GRIK2

Summary

GRIK2 (glutamate ionotropic receptor kainate type subunit 2, HGNC:4580) is a protein-coding gene on chromosome 6q16.3, encoding Glutamate receptor ionotropic, kainate 2 (Q13002). Ionotropic glutamate receptor that functions as a cation-permeable ligand-gated ion channel, gated by L-glutamate and the glutamatergic agonist kainic acid.

Glutamate receptors are the predominant excitatory neurotransmitter receptors in the mammalian brain and are activated in a variety of normal neurophysiologic processes. This gene product belongs to the kainate family of glutamate receptors, which are composed of four subunits and function as ligand-activated ion channels. The subunit encoded by this gene is subject to RNA editing at multiple sites within the first and second transmembrane domains, which is thought to alter the structure and function of the receptor complex. Alternatively spliced transcript variants encoding different isoforms have also been described for this gene. Mutations in this gene have been associated with autosomal recessive cognitive disability.

Source: NCBI Gene 2898 — RefSeq curated summary.

At a glance

• Gene–disease (curated): complex neurodevelopmental disorder (Definitive, ClinGen) — +3 more curated relationships
• GWAS associations: 16
• Clinical variants (ClinVar): 306 total — 5 pathogenic, 10 likely-pathogenic
• Phenotypes (HPO): 65
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity no evidence
• MANE Select transcript: NM_021956

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4580
Approved symbol	GRIK2
Name	glutamate ionotropic receptor kainate type subunit 2
Location	6q16.3
Locus type	gene with protein product
Status	Approved
Aliases	GluK2, MRT6, GluR-6, EAA4, GLUK6
Ensembl gene	ENSG00000164418
Ensembl biotype	protein_coding
OMIM	138244
Entrez	2898

Gene structure

Transcript identifiers

Ensembl transcripts: 41 — 18 retained_intron, 11 protein_coding, 8 nonsense_mediated_decay, 4 protein_coding_CDS_not_defined

ENST00000358361, ENST00000369134, ENST00000369137, ENST00000369138, ENST00000413795, ENST00000421544, ENST00000436862, ENST00000455610, ENST00000487161, ENST00000487395, ENST00000681975, ENST00000682039, ENST00000682052, ENST00000682090, ENST00000682115, ENST00000682222, ENST00000682261, ENST00000682312, ENST00000682328, ENST00000682716, ENST00000682823, ENST00000682962, ENST00000683054, ENST00000683208, ENST00000683215, ENST00000683264, ENST00000683298, ENST00000683546, ENST00000683618, ENST00000683747, ENST00000683774, ENST00000683806, ENST00000683903, ENST00000683913, ENST00000684027, ENST00000684068, ENST00000684185, ENST00000684279, ENST00000684380, ENST00000684491, ENST00000684518

RefSeq mRNA: 3 — MANE Select: NM_021956 NM_001166247, NM_021956, NM_175768

CCDS: CCDS5048, CCDS5049, CCDS55045

Canonical transcript exons

ENST00000369134 — 17 exons

Exon	Start	End
ENSE00001084208	101799648	101799791
ENSE00001175424	101686180	101686353
ENSE00001175433	101682553	101682606
ENSE00001175441	101676623	101676804
ENSE00001175451	101626380	101626637
ENSE00001310137	102055330	102055580
ENSE00001318693	101859287	101859493
ENSE00001319383	101818370	101818483
ENSE00001327598	101802331	101802438
ENSE00001358806	102035341	102035566
ENSE00001609672	101928415	101928632
ENSE00001634244	101889640	101889863
ENSE00001773416	101924601	101924719
ENSE00003501564	101621949	101622116
ENSE00003665433	102068347	102070083
ENSE00003834743	101398985	101399392
ENSE00003907970	101393708	101393837

Expression profiles

Bgee: expression breadth ubiquitous, 213 present calls, max score 98.27.

FANTOM5 (CAGE): breadth broad, TPM avg 2.3504 / max 193.8676, expressed in 194 samples.

FANTOM5 promoters (12 alternative TSS)

Promoter ID	TPM avg	Samples expressed
69004	5.5778	770
69003	0.9478	324
69006	0.9410	117
69011	0.5770	113
69012	0.2643	89
69013	0.1481	73
69010	0.1124	62
69038	0.1068	44
69002	0.0753	36
204115	0.0546	43

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cerebellar vermis	UBERON:0004720	98.27	gold quality
cerebellar cortex	UBERON:0002129	96.59	gold quality
cerebellar hemisphere	UBERON:0002245	96.56	gold quality
cerebellum	UBERON:0002037	96.43	gold quality
right hemisphere of cerebellum	UBERON:0014890	96.35	gold quality
middle temporal gyrus	UBERON:0002771	95.94	gold quality
paraflocculus	UBERON:0005351	95.40	gold quality
Brodmann (1909) area 23	UBERON:0013554	93.37	gold quality
Brodmann (1909) area 10	UBERON:0013541	92.17	gold quality
cortical plate	UBERON:0005343	91.71	gold quality
orbitofrontal cortex	UBERON:0004167	90.54	gold quality
superior frontal gyrus	UBERON:0002661	89.99	gold quality
entorhinal cortex	UBERON:0002728	89.89	gold quality
Brodmann (1909) area 46	UBERON:0006483	89.05	gold quality
endothelial cell	CL:0000115	88.76	gold quality
right frontal lobe	UBERON:0002810	88.74	gold quality
postcentral gyrus	UBERON:0002581	88.60	gold quality
buccal mucosa cell	CL:0002336	87.97	gold quality
frontal pole	UBERON:0002795	87.94	gold quality
parietal lobe	UBERON:0001872	87.87	gold quality
sural nerve	UBERON:0015488	87.75	gold quality
trigeminal ganglion	UBERON:0001675	87.35	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	87.33	gold quality
Brodmann (1909) area 9	UBERON:0013540	87.20	gold quality
primary visual cortex	UBERON:0002436	86.89	gold quality
cingulate cortex	UBERON:0003027	86.89	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	86.87	gold quality
anterior cingulate cortex	UBERON:0009835	86.84	gold quality
cerebral cortex	UBERON:0000956	86.69	gold quality
temporal lobe	UBERON:0001871	86.60	gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-HCAD-35	yes	5238.46
E-HCAD-25	yes	2683.31
E-HCAD-5	yes	12.97
E-GEOD-137537	yes	6.05
E-ANND-3	yes	5.30

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

176 targeting GRIK2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-4425	100.00	67.59	1049
HSA-MIR-33A-5P	99.99	68.62	1055
HSA-MIR-33B-5P	99.99	68.58	1062
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-3692-3P	99.98	70.27	2139
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-507	99.97	70.11	1915
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-557	99.96	70.01	1640
HSA-MIR-548AJ-3P	99.96	73.38	5345

Functional genomics

ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 40)

• Linkage and association of the glutamate receptor 6 gene with autism (PMID:11920157)
• Specific alleles in GluR6 and CA150 locus were only observed in HD patients. (PMID:12821179)
• describes the time course of the open-channel form of the receptor as a function of glutamate concentration (PMID:14567698)
• Using three single nucleotide polymorphisms in GRIK2 and one in GRIK3, we found no evidence for association with Obssessive-Compulsive disorder in case-control or family-based analyses. (PMID:15094479)
• In this study, the maternal transmission disequilibrium of the glutamate receptor GRIK2 in schizophrenia. (PMID:15305151)
• The modifier effect is actually due to the TAA repeat itself, possibly via a functional consequence on the GRIK2 mRNA. (PMID:16959037)
• Our data on altered functional properties of GluR6(M836I) provide a functional basis for the postulated linkage of GluR6 to autism. (PMID:17167233)
• phosphorylation of the C-terminal tail of GluR6 by PKA leads to potentiation of whole cell response (PMID:17379418)
• These results suggest a potential association between GRIK2 and autism in the Korean population. (PMID:17428563)
• Mutations of GluR6 are unlikely to be associated with autism in the Indian population. (PMID:17712621)
• report a complex mutation in the ionotropic glutamate receptor 6 gene (GRIK2, also called “GLUR6”) that cosegregates with moderate-to-severe nonsyndromic autosomal recessive mental retardation in a large, consanguineous Iranian family (PMID:17847003)
• Overall, our data indicate that hGluR6c might have unique properties in non-nervous cells and in the first stages of CNS development. (PMID:18289788)
• results support the involvement of genes GRIA3 and GRIK2 in antidepressant treatment-emergent suicidal ideation (PMID:18593792)
• the apo state of GluR6 undergoes a cleft closure of 29-30 degrees upon binding full agonists, one of the largest observed in the glutamate receptor family. (PMID:18658129)
• Mutations to GLUR6 binding pocket that selectively affect domoate binding are freported. (PMID:18664604)
• nonconserved residues in GluR6 define the size of the agonist-binding pocket, exerting a steric influence on the bound agonist and the extent of binding-domain closure (PMID:18690046)
• GluR6 C-terminal domain KRIP6 regulates kainate receptors by inhibiting PICK1 modulation via competition or a mutual blocking effect (PMID:18692513)
• in silico ligand-docking predicted that most partial agonists select for the closed and not, as expected, the open or intermediate conformations of the GluK2 agonist binding domain. (PMID:19225180)
• Results indicate that ions can contribute substantial free energy to active state stabilization in GluR6, and provide quantitative measurements of the energetic consequences of allosteric ion binding to a ligand-gated ion channel. (PMID:19617541)
• phosphorylation of PKC sites on GluR6 regulates surface expression of GluR6 at distinct intracellular trafficking pathways (PMID:19920140)
• Spliced variants of ionotropic glutamate receptor GluR6 is associated with astrocytoma. (PMID:20230879)
• This study supports previously reported findings of association between proximal GRIK2 single nucleotide polymorphism and obsessive-compulsive disorder in a comprehensive evaluation of the gene (PMID:20370803)
• human GluK2 is a slowly activating channel but more sensitive to glutamate, as compared to the rat ortholog; the M867I mutation does not affect the rate the equilibrium constants of the channel opening but does slow down the channel desensitization rate (PMID:20863077)
• Genotyping and linkage analysis excluded linkage of the GRIK2 gene and TUSC3 gene with mental retardation. (PMID:21557188)
• Convergent functional genomics allowed the identification of novel candidate genes, GRIK2 and NPAS2, involved in glutamatergic neurotransmission and the circadian rhythm, respectively, that are potentially associated with CFS. (PMID:21912186)
• The ACAG haplotype in the 13th haplotype block of the GRIK2 gene was associated with somatic anxiety. (PMID:22429480)
• Comprehensive analytical methods applied to a much larger sample than in previous studies do not support a role for GRIK2 as a genetic modifier of age at onset of clinical symptoms in Huntington’s disease. (PMID:22771793)
• Eight chromosome 6 SNPs, having the most significant differences, were delineated: rs10499298, rs10499299, rs17827966, rs1224329, rs1150790, rs713050, rs2518344 and rs487083; all were associated with genes GRIK2. (PMID:23037145)
• Kainate receptor GluK2a post-translational modifications differentially regulate association with 4.1N to control activity-dependent receptor endocytosis (PMID:23400781)
• we found no association between rs1556995 in GRIK2 and clozapine-induced obsessive-compulsive (OC) symptoms, implying that that GRIK2 may not play a role in the development of OC symptoms in schizophrenia patients (PMID:23660601)
• Crosslinking the ligand-binding domain dimer interface locks kainate receptors out of the main open state. (PMID:23713029)
• 14-3-3 proteins are an important regulator of GluK2a-containing KARs and may contribute to the slow decay kinetics of native KAR-EPSCs. (PMID:23861400)
• This study found in GRIK2 (glutamate receptor, ionotropic kainate 2) was most significant and also showed significant correlations with gene expression. (PMID:24662927)
• This study showed that Gluk2 association with obsessive-compulsive disorder. (PMID:24821223)
• The present study reveals an additional mechanism for the regulation of GluK2-containing kainate receptors by Src family kinases, which may be of pathological significance in ischemic stroke. (PMID:25201974)
• Parkin interacts with the kainate receptor GluK2 subunit and regulates KAR function. (PMID:25316086)
• High risk genetic markers of paranoid schizophrenia were GRIK2*ATG and GRIK2*TGG in Tatars. (PMID:25842862)
• Study demonstrates that co-assembly of recombinant kainate receptors (GluK1 and GluK2) with the Neto1 and Neto2 auxiliary subunits alters their onset and recovery from desensitization in a subunit-dependent manner (PMID:26277340)
• In the Han population in Central China, the polymorphisms of SNP rs9390754 in the GRIK2 gene may be associated with epilepsy susceptibility. (PMID:27324535)
• TTBK2 down-regulates GluK2 activity by decreasing the receptor protein abundance in the cell membrane via RAB5-dependent endocytosis. (PMID:27607061)

Cross-species orthologs

42 orthologs

Organism	Symbol	Gene ID
danio_rerio	GRIK2	ENSDARG00000113771
mus_musculus	Grik2	ENSMUSG00000056073
rattus_norvegicus	Grik2	ENSRNOG00000000368
drosophila_melanogaster	GluRIA	FBGN0004619
drosophila_melanogaster	GluRIIA	FBGN0004620
drosophila_melanogaster	GluRIIB	FBGN0020429
drosophila_melanogaster	clumsy	FBGN0026255
drosophila_melanogaster	GluRIID	FBGN0028422
drosophila_melanogaster	Ir7b	FBGN0029965
drosophila_melanogaster	Ir7c	FBGN0029966
drosophila_melanogaster	Ir7g	FBGN0029968
drosophila_melanogaster	Ir25a	FBGN0031634
drosophila_melanogaster	Ir60a	FBGN0034994
drosophila_melanogaster	Ir64a	FBGN0035604
drosophila_melanogaster	Ir68a	FBGN0036150
drosophila_melanogaster	Ir68b	FBGN0036250
drosophila_melanogaster	Ir75a	FBGN0036757
drosophila_melanogaster	Ir75d	FBGN0036829
drosophila_melanogaster	Ir76b	FBGN0036937
drosophila_melanogaster	Ir84a	FBGN0037501
drosophila_melanogaster	Ir85a	FBGN0037630
drosophila_melanogaster	Ir92a	FBGN0038789
drosophila_melanogaster	Grik	FBGN0038840
drosophila_melanogaster	Ekar	FBGN0039916
drosophila_melanogaster	CG11155	FBGN0039927
drosophila_melanogaster	Ir41a	FBGN0040849
drosophila_melanogaster	GluRIIC	FBGN0046113
drosophila_melanogaster	GluRIIE	FBGN0051201
drosophila_melanogaster	Nmdar2	FBGN0053513
drosophila_melanogaster	Ir7e	FBGN0259189
drosophila_melanogaster	Ir94d	FBGN0259193
drosophila_melanogaster	Ir93a	FBGN0259215
drosophila_melanogaster	Ir40a	FBGN0259683
drosophila_melanogaster	Ir76a	FBGN0260874
drosophila_melanogaster	Ir75c	FBGN0261401
drosophila_melanogaster	Ir75b	FBGN0261402
drosophila_melanogaster	GluRIB	FBGN0264000
caenorhabditis_elegans		WBGENE00001612
caenorhabditis_elegans	glr-3	WBGENE00001614
caenorhabditis_elegans		WBGENE00001618
caenorhabditis_elegans		WBGENE00003775
caenorhabditis_elegans		WBGENE00012190

Paralogs (17): GRIN2D (ENSG00000105464), GRIK5 (ENSG00000105737), GRIN3B (ENSG00000116032), GRIA2 (ENSG00000120251), GRIA3 (ENSG00000125675), GRIK4 (ENSG00000149403), GRID2 (ENSG00000152208), GRIA4 (ENSG00000152578), GRIA1 (ENSG00000155511), GRIN2C (ENSG00000161509), GRIK3 (ENSG00000163873), GRIK1 (ENSG00000171189), GRIN1 (ENSG00000176884), GRID1 (ENSG00000182771), GRIN2A (ENSG00000183454), GRIN3A (ENSG00000198785), GRIN2B (ENSG00000273079)

Protein

Protein identifiers

Glutamate receptor ionotropic, kainate 2 — Q13002 (reviewed: Q13002)

Alternative names: Excitatory amino acid receptor 4, Glutamate receptor 6

All UniProt accessions (14): A0A0A0MRL4, A0A804HHV9, A0A804HI04, A0A804HIH6, A0A804HKP5, A0A804HKS7, A0A804HKU0, A0A804HL10, A0A8D9PH75, Q13002, F8WEZ8, G3XAD3, H7BZX7, H7C2P5

UniProt curated annotations — full annotation on UniProt →

Function. Ionotropic glutamate receptor that functions as a cation-permeable ligand-gated ion channel, gated by L-glutamate and the glutamatergic agonist kainic acid. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformational change leading to the opening of the cation channel, converting the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. Modulates cell surface expression of NETO2. In association with GRIK3, involved in presynaptic facilitation of glutamate release at hippocampal mossy fiber synapses. Independent of its ionotropic glutamate receptor activity, acts as a thermoreceptor conferring sensitivity to cold temperatures. Functions in dorsal root ganglion neurons.

Subunit / interactions. Homotetramer; formed by the dimerization of dimers via its N-terminal domain. Assembles into a kainate-gated homomeric channel that does not bind AMPA. Can form functional heteromeric receptors with GRIK5. Can form functional heteromeric receptors with GRIK3 and GRIK4. Interacts with DLG4. Interacts with NETO2. Interacts (via C-terminus) with KLHL17 (via kelch repeats); the interaction targets GRIK2 for degradation via ubiquitin-proteasome pathway.

Subcellular location. Cell membrane. Postsynaptic cell membrane.

Tissue specificity. Expression is higher in cerebellum than in cerebral cortex.

Post-translational modifications. Sumoylation mediates kainate receptor-mediated endocytosis and regulates synaptic transmission. Sumoylation is enhanced by PIAS3 and desumoylated by SENP1. Ubiquitinated. Ubiquitination regulates the GRIK2 levels at the synapse by leading kainate receptor degradation through proteasome. Phosphorylated by PKC at Ser-868 upon agonist activation, this directly enhance sumoylation.

Disease relevance. Intellectual developmental disorder, autosomal recessive 6 (MRT6) [MIM:611092] A disorder characterized by significantly below average general intellectual functioning associated with impairments in adaptive behavior and manifested during the developmental period. MRT6 patients display mild to severe intellectual disability and psychomotor development delay in early childhood. Patients do not have neurologic problems, congenital malformations, or facial dysmorphism. Body height, weight, and head circumference are normal. The disease is caused by variants affecting the gene represented in this entry. Neurodevelopmental disorder with impaired language and ataxia and with or without seizures (NEDLAS) [MIM:619580] An autosomal dominant disorder characterized by axial hypotonia and global developmental delay. Affected individuals show impaired intellectual development, delayed walking, poor speech, and behavioral abnormalities. Some patients have a more severe phenotype with early-onset seizures resembling epileptic encephalopathy, inability to walk or speak, and hypomyelination on brain imaging. The disease is caused by variants affecting the gene represented in this entry.

Activity regulation. Ionotropic glutamate receptor activity is promoted by positive allosteric modulators that inhibit receptor desensitization. Ionotropic glutamate receptor activity is inhibited by ion channel blockers.Cold receptor activity is activated by temperatures between 10-19 degrees Celsius.

Domain organisation. The gate of the ion channel is formed by four transmembrane M3 helices and it opens upon stimulation by positive allosteric modulators.

Miscellaneous. The postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists. This receptor binds domoate > kainate > quisqualate > 6-cyano-7-nitroquinoxaline-2,3-dione > L-glutamate = 6,7-dinitroquinoxaline-2,3-dione > dihydrokainate.

Similarity. Belongs to the glutamate-gated ion channel (TC 1.A.10.1) family. GRIK2 subfamily.

Isoforms (7)

UniProt ID	Names	Canonical?
Q13002-1	1, A	yes
Q13002-2	2, B
Q13002-3	3
Q13002-4	4
Q13002-5	5, C
Q13002-6	6, D
Q13002-7	7, E

RefSeq proteins (3): NP_001159719, NP_068775, NP_786944 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001320	Iontro_rcpt_C	Domain
IPR001508	Iono_Glu_rcpt_met	Family
IPR001828	ANF_lig-bd_rcpt	Domain
IPR015683	Ionotropic_Glu_rcpt	Family
IPR019594	Glu/Gly-bd	Domain
IPR028082	Peripla_BP_I	Homologous_superfamily

Pfam: PF00060, PF01094, PF10613

Catalyzed reactions (Rhea), 2 shown:

• Ca(2+)(in) = Ca(2+)(out) (RHEA:29671)
• Na(+)(in) = Na(+)(out) (RHEA:34963)

UniProt features (77 total): strand 14, helix 12, sequence variant 10, glycosylation site 9, binding site 6, splice variant 6, topological domain 5, transmembrane region 3, modified residue 2, disulfide bond 2, sequence conflict 2, turn 2, signal peptide 1, chain 1, cross-link 1, intramembrane region 1

Structure

Experimental structures (PDB)

2 structures.

PDB	Method	Resolution (Å)
5CMM	X-RAY DIFFRACTION	1.27
3QXM	X-RAY DIFFRACTION	1.65

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q13002-F1	83.67	0.48

Functional residue map

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

Ligand- & substrate-binding residues (6): 516; 518; 523; 689; 690; 738

Post-translational modifications (3): 846, 868, 886

Disulfide bonds (2): 96–347, 750–804

Glycosylation sites (9): 67, 73, 275, 378, 412, 423, 430, 546, 751

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-451307	Activation of Na-permeable kainate receptors
R-HSA-451308	Activation of Ca-permeable Kainate Receptor

MSigDB gene sets: 433 (showing top): BROWNE_HCMV_INFECTION_4HR_UP, GOBP_NEGATIVE_REGULATION_OF_NEURON_APOPTOTIC_PROCESS, REACTOME_IONOTROPIC_ACTIVITY_OF_KAINATE_RECEPTORS, MODULE_274, GOBP_SENSORY_PERCEPTION_OF_TEMPERATURE_STIMULUS, GOBP_BEHAVIOR, GOMF_GLUTAMATE_GATED_RECEPTOR_ACTIVITY, GOBP_REGULATION_OF_NEURONAL_SYNAPTIC_PLASTICITY, GOBP_REGULATION_OF_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, GOBP_REGULATION_OF_SHORT_TERM_NEURONAL_SYNAPTIC_PLASTICITY, ATGCAGT_MIR217, GOBP_MULTICELLULAR_ORGANISMAL_RESPONSE_TO_STRESS, GOBP_CELL_CELL_SIGNALING, NFKB_Q6, GOBP_DETECTION_OF_TEMPERATURE_STIMULUS

GO Biological Process (27): behavioral fear response (GO:0001662), intracellular calcium ion homeostasis (GO:0006874), glutamate receptor signaling pathway (GO:0007215), chemical synaptic transmission (GO:0007268), neuronal action potential (GO:0019228), synaptic transmission, glutamatergic (GO:0035249), receptor clustering (GO:0043113), negative regulation of neuron apoptotic process (GO:0043524), positive regulation of neuron apoptotic process (GO:0043525), regulation of JNK cascade (GO:0046328), regulation of long-term neuronal synaptic plasticity (GO:0048169), regulation of short-term neuronal synaptic plasticity (GO:0048172), modulation of chemical synaptic transmission (GO:0050804), positive regulation of synaptic transmission (GO:0050806), neuron apoptotic process (GO:0051402), negative regulation of synaptic transmission, glutamatergic (GO:0051967), inhibitory postsynaptic potential (GO:0060080), modulation of excitatory postsynaptic potential (GO:0098815), presynaptic modulation of chemical synaptic transmission (GO:0099171), detection of cold stimulus involved in thermoception (GO:0120169), monoatomic ion transport (GO:0006811), calcium-mediated signaling (GO:0019722), monoatomic ion transmembrane transport (GO:0034220), ionotropic glutamate receptor signaling pathway (GO:0035235), regulation of membrane potential (GO:0042391), excitatory postsynaptic potential (GO:0060079), regulation of presynaptic membrane potential (GO:0099505)

GO Molecular Function (16): SNARE binding (GO:0000149), glutamate-gated receptor activity (GO:0004970), extracellularly glutamate-gated ion channel activity (GO:0005234), kainate selective glutamate receptor activity (GO:0015277), glutamate-gated calcium ion channel activity (GO:0022849), PDZ domain binding (GO:0030165), ubiquitin conjugating enzyme binding (GO:0031624), ubiquitin protein ligase binding (GO:0031625), identical protein binding (GO:0042802), scaffold protein binding (GO:0097110), ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential (GO:0099507), transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential (GO:1904315), monoatomic ion channel activity (GO:0005216), glutamate receptor activity (GO:0008066), ligand-gated monoatomic ion channel activity (GO:0015276), signaling receptor activity (GO:0038023)

GO Cellular Component (18): plasma membrane (GO:0005886), dendrite cytoplasm (GO:0032839), kainate selective glutamate receptor complex (GO:0032983), presynaptic membrane (GO:0042734), terminal bouton (GO:0043195), perikaryon (GO:0043204), mossy fiber rosette (GO:0097471), hippocampal mossy fiber to CA3 synapse (GO:0098686), postsynaptic density membrane (GO:0098839), glutamatergic synapse (GO:0098978), ionotropic glutamate receptor complex (GO:0008328), postsynaptic density (GO:0014069), membrane (GO:0016020), axon (GO:0030424), dendrite (GO:0030425), neuronal cell body (GO:0043025), synapse (GO:0045202), postsynaptic membrane (GO:0045211)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Ionotropic activity of kainate receptors	2

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
chemical synaptic transmission	3
modulation of chemical synaptic transmission	3
presynapse	3
protein binding	3
glutamate receptor activity	2
regulation of neuron apoptotic process	2
neuron apoptotic process	2
regulation of neuronal synaptic plasticity	2
regulation of postsynaptic membrane potential	2
transmitter-gated monoatomic ion channel activity	2
glutamate-gated receptor activity	2
synaptic membrane	2
cellular anatomical structure	2
asymmetric synapse	2
neuron projection	2
behavioral defense response	1
fear response	1
intracellular monoatomic cation homeostasis	1
calcium ion homeostasis	1
cell surface receptor signaling pathway	1
anterograde trans-synaptic signaling	1
action potential	1
transmission of nerve impulse	1
plasma membrane	1
protein localization to membrane	1
negative regulation of apoptotic process	1
positive regulation of apoptotic process	1
JNK cascade	1
regulation of MAPK cascade	1
regulation of trans-synaptic signaling	1
positive regulation of cell communication	1
positive regulation of signaling	1
apoptotic process	1
synaptic transmission, glutamatergic	1
negative regulation of synaptic transmission	1
regulation of synaptic transmission, glutamatergic	1
chemical synaptic transmission, postsynaptic	1
regulation of signal transduction	1
regulation of nervous system process	1
regulation of membrane potential	1

Protein interactions and networks

STRING

1978 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GRIK2	DLG4	P78352	991
GRIK2	GRIK5	Q16478	983
GRIK2	GRIK4	Q16099	982
GRIK2	GRIK1	P39086	980
GRIK2	GRIK3	Q13003	967
GRIK2	NETO1	Q8TDF5	872
GRIK2	NETO2	Q8NC67	869
GRIK2	KLHL24	Q6TFL4	841
GRIK2	UBE2I	P50550	833
GRIK2	GRM7	Q14831	799
GRIK2	KARS1	Q15046	795
GRIK2	SDCBP	O00560	795
GRIK2	PICK1	Q9NRD5	792
GRIK2	GRIP1	Q9Y3R0	744
GRIK2	GNB4	Q9HAV0	729

IntAct

132 interactions, top by confidence:

A	B	Type	Score
GRIK2	GRIK2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	DLG3	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	TIAM2	psi-mi:“MI:0407”(direct interaction)	0.440
APBA3	GRIK2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	MAST1	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	PDZD7	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	APBA2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	GRIP2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	MPP2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	GRID2IP	psi-mi:“MI:0407”(direct interaction)	0.440
PICK1	GRIK2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	HTRA4	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	NHERF4	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	WHRN	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	PDZRN4	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	TAX1BP3	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	PATJ	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	MPP7	psi-mi:“MI:0407”(direct interaction)	0.440
PDZK1	GRIK2	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	DLG4	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	PARD3B	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	MAGI1	psi-mi:“MI:0407”(direct interaction)	0.440
GRIK2	GOPC	psi-mi:“MI:0407”(direct interaction)	0.440
SCRIB	GRIK2	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (44): GRIK2 (Affinity Capture-Western), GRIK5 (Affinity Capture-Western), GRIK2 (Affinity Capture-RNA), GRIK2 (Affinity Capture-RNA), PICK1 (Reconstituted Complex), SDCBP (Reconstituted Complex), DLG4 (Reconstituted Complex), GRIP1 (Reconstituted Complex), DLG4 (Affinity Capture-Western), SDCBP (Affinity Capture-Western), PICK1 (Affinity Capture-Western), GRID2 (Affinity Capture-Western), GRIK2 (Affinity Capture-Western), GRIK2 (Affinity Capture-Western), GRIK2 (Affinity Capture-Western)

ESM2 similar proteins: A0A2R8QF68, B1AS29, P19439, P19490, P19491, P19492, P19493, P20262, P22756, P23818, P23819, P26591, P31422, P34299, P39086, P39087, P42260, P42261, P42262, P42263, P42264, P48058, Q01812, Q03445, Q13002, Q13003, Q14832, Q16099, Q16478, Q1ZZH1, Q21415, Q38PU2, Q38PU3, Q38PU4, Q38PU5, Q38PU6, Q38PU7, Q38PU8, Q5IS46, Q5R4M0

Diamond homologs: A0A2R8QF68, A7XY94, B1AS29, E9NA96, P19439, P19490, P19491, P19492, P19493, P20262, P22756, P23818, P23819, P26591, P34299, P35436, P39086, P39087, P42260, P42261, P42262, P42263, P42264, P48058, Q00959, Q01812, Q03445, Q10914, Q12879, Q13002, Q13003, Q16099, Q16478, Q21415, Q38PU2, Q38PU3, Q38PU4, Q38PU5, Q38PU6, Q38PU7

SIGNOR signaling

9 interactions.

A	Effect	B	Mechanism
PRKACA	“up-regulates activity”	GRIK2	phosphorylation
GRIK2	up-regulates	Excitatory_synaptic_transmission
“glutamic acid”	“up-regulates activity”	GRIK2	“chemical activation”
GRIK2	“up-regulates quantity”	calcium(2+)	relocalization
GRIK2	“up-regulates quantity”	D-serine	relocalization
SRC	“up-regulates activity”	GRIK2	phosphorylation
PRKN	“down-regulates quantity by destabilization”	GRIK2	ubiquitination
KLHL17	“down-regulates quantity by destabilization”	GRIK2	binding
“Cullin 3-RBX1-Skp1”	“down-regulates quantity by destabilization”	GRIK2	polyubiquitination

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 84 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	51.9×	2e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	49.4×	2e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	49.4×	2e-06
Long-term potentiation	5	43.3×	3e-06
Assembly and cell surface presentation of NMDA receptors	9	41.5×	6e-11
Neurexins and neuroligins	10	35.8×	3e-11
Protein-protein interactions at synapses	6	29.0×	2e-06
RHOB GTPase cycle	5	14.0×	6e-04

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	11	78.9×	3e-16
protein localization to synapse	6	56.7×	1e-07
receptor clustering	7	53.9×	1e-08
regulation of postsynaptic membrane neurotransmitter receptor levels	7	42.8×	4e-08
protein-containing complex assembly	9	12.7×	3e-06
cell-cell adhesion	10	12.5×	6e-07
regulation of small GTPase mediated signal transduction	5	8.9×	6e-03
chemical synaptic transmission	7	6.7×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	5
Likely pathogenic	10
Uncertain significance	201
Likely benign	53
Benign	10

Top pathogenic / likely-pathogenic (15)

Variant ID	HGVS	Classification
1180451	NM_021956.5(GRIK2):c.1979C>G (p.Thr660Arg)	Pathogenic
16087	GRIK2, DEL/INV, EX7-11	Pathogenic
189252	NM_021956.5(GRIK2):c.592C>T (p.Arg198Ter)	Pathogenic
870382	NM_021956.5(GRIK2):c.1979C>A (p.Thr660Lys)	Pathogenic
985841	NM_021956.5(GRIK2):c.1969G>A (p.Ala657Thr)	Pathogenic
1180452	NM_021956.5(GRIK2):c.2003T>C (p.Ile668Thr)	Likely pathogenic
1693459	NM_021956.5(GRIK2):c.1960A>G (p.Asn654Asp)	Likely pathogenic
2503314	NM_021956.5(GRIK2):c.283+1G>C	Likely pathogenic
2582447	NM_021956.5(GRIK2):c.355C>T (p.Gln119Ter)	Likely pathogenic
3064934	NM_021956.5(GRIK2):c.1204-1G>T	Likely pathogenic
3765562	NM_021956.5(GRIK2):c.571G>T (p.Ala191Ser)	Likely pathogenic
4081438	NM_021956.5(GRIK2):c.126dup (p.Glu43Ter)	Likely pathogenic
4527140	NM_021956.5(GRIK2):c.1567C>T (p.Arg523Ter)	Likely pathogenic
4823848	GRCh37/hg19 6q16.3(chr6:102503205-102503455)x0	Likely pathogenic
637968	NM_021956.5(GRIK2):c.808C>T (p.Arg270Ter)	Likely pathogenic

SpliceAI

2335 predictions. Top by Δscore:

Variant	Effect	Δscore
6:101454095:G:GT	donor_gain	1.0000
6:101399243:G:GT	donor_gain	0.9900
6:101399243:G:T	donor_gain	0.9900
6:101418596:G:T	donor_gain	0.9900
6:101439129:C:G	donor_gain	0.9900
6:101475669:G:GT	donor_gain	0.9900
6:101475677:A:AG	donor_gain	0.9900
6:101475677:A:G	donor_gain	0.9900
6:101501139:A:AG	donor_gain	0.9900
6:101564789:TGCA:T	donor_gain	0.9900
6:101451509:G:GC	acceptor_gain	0.9800
6:101457761:A:G	acceptor_gain	0.9800
6:101466737:C:T	donor_gain	0.9800
6:101483276:G:GT	donor_gain	0.9800
6:101483287:C:T	donor_gain	0.9800
6:101564790:GCAA:G	donor_gain	0.9800
6:101399095:G:GG	donor_gain	0.9700
6:101399295:GATTC:G	donor_gain	0.9700
6:101454018:G:GT	donor_gain	0.9700
6:101501139:A:G	acceptor_gain	0.9700
6:101418596:G:GT	acceptor_gain	0.9600
6:101466797:G:GT	donor_gain	0.9600
6:101466820:TTG:T	donor_gain	0.9600
6:101564222:A:AG	acceptor_gain	0.9600
6:101451533:T:TA	acceptor_gain	0.9500
6:101457756:A:AG	acceptor_gain	0.9500
6:101457757:A:G	acceptor_gain	0.9500
6:101463577:G:T	acceptor_gain	0.9500
6:101505351:T:G	donor_gain	0.9500
6:101466798:A:T	donor_gain	0.9400

AlphaMissense

5757 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
6:101622012:C:A	A60D	1.000
6:101626382:T:A	C96S	1.000
6:101626382:T:C	C96R	1.000
6:101626383:G:A	C96Y	1.000
6:101626383:G:C	C96S	1.000
6:101626383:G:T	C96F	1.000
6:101626384:T:G	C96W	1.000
6:101626392:T:C	L99P	1.000
6:101626400:G:T	G102W	1.000
6:101626418:G:A	G108R	1.000
6:101626418:G:C	G108R	1.000
6:101626419:G:A	G108E	1.000
6:101626462:C:G	C122W	1.000
6:101626476:T:A	V127D	1.000
6:101626601:T:A	W169R	1.000
6:101626601:T:C	W169R	1.000
6:101626617:T:A	V174D	1.000
6:101676626:T:A	L182H	1.000
6:101676626:T:C	L182P	1.000
6:101676686:G:C	R202P	1.000
6:101676725:T:C	L215P	1.000
6:101799658:C:A	A321D	1.000
6:101799661:T:C	L322P	1.000
6:101799672:G:C	A326P	1.000
6:101799735:T:A	C347S	1.000
6:101799735:T:C	C347R	1.000
6:101799736:G:A	C347Y	1.000
6:101799736:G:C	C347S	1.000
6:101799737:T:G	C347W	1.000
6:101799753:T:A	W353R	1.000

dbSNP variants (sampled 300 via entrez): RS1000003439 (6:102044504 G>T), RS1000010011 (6:101953385 G>A), RS1000011871 (6:101878742 C>T), RS1000019550 (6:101723785 C>G,T), RS1000023898 (6:102001595 C>G,T), RS1000033262 (6:101505918 A>T), RS1000039625 (6:101548284 G>T), RS1000056485 (6:102001306 T>C), RS1000066063 (6:101946731 A>G), RS1000070476 (6:101835596 G>A,C,T), RS1000071542 (6:101683179 C>T), RS1000082041 (6:101878533 T>C), RS1000084453 (6:101801809 A>G), RS1000091582 (6:101548527 C>G,T), RS1000097775 (6:101962975 T>C)

Disease associations

OMIM: gene MIM:138244 | disease phenotypes: MIM:611092, MIM:619580

GenCC curated gene-disease

Disease	Classification	Inheritance
intellectual disability, autosomal recessive 6	Definitive	Autosomal recessive
neurodevelopmental disorder with impaired language and ataxia and with or without seizures	Strong	Autosomal dominant
autosomal recessive non-syndromic intellectual disability	Supportive	Autosomal recessive

ClinGen Gene-Disease Validity (2)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

Disease	Classification	Inheritance
complex neurodevelopmental disorder	Moderate	AR
complex neurodevelopmental disorder	Definitive	AD

Mondo (5): intellectual disability, autosomal recessive 6 (MONDO:0012614), intellectual disability (MONDO:0001071), neurodevelopmental disorder with impaired language and ataxia and with or without seizures (MONDO:0859201), lip and oral cavity carcinoma (MONDO:0023644), autosomal recessive non-syndromic intellectual disability (MONDO:0019502)

Orphanet (3): Autosomal recessive non-syndromic intellectual disability (Orphanet:88616), Cerebral visual impairment (Orphanet:447788), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

65 total (30 of 65 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000007	Autosomal recessive inheritance
HP:0000252	Microcephaly
HP:0000365	Hearing impairment
HP:0000473	Torticollis
HP:0000486	Strabismus
HP:0000712	Emotional lability
HP:0000718	Aggressive behavior
HP:0000729	Autistic behavior
HP:0000733	Motor stereotypy
HP:0000736	Short attention span
HP:0000739	Anxiety
HP:0000749	Paroxysmal bursts of laughter
HP:0000750	Delayed speech and language development
HP:0000961	Cyanosis
HP:0001188	Hand clenching
HP:0001249	Intellectual disability
HP:0001251	Ataxia
HP:0001252	Hypotonia
HP:0001256	Mild intellectual disability
HP:0001263	Global developmental delay
HP:0001266	Choreoathetosis
HP:0001270	Motor delay
HP:0001272	Cerebellar atrophy
HP:0001290	Generalized hypotonia
HP:0001298	Encephalopathy
HP:0001336	Myoclonus
HP:0001344	Absent speech
HP:0002066	Gait ataxia
HP:0002069	Bilateral tonic-clonic seizure

GWAS associations

16 associations (top):

Study	Trait	p-value
GCST000328_15	Biochemical measures	2.000000e-06
GCST000960_9	Cardiac hypertrophy	3.000000e-06
GCST001607_5	Renal function-related traits (eGRFcrea)	1.000000e-07
GCST001636_2	Obsessive-compulsive disorder	3.000000e-06
GCST001762_430	Obesity-related traits	5.000000e-06
GCST001838_5	Palmitic acid (16:0) levels	2.000000e-07
GCST002599_1	Longevity (90 years and older)	5.000000e-08
GCST002945_37	Emphysema imaging phenotypes	3.000000e-07
GCST005024_41	Pursuit maintenance gain	5.000000e-07
GCST005847_6	Heart rate response to recovery post exercise (20 sec)	6.000000e-09
GCST008152_161	Weight	7.000000e-06
GCST009439_1	Age-related cognitive decline (language) (slope of z-scores)	8.000000e-06
GCST012322_34	Triglyceride levels x SSRI defined daily dose interaction in schizophrenia or bipolar disorder	5.000000e-08
GCST012484_25	Cerebral amyloid angiopathy x APOEe4 status interaction in Alzheimer’s disease	1.000000e-05
GCST90020024_591	A body shape index	3.000000e-09
GCST90020029_1413	Waist circumference adjusted for body mass index	1.000000e-08

EFO canonical traits (10, from GWAS)

EFO ID	Trait name
EFO:0002503	cardiac hypertrophy
EFO:0007626	emphysema imaging measurement
EFO:0008433	pursuit maintenance gain measurement
EFO:0009185	heart rate response to recovery post exercise
EFO:0004338	body weight
EFO:0007710	cognitive decline measurement
EFO:0004530	triglyceride measurement
EFO:0005658	response to selective serotonin reuptake inhibitor
EFO:0007659	APOE carrier status
EFO:0007789	BMI-adjusted waist circumference

MeSH disease descriptors (2)

Descriptor	Name	Tree numbers
D008607	Intellectual Disability	C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
C567017	Mental Retardation, Autosomal Recessive 6 (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL2109241 (PROTEIN COMPLEX GROUP), CHEMBL3038480 (PROTEIN COMPLEX), CHEMBL3683 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 944,840 (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
CHEMBL575060	GLUTAMIC ACID	3	929,756
CHEMBL275040	KAINIC ACID	2	15,084

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2518224	GRIK2		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: lgic — Ionotropic glutamate receptors

Most potent curated ligand interactions (7 total), top 7:

Ligand	Action	Affinity	Parameter
dysiherbaine	Full agonist	8.92	pKi
[3H]kainate	Full agonist	8.18	pKd
SYM2081	Agonist	8.0	pKi
domoic acid	Full agonist	7.74	pKi
kainate	Full agonist	7.49	pKi
LY339434	Agonist	4.92	pKi
BPAM344	Positive	4.1	pEC50

Binding affinities (BindingDB)

3 measured of 7 human assays (8 total across all organisms); most potent 3 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
SPD 502	KI	620 nM
NS3763	KI	1600 nM
LY-293558	KI	3200 nM

ChEMBL bioactivities

127 potent at pChembl≥5 of 177 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.92	Ki	1.2	nM	DYSIHERBAINE
8.22	Ki	6.04	nM	DOMOIC ACID
8.00	Ki	10	nM	2S,4R-4-METHYLGLUTAMATE
7.74	Ki	18.3	nM	DOMOATE
7.53	Ki	29.8	nM	CHEMBL121741
7.50	Ki	32	nM	KAINIC ACID
7.50	Ki	31.7	nM	CHEMBL431839
7.49	Ki	32.4	nM	KAINIC ACID
7.42	Ki	38.4	nM	CHEMBL120003
7.39	Ki	41.1	nM	CHEMBL332334
7.32	Ki	48	nM	CHEMBL59284
7.30	Ki	50	nM	CHEMBL1234118
7.28	Ki	53	nM	KAINIC ACID
7.26	Ki	54.3	nM	CHEMBL120785
7.24	Ki	57.4	nM	CHEMBL333015
7.23	Ki	59	nM	CHEMBL59284
7.16	Ki	70	nM	CHEMBL13076
7.11	IC50	77	nM	KAINIC ACID
7.08	Ki	82.2	nM	CHEMBL332467
7.04	Ki	90.6	nM	CHEMBL121113
7.03	Ki	93.5	nM	CHEMBL332168
6.97	Ki	107.8	nM	CHEMBL334119
6.96	Ki	110	nM	CHEMBL12696
6.96	Ki	110	nM	CHEMBL273675
6.91	Ki	122.5	nM	CHEMBL332818
6.90	Ki	126.2	nM	CHEMBL332114
6.89	Ki	130	nM	CHEMBL5591383
6.89	Ki	129.3	nM	CHEMBL121514
6.88	Ki	131.5	nM	CHEMBL120753
6.88	Ki	130.6	nM	CHEMBL333790
6.84	Ki	145.6	nM	CHEMBL120450
6.83	Ki	146.8	nM	CHEMBL120288
6.83	Ki	146.6	nM	CHEMBL122507
6.80	Ki	160	nM	CHEMBL59551
6.77	Ki	169.3	nM	CHEMBL121461
6.68	Ki	209.6	nM	CHEMBL368275
6.58	Ki	262.7	nM	CHEMBL331339
6.56	Ki	275.3	nM	CHEMBL431657
6.54	Ki	288	nM	CHEMBL118502
6.47	Ki	339	nM	CHEMBL58808
6.39	Ki	410	nM	CHEMBL268284
6.35	Ki	450	nM	CHEMBL38499
6.30	Ki	500	nM	CHEMBL61697
6.25	Ki	559	nM	CHEMBL294683
6.21	Ki	610	nM	CHEMBL13076
6.18	Ki	663.3	nM	CHEMBL123006
6.18	Ki	667	nM	CHEMBL334024
6.16	EC50	700	nM	KAINIC ACID
6.16	IC50	700	nM	CHEMBL3104225
6.16	Ki	700	nM	CHEMBL84142

PubChem BioAssay actives

101 with measured affinity, of 408 total; 50 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
(2R,3aR,6S,7R,7aR)-2-[(2S)-2-amino-2-carboxyethyl]-6-hydroxy-7-(methylamino)-3,3a,5,6,7,7a-hexahydrofuro[3,2-b]pyran-2-carboxylic acid	1325015: Displacement of [3H]kianic acid from recombinant GluK2 kainate receptor (unknown origin) expressed in HEK293 cell membranes measured after 1 hr	ki	0.0012	uM
(2S,3S,4S)-4-[(2Z,4E,6R)-6-carboxyhepta-2,4-dien-2-yl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	2114774: Displacement of [3H](2S, 4R)-4-MeGlu (SYM-2081) from GluK2 (unknown origin)	ki	0.0060	uM
(2S,4R)-2-amino-4-methylpentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.0100	uM
(3R,4E,6E)-7-[4,5-bis(1-hydroxyethenyl)pyrrolidin-3-yl]-3-methylocta-1,4,6-trien-2-ol	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0183	uM
(2S,3S,4S)-3-(carboxymethyl)-4-(1-phenylethenyl)pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0298	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-chlorophenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0317	uM
(2S,3S,4S)-3-(carboxymethyl)-4-prop-1-en-2-ylpyrrolidine-2-carboxylic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.0320	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-fluorophenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0384	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-methylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0411	uM
(2S,4R)-2-amino-4-[(E)-3-(2-methoxyphenyl)prop-2-enyl]pentanedioic acid	93267: Compound was tested for binding affinity against human Ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]-kainate as radioligand	ki	0.0480	uM
(3S,4aR,6S,8aR)-6-[[(2S)-2-carboxy-4,4-difluoropyrrolidin-1-yl]methyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid	1325319: Displacement of [3H]-kainate from human recombinant GluK2 receptor expressed in HEK293 cell membranes after 60 mins	ki	0.0500	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-fluoro-3-methylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0543	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-methoxyphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0574	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-ethylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0822	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(3-phenylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0906	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(3-methoxyphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.0935	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(3,4-dimethylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1078	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(3-methylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1225	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-[4-(2-phenylethoxy)phenyl]ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1262	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-[3-methyl-4-(2-phenylethoxy)phenyl]ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1293	uM
(2S,3S,4S)-4-[(2Z,5E)-6-carboxyhepta-2,5-dien-2-yl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	2114776: Displacement of [3H]-kainic acid from GluR6 (unknown origin) expressed in Sf9 cells membrane	ki	0.1300	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-phenylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1306	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-prop-1-en-2-ylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1315	uM
(2S,3S,4S)-4-[1-(4-butylphenyl)ethenyl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1456	uM
(2S,3S,4S)-4-[1-(4-butoxyphenyl)ethenyl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1466	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-propylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1468	uM
(2S,4R)-2-amino-4-prop-2-ynylpentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.1600	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(3,5-dimethylphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.1693	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(4-phenoxyphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.2096	uM
(2S,3S,4S)-4-[1-(4-tert-butylphenyl)ethenyl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.2627	uM
(2S,3S,4S)-4-[1-(3-butoxyphenyl)ethenyl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.2753	uM
(2S,3S,4S)-4-[1-(4-but-1-en-2-ylphenyl)ethenyl]-3-(carboxymethyl)pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.2880	uM
(2S,4R)-2-amino-4-[(Z)-3-phenylprop-2-enyl]pentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.3390	uM
(2S)-2-amino-4-methylidenepentanedioic acid	93265: Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 2 using cell membranes prepared from HEK293 cells	ki	0.4500	uM
(2S,4R)-2-amino-4-[(E)-2-methyl-3-phenylprop-2-enyl]pentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.5000	uM
(2S,4R)-2-amino-4-[(E)-3-(4-fluorophenyl)prop-2-enyl]pentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.5590	uM
2-[7-[3-[[(4-nitrophenyl)carbamoylamino]methyl]pyrrol-1-yl]-2,3-dioxo-6-(trifluoromethyl)-4H-quinoxalin-1-yl]acetic acid	75679: Binding affinity for human GluR6 expressed in HEK293 cells using [3]H-kainate	ki	0.6100	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-(3-methyl-4-pentoxyphenyl)ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.6633	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-[3-(2-phenylethoxy)phenyl]ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	0.6670	uM
1-ethyl-5-methoxy-2-(4-methoxyphenyl)-3-methylindole	1063863: Displacement of [3H]-kainate from GluK2 receptor (unknown origin)	ic50	0.7000	uM
(2S,4S)-2-amino-4-prop-2-ynylpentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	0.8230	uM
N-[7-fluoro-2,3-dioxo-6-(trifluoromethyl)-4H-quinoxalin-1-yl]-2-hydroxybenzamide	1859139: Binding affinity to GluK2 receptor (unknown origin)	ki	0.9080	uM
(2S,4R)-2-amino-4-(3-phenylprop-2-ynyl)pentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	1.0000	uM
glutamic acid	93265: Binding affinity of compound was determined against Ionotropic glutamate receptor ionotropic kainate 2 using cell membranes prepared from HEK293 cells	ki	1.1060	uM
(2S,4R)-2-amino-4-[(E)-3-(3-chlorophenyl)prop-2-enyl]pentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	1.1320	uM
3-(6-nitro-2,3-dioxo-7-pyrrol-1-yl-4H-quinoxalin-1-yl)propanoic acid	75679: Binding affinity for human GluR6 expressed in HEK293 cells using [3]H-kainate	ki	1.2000	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-[3-methoxy-4-(2-phenylethoxy)phenyl]ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	1.2840	uM
(2S,3S,4S)-3-(carboxymethyl)-4-[1-[4-(5-phenylpentoxy)phenyl]ethenyl]pyrrolidine-2-carboxylic acid	93266: Inhibition of [3H]kainate binding at ionotropic glutamate receptor kainate 2	ki	1.2957	uM
2-[6-nitro-2,3-dioxo-7-[3-[[4-(2-phenylethyl)piperazin-1-yl]methyl]pyrrol-1-yl]-4H-quinoxalin-1-yl]acetic acid	75679: Binding affinity for human GluR6 expressed in HEK293 cells using [3]H-kainate	ki	1.4000	uM
(2S,4R)-2-amino-4-[(E)-3-(2-chlorophenyl)prop-2-enyl]pentanedioic acid	93392: Binding affinity against human ionotropic glutamate receptor ionotropic kainate 2 in HEK293 cells using [3H]kainate as radioligand	ki	1.4040	uM

CTD chemical–gene interactions

34 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, decreases methylation	2
sodium arsenite	decreases expression, increases expression	2
Nickel	decreases expression	2
Valproic Acid	increases expression	2
aristolochic acid I	decreases expression	1
ethyl-p-hydroxybenzoate	decreases expression	1
trichostatin A	increases expression	1
zinc chloride	increases expression	1
butyraldehyde	decreases expression	1
pentanal	decreases expression	1
abrine	increases expression	1
bisphenol S	affects cotreatment, increases methylation	1
Temozolomide	increases expression	1
Sunitinib	increases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Benzo(a)pyrene	increases methylation	1
Benzoates	decreases activity, affects binding	1
Cannabidiol	increases expression	1
Diethylhexyl Phthalate	decreases expression	1
Doxorubicin	decreases expression	1
Endosulfan	increases expression	1
Estradiol	affects expression	1
Silicon Dioxide	decreases expression	1
Thimerosal	increases expression	1
Tobacco Smoke Pollution	decreases expression	1
Tretinoin	increases expression	1
Triclosan	decreases expression	1
Zinc	increases expression	1
Citalopram	affects response to substance	1
Aflatoxin B1	decreases methylation	1

ChEMBL screening assays

92 unique, capped per target: 66 binding, 26 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL6140042	Binding	Inhibition of kainate receptor (unknown origin) expressed in Xenopus oocytes at 5 uM by radioligand binding assay	Thienopyrimidinone Derivatives as a GluN2B/C/D Biased, Positive Allosteric Modulator of the N-Methyl-d-Aspartate Receptor. — J Med Chem
CHEMBL1226258	Functional	Agonist activity at iGluR6 L439C mutant expressed in human HEK293 cells assessed as increase in intracellular Ca2+ levels by FURA-2-M staining based fluorimetric method	Allosteric control of an ionotropic glutamate receptor with an optical switch. — Nat Chem Biol

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_D1JQ	PrecisION hGluR6-HEK	Transformed cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT05657860	PHASE4	COMPLETED	Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479	PHASE4	RECRUITING	Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829	PHASE4	WITHDRAWN	Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198	PHASE4	NOT_YET_RECRUITING	Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT01418118	PHASE4	COMPLETED	Assessment of the Effects of Pressors on Graft Blood Flow After Free Tissue Transfer Surgery
NCT03017053	PHASE4	UNKNOWN	The Optimal Neck Treatments Strategy of Early Oral Cancer Based on Adverse Pathological Factor
NCT03684707	PHASE4	UNKNOWN	Cancer Chemoprevention by Metformin Hydrochloride Compared to Placebo in Oral Potentially Malignant Lesions
NCT02270736	PHASE3	COMPLETED	Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability
NCT00158652	PHASE3	COMPLETED	Accelerated Radiotherapy and Concomitant Chemo-radiotherapy in HNSCC
NCT00158678	PHASE3	COMPLETED	IMRT Plus Cisplatin Versus Conventional Radiotherapy Plus Cisplatin in Stage III-IV HNSCC
NCT00402779	PHASE3	COMPLETED	Erlotinib Prevention of Oral Cancer (EPOC)
NCT00655421	PHASE3	UNKNOWN	Oral Cancer Screening in Mumbai, India by Primary Health Care Workers
NCT00750503	PHASE3	COMPLETED	Workplace Tobacco Cessation And Oral Cancer Screening Study
NCT00964977	PHASE3	COMPLETED	Effectiveness of Adjuvant Radiotherapy in Small Oropharyngeal Squamous Cell Cancer and Single Lymph Node Metastasis.
NCT01039298	PHASE3	UNKNOWN	Efficacy of Optically-guided Surgery in the Management of Early-staged Oral Cancer - COOLS TRIAL
NCT03685409	PHASE3	UNKNOWN	Cancer Chemoprevention by Metformin Hydrochloride in Oral Potentially Malignant Lesions
NCT05721755	PHASE3	ACTIVE_NOT_RECRUITING	Combining Radiation Therapy With Immunotherapy for the Treatment of Metastatic Squamous Cell Carcinoma of the Head and Neck
NCT06589804	PHASE3	RECRUITING	Testing the Addition of Anti-Cancer Drug, Cetuximab, to Standard of Care Treatment (Pembrolizumab) for Returning or Spreading Head and Neck Cancer After Previous Treatment
NCT06737822	PHASE3	RECRUITING	Upfront Surgery Vs Induction Chemotherapy Followed By Surgery In Oral Cancers:
NCT07402538	PHASE3	NOT_YET_RECRUITING	Surgery With or Without Neoadjuvant Treatment of SBRT Plus Chemoimmunotherapy in Resectable Locally Advanced Oral and HPV-unrelated Oropharyngeal Squamous Cell Carcinoma
NCT07441681	PHASE3	NOT_YET_RECRUITING	Comparing Radiation Plus Cetuximab to Radiation Plus Chemotherapy in People With Head and Neck Cancer Who Cannot Receive Cisplatin
NCT02304302	PHASE2	COMPLETED	Down Syndrome Memantine Follow-up Study
NCT03862950	PHASE2	COMPLETED	A Trial of Metformin in Individuals With Fragile X Syndrome (Met)
NCT04529226	PHASE2	UNKNOWN	Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis
NCT04821856	PHASE2	COMPLETED	Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability
NCT00330382	PHASE2	COMPLETED	Bowman-Birk Inhibitor Concentrate in Preventing Cancer in Patients With Oral Leukoplakia
NCT00400205	PHASE2	TERMINATED	Study of Induction Docetaxel, Cisplatin and 5-Fluorouracil
NCT00933387	PHASE2	COMPLETED	A Study of Neoadjuvant Bio-C/T Followed by Concurrent Bio-R/T in High-risk Locally Advanced Oral Squamous Cell Carcinoma
NCT01440270	PHASE2	COMPLETED	Neo-adjuvant Erbitux-based Chemotherapy for Locally Advanced Oral/Oropharyngeal Cancer
NCT01733797	PHASE2	COMPLETED	Trismus Trial of Therabite vs Wooden Spatula in Head and Neck Cancer Patients
NCT02734537	PHASE2	RECRUITING	Radiation Therapy With or Without Cisplatin in Treating Patients With Stage III-IVA Squamous Cell Carcinoma of the Head and Neck Who Have Undergone Surgery
NCT02960724	PHASE2	UNKNOWN	uPAR PET/CT for Staging Advanced and Localised Oral and Oropharyngeal Cancer
NCT03008694	PHASE2	UNKNOWN	Effect of FDG-PET/CT for Simulation and Radiation Treatment Planning in Oral Cancer Patients
NCT03174275	PHASE2	ACTIVE_NOT_RECRUITING	Carboplatin, Nab-Paclitaxel, Durvalumab Before Surgery and Adjuvant Therapy in Head and Neck Squamous Cell Carcinoma
NCT03383094	PHASE2	ACTIVE_NOT_RECRUITING	Chemoradiation vs Immunotherapy and Radiation for Head and Neck Cancer
NCT03529422	PHASE2	ACTIVE_NOT_RECRUITING	Durvalumab With Radiotherapy for Adjuvant Treatment of Intermediate Risk SCCHN
NCT04191460	PHASE2	RECRUITING	Fluorescence-guided Surgery Using cRGD-ZW800-1 in Oral Cancer
NCT04251949	PHASE2	COMPLETED	Evaluation of the Photobiomodulation Using LED Lamp for Curative Treatment of Radio-induced Mucositis.
NCT04541355	PHASE2	COMPLETED	Sodium Thiosulfate in Preventing Ototoxicity for Squamous Cell Cancer Patients Undergoing Chemoradiation With Cisplatin
NCT04862650	PHASE2	ACTIVE_NOT_RECRUITING	Cemiplimab, Low-Dose Paclitaxel and Carboplatin for the Treatment of Recurrent/Metastatic Squamous Cell Carcinoma of the Head and Neck