist.

Similarity. Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily.

RefSeq proteins (1): NP_631948* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000239	GPCR_kinase	Family
IPR000719	Prot_kinase_dom	Domain
IPR000961	AGC-kinase_C	Domain
IPR008271	Ser/Thr_kinase_AS	Active_site
IPR011009	Kinase-like_dom_sf	Homologous_superfamily
IPR016137	RGS	Domain
IPR017441	Protein_kinase_ATP_BS	Binding_site
IPR036305	RGS_sf	Homologous_superfamily
IPR044926	RGS_subdomain_2	Homologous_superfamily

Pfam: PF00069, PF00615

Enzyme classification (BRENDA):

• EC 2.7.11.14 — rhodopsin kinase (BRENDA: 15 organisms, 212 substrates, 103 inhibitors, 43 Km, 3 kcat entries)

Substrate kinetics (BRENDA)

6 substrates with measured Km, best-characterized 6. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
RHODOPSIN	0.0006–30	15
ATP	0.003–0.166	11
GTP	0.4–1	2
ATPGAMMAS	0.027	1
DDEASTTVSKTETSQVARRR	7.1	1
RRREEEEESAAA	2	1

Catalyzed reactions (Rhea), 2 shown:

• L-seryl-[rhodopsin] + ATP = O-phospho-L-seryl-[rhodopsin] + ADP + H(+) (RHEA:23356)
• L-threonyl-[rhodopsin] + ATP = O-phospho-L-threonyl-[rhodopsin] + ADP + H(+) (RHEA:56552)

UniProt features (26 total): sequence variant 13, domain 3, mutagenesis site 2, binding site 2, modified residue 2, chain 1, propeptide 1, lipid moiety-binding region 1, active site 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8WTQ7-F1	90.79	0.76

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 316 (proton acceptor)

Ligand- & substrate-binding residues (2): 197–205; 220

Post-translational modifications (3): 550, 36, 550

Mutagenesis-validated functional residues (2):

Position	Phenotype
23	no effect on kinase activity. increase kinase activity; when associated with a-36.
36	no effect on kinase activity. increase kinase activity; when associated with a-23.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-2514859	Inactivation, recovery and regulation of the phototransduction cascade

MSigDB gene sets: 55 (showing top): GOBP_CELLULAR_RESPONSE_TO_LIGHT_STIMULUS, GOBP_PHOTOTRANSDUCTION, MEF2_02, PID_CONE_PATHWAY, GOBP_PHOTOTRANSDUCTION_VISIBLE_LIGHT, GOBP_SENSORY_PERCEPTION_OF_LIGHT_STIMULUS, GOBP_RESPONSE_TO_RADIATION, GOBP_DETECTION_OF_LIGHT_STIMULUS, GOBP_RESPONSE_TO_ABIOTIC_STIMULUS, GOBP_DETECTION_OF_ABIOTIC_STIMULUS, GOBP_REGULATION_OF_RESPONSE_TO_EXTERNAL_STIMULUS, GOBP_DETECTION_OF_STIMULUS, GOBP_CELLULAR_RESPONSE_TO_RADIATION, GOBP_SENSORY_PERCEPTION, GOCC_NEURON_PROJECTION

GO Biological Process (7): signal transduction (GO:0007165), visual perception (GO:0007601), regulation of signal transduction (GO:0009966), regulation of opsin-mediated signaling pathway (GO:0022400), protein autophosphorylation (GO:0046777), protein phosphorylation (GO:0006468), regulation of G protein-coupled receptor signaling pathway (GO:0008277)

GO Molecular Function (9): ATP binding (GO:0005524), rhodopsin kinase activity (GO:0050254), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein serine/threonine kinase activity (GO:0004674), G protein-coupled receptor kinase activity (GO:0004703), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740)

GO Cellular Component (3): cytoplasm (GO:0005737), photoreceptor disc membrane (GO:0097381), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
The phototransduction cascade	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	2
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
sensory perception of light stimulus	1
signal transduction	1
regulation of cell communication	1
regulation of signaling	1
regulation of response to stimulus	1
regulation of G protein-coupled receptor signaling pathway	1
G protein-coupled opsin signaling pathway	1
regulation of response to external stimulus	1
protein phosphorylation	1
phosphorylation	1
protein modification process	1
G protein-coupled receptor signaling pathway	1
regulation of signal transduction	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
G protein-coupled receptor kinase activity	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
kinase activity	1
phosphotransferase activity, alcohol group as acceptor	1
catalytic activity, acting on a protein	1
protein kinase activity	1
protein serine/threonine kinase activity	1
binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity	1
intracellular anatomical structure	1
photoreceptor outer segment	1
organelle membrane	1

Protein interactions and networks

STRING

883 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GRK7	RHO	P08100	994
GRK7	SAG	P10523	957
GRK7	RCVRN	P35243	955
GRK7	MPP4	Q96JB8	762
GRK7	ARRB1	P49407	725
GRK7	CALML3	P27482	672
GRK7	ARRB2	P32121	672
GRK7	CALML6	Q8TD86	672
GRK7	CALML4	Q96GE6	672
GRK7	CALML5	Q9NZT1	672
GRK7	ITPR2	Q14571	669
GRK7	GUCA1A	P43080	630
GRK7	PDE6A	P16499	617
GRK7	SLC24A1	O60721	595
GRK7	ARR3	P36575	583

IntAct

10 interactions, top by confidence:

A	B	Type	Score
GRK7	HSP90AB1	psi-mi:“MI:0915”(physical association)	0.560
GRK7	HSP90AA1	psi-mi:“MI:0914”(association)	0.530
GRK7	FAAP100	psi-mi:“MI:0915”(physical association)	0.500
GRK7	YWHAE	psi-mi:“MI:0915”(physical association)	0.400
SFN	GRK7	psi-mi:“MI:0915”(physical association)	0.400
DSC1	TBC1D4	psi-mi:“MI:0914”(association)	0.350
ACACB	TACC1	psi-mi:“MI:0914”(association)	0.350

BioGRID (25): ZYG11B (Affinity Capture-MS), HSP90AA1 (Affinity Capture-MS), GRK7 (Affinity Capture-MS), C17orf70 (Affinity Capture-MS), THUMPD3 (Affinity Capture-MS), HDLBP (Affinity Capture-MS), HSP90AB3P (Affinity Capture-MS), GRK7 (Affinity Capture-MS), HSP90AA1 (Affinity Capture-MS), HSP90AB1 (Affinity Capture-MS), H2AFZ (Affinity Capture-MS), TOP2A (Affinity Capture-MS), MKI67 (Affinity Capture-MS), AHNAK (Affinity Capture-MS), MOGS (Affinity Capture-MS)

ESM2 similar proteins: A8KBH6, B6CZ17, B6CZ18, O75582, P04409, P05126, P05128, P05129, P05130, P05696, P05771, P05772, P09215, P09216, P10102, P10829, P10830, P13677, P13678, P16054, P17252, P20444, P23298, P24723, P28867, P34722, P34885, P54644, P63318, P63319, P68403, P68404, P90980, Q02111, Q02156, Q05655, Q16974, Q16975, Q17941, Q1XHL7

Diamond homologs: A1A4I4, A1Z7T0, A7MBL8, B6CZ17, B6CZ18, J9W0G9, O08874, O19111, O70291, O70293, O97627, P04409, P05130, P05696, P09215, P09217, P10102, P10830, P12688, P13678, P16054, P17252, P18961, P21146, P23298, P24723, P25098, P26817, P26818, P26819, P28327, P28867, P31748, P31749, P31750, P31751, P32298, P32865, P32866, P34102

SIGNOR signaling

8 interactions.

A	Effect	B	Mechanism
GRK7	unknown	GRK7	phosphorylation
PKA	“down-regulates activity”	GRK7	phosphorylation
PKA	“up-regulates activity”	GRK7	phosphorylation

Disease & clinical

Clinical variants and AI predictions

ClinVar

88 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	86
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

669 predictions. Top by Δscore:

Variant	Effect	Δscore
3:141780370:TAAGG:T	acceptor_loss	1.0000
3:141780371:AAG:A	acceptor_gain	1.0000
3:141780373:GGTAT:G	acceptor_gain	1.0000
3:141780808:GAGG:G	donor_gain	1.0000
3:141780810:GG:G	donor_gain	1.0000
3:141780811:GG:G	donor_gain	1.0000
3:141780812:GTGA:G	donor_loss	1.0000
3:141807633:G:A	acceptor_gain	1.0000
3:141778846:GACAA:G	donor_gain	0.9900
3:141778851:G:GG	donor_gain	0.9900
3:141778864:TTCA:T	donor_gain	0.9900
3:141778884:T:TA	donor_gain	0.9900
3:141778885:G:GA	donor_gain	0.9900
3:141778892:GGGAG:G	donor_gain	0.9900
3:141778893:GGAG:G	donor_gain	0.9900
3:141778893:GGAGG:G	donor_gain	0.9900
3:141778894:GAGG:G	donor_gain	0.9900
3:141778895:AGGTA:A	donor_loss	0.9900
3:141778896:GGT:G	donor_loss	0.9900
3:141778897:G:A	donor_loss	0.9900
3:141778898:T:TC	donor_loss	0.9900
3:141780370:TAAG:T	acceptor_gain	0.9900
3:141780372:AG:A	acceptor_gain	0.9900
3:141780373:G:A	acceptor_gain	0.9900
3:141780373:GGT:G	acceptor_gain	0.9900
3:141780373:GGTA:G	acceptor_gain	0.9900
3:141780812:G:GG	donor_gain	0.9900
3:141780813:TGAG:T	donor_loss	0.9900
3:141780814:GAGT:G	donor_loss	0.9900
3:141807628:T:TA	acceptor_gain	0.9900

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000008809 (3:141748487 T>C), RS1000024876 (3:141748702 C>T), RS1000045189 (3:141793904 T>C), RS1000136681 (3:141802453 G>T), RS1000255308 (3:141818073 G>A), RS1000260309 (3:141768528 C>T), RS1000393037 (3:141817662 A>C,G,T), RS1000411256 (3:141813573 T>G), RS1000418598 (3:141787523 C>T), RS1000480463 (3:141772650 A>G,T), RS1000507416 (3:141802107 G>A), RS1000509378 (3:141791200 G>A), RS1000529818 (3:141755803 C>A,G), RS1000603620 (3:141769996 C>A,T), RS1000618687 (3:141797576 A>G)

Disease associations

OMIM: gene MIM:606987 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST90006919_1	Anti-herpes simplex virus 2 IgG seropositivity	3.000000e-08

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0009339	Herpes simplex virus 2 seropositivity

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1075133 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

19 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 176,067 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1287853	FEDRATINIB	4	3,554
CHEMBL1789941	RUXOLITINIB	4	11,547
CHEMBL2103743	TOFACITINIB CITRATE	4	1,672
CHEMBL221959	TOFACITINIB	4	10,408
CHEMBL288441	BOSUTINIB	4	12,255
CHEMBL502835	NINTEDANIB	4	8,545
CHEMBL535	SUNITINIB	4	79,020
CHEMBL608533	MIDOSTAURIN	4	7,259
CHEMBL300138	ENZASTAURIN	3	3,209
CHEMBL428690	ALVOCIDIB	3	27,781
CHEMBL522892	DOVITINIB	3	4,944
CHEMBL603469	LESTAURTINIB	3
CHEMBL91829	RUBOXISTAURIN	3	77
CHEMBL1721885	SU-014813	2	363
CHEMBL475251	R-406	2	762
CHEMBL513909	BI-2536	2	895
CHEMBL1908394	GSK-461364	1	1,093
CHEMBL1908397	KW-2449	1	622
CHEMBL494089	GSK-690693	1	2,061

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — Opsin/rhodopsin kinases

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
balanol	Inhibition	6.74	pIC50

ChEMBL bioactivities

40 potent at pChembl≥5 of 42 total, top 37 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.07	Kd	0.86	nM	STAUROSPORINE
8.34	IC50	4.56	nM	STAUROSPORINE
8.29	IC50	5.12	nM	STAUROSPORINE
8.22	IC50	5.96	nM	STAUROSPORINE
8.19	IC50	6.4	nM	CHEMBL4877302
8.14	Kd	7.2	nM	LESTAURTINIB
7.82	IC50	15	nM	CHEMBL4854871
7.44	IC50	36	nM	CHEMBL4847703
7.32	Kd	48	nM	MIDOSTAURIN
7.21	Kd	61	nM	PHA-665752
6.75	IC50	180	nM	BALANOL
6.75	Kd	180	nM	SUNITINIB
6.51	Kd	310	nM	RUBOXISTAURIN
6.44	Kd	360	nM	TAE-684
6.42	Kd	380	nM	GSK-690693
6.33	Kd	470	nM	SU-014813
6.27	Kd	540	nM	RUXOLITINIB
6.27	Kd	540	nM	CHEMBL464552
6.26	Kd	550	nM	CGP-52421
6.09	Kd	820	nM	CHEMBL1908395
6.07	Kd	850	nM	BI-2536
6.01	Kd	980	nM	ALVOCIDIB
5.92	Kd	1200	nM	NINTEDANIB
5.89	Kd	1300	nM	ENZASTAURIN
5.89	Kd	1300	nM	DOVITINIB
5.85	Kd	1400	nM	CHEMBL1241674
5.77	Kd	1700	nM	BOSUTINIB
5.72	Kd	1900	nM	CHEMBL379218
5.70	Kd	2000	nM	R-406
5.62	IC50	2400	nM	CHEMBL4072828
5.58	Kd	2600	nM	FEDRATINIB
5.37	Kd	4300	nM	TOFACITINIB CITRATE
5.37	Kd	4300	nM	TOFACITINIB
5.30	Kd	5000	nM	KW-2449
5.12	Kd	7500	nM	GSK-461364
5.06	IC50	8800	nM	CHEMBL4082775
5.04	IC50	9137	nM	CHEMBL4742990

PubChem BioAssay actives

39 with measured affinity, of 541 total; 33 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one	624719: Binding constant for GRK7 kinase domain	kd	0.0009	uM
2-N-[(4-chloro-2-methoxyphenyl)methyl]-4-N-(5-ethyl-1H-pyrazol-3-yl)-5-methoxyquinazoline-2,4-diamine	1751901: Inhibition of recombinant full length human GRK7 using casein as substrate incubated for 40 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay	ic50	0.0064	uM
(15S,16S,18R)-16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaen-3-one	507965: Binding affinity to GRK7	kd	0.0072	uM
4-N-(5-ethyl-1H-pyrazol-3-yl)-2-N-[(1S)-1-(5-fluoro-2-pyridinyl)ethyl]-5-methoxyquinazoline-2,4-diamine	1751901: Inhibition of recombinant full length human GRK7 using casein as substrate incubated for 40 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay	ic50	0.0150	uM
4-N-(5-ethyl-1H-pyrazol-3-yl)-2-N-[(5-fluoro-2-pyridinyl)methyl]-5-methoxyquinazoline-2,4-diamine	1751901: Inhibition of recombinant full length human GRK7 using casein as substrate incubated for 40 mins in presence of [gamma-33ATP] by scintillation counting based radiometry assay	ic50	0.0360	uM
Midostaurin	507965: Binding affinity to GRK7	kd	0.0480	uM
(3Z)-5-[(2,6-dichlorophenyl)methylsulfonyl]-3-[[3,5-dimethyl-4-[(2R)-2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl]-1H-pyrrol-2-yl]methylidene]-1H-indol-2-one	624719: Binding constant for GRK7 kinase domain	kd	0.0610	uM
2-[2,6-dihydroxy-4-[(3R,4R)-3-[(4-hydroxybenzoyl)amino]azepan-4-yl]oxycarbonylbenzoyl]-3-hydroxybenzoic acid	464313: Inhibition of GRK7-mediated bovine tubulin phosphorylation by scintillation counting	ic50	0.1800	uM
Sunitinib	507965: Binding affinity to GRK7	kd	0.1800	uM
(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione	624719: Binding constant for GRK7 kinase domain	kd	0.3100	uM
5-chloro-2-N-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine	624719: Binding constant for GRK7 kinase domain	kd	0.3600	uM
4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[[(3S)-piperidin-3-yl]methoxy]imidazo[4,5-c]pyridin-4-yl]-2-methylbut-3-yn-2-ol	624719: Binding constant for GRK7 kinase domain	kd	0.3800	uM
5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide	624719: Binding constant for GRK7 kinase domain	kd	0.4700	uM
Ruxolitinib	624719: Binding constant for GRK7 kinase domain	kd	0.5400	uM
2-[[2-[[1-[2-(dimethylamino)acetyl]-5-methoxy-2,3-dihydroindol-6-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amino]-6-fluoro-N-methylbenzamide	624719: Binding constant for GRK7 kinase domain	kd	0.5400	uM
N-[(2S,3R,4R,6R,18S)-18-hydroxy-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-4-yl]-N-methylbenzamide	507965: Binding affinity to GRK7	kd	0.5500	uM
5-cyano-N-[2-(cyclohexen-1-yl)-4-[1-[2-(dimethylamino)acetyl]piperidin-4-yl]phenyl]-1H-imidazole-2-carboxamide;hydrochloride	624719: Binding constant for GRK7 kinase domain	kd	0.8200	uM
4-[[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide	624719: Binding constant for GRK7 kinase domain	kd	0.8500	uM
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one	624719: Binding constant for GRK7 kinase domain	kd	0.9800	uM
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate	624719: Binding constant for GRK7 kinase domain	kd	1.2000	uM
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one	624719: Binding constant for GRK7 kinase domain	kd	1.3000	uM
3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione	624719: Binding constant for GRK7 kinase domain	kd	1.3000	uM
2-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol	624719: Binding constant for GRK7 kinase domain	kd	1.4000	uM
Bosutinib	624719: Binding constant for GRK7 kinase domain	kd	1.7000	uM
(2S)-1-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]-3-phenylpropan-2-amine	624719: Binding constant for GRK7 kinase domain	kd	1.9000	uM
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one	624719: Binding constant for GRK7 kinase domain	kd	2.0000	uM
3-(9-oxa-3,4,6,12-tetrazatricyclo[8.4.0.02,6]tetradeca-1(10),2,4,11,13-pentaen-5-ylmethylamino)-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide	1457946: Inhibition of recombinant human full length GST-tagged GRK7 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins followed by substrate addition measured after 10 mins by Lance TR-FRET assay	ic50	2.4000	uM
Fedratinib	624719: Binding constant for GRK7 kinase domain	kd	2.6000	uM
Tofacitinib	624719: Binding constant for GRK7 kinase domain	kd	4.3000	uM
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone	624719: Binding constant for GRK7 kinase domain	kd	5.0000	uM
5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide	624719: Binding constant for GRK7 kinase domain	kd	7.5000	uM
N-benzyl-3-[(3-pyridin-4-yl-1H-1,2,4-triazol-5-yl)methylamino]benzamide	1457946: Inhibition of recombinant human full length GST-tagged GRK7 expressed in baculovirus using ulight topo2alpha as substrate preincubated for 60 mins followed by substrate addition measured after 10 mins by Lance TR-FRET assay	ic50	8.8000	uM
3-[(3-methoxyphenyl)methyl]-6-(1H-pyrazol-4-yl)quinazolin-4-one	1698799: Inhibition of human GRK7	ic50	9.1370	uM

CTD chemical–gene interactions

7 total (human), top 7 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
aristolochic acid I	increases expression	1
propionaldehyde	decreases expression	1
bisphenol A	decreases methylation	1
Oxaliplatin	decreases expression	1
Benzo(a)pyrene	increases methylation	1
Valproic Acid	increases methylation	1
Aflatoxin B1	increases methylation	1

ChEMBL screening assays

155 unique, capped per target: 155 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1100486	Binding	Inhibition of GRK7 at 10 uM	Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase. — Bioorg Med Chem Lett

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.