GRIN3B
gene geneOn this page
Also known as GluN3B
Summary
GRIN3B (glutamate ionotropic receptor NMDA type subunit 3B, HGNC:16768) is a protein-coding gene on chromosome 19p13.3, encoding Glutamate receptor ionotropic, NMDA 3B (O60391). Component of a non-conventional N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with low calcium permeability and low voltage-dependent block by Mg(2+).
The protein encoded by this gene is a subunit of an N-methyl-D-aspartate (NMDA) receptor. The encoded protein is found primarily in motor neurons, where it forms a heterotetramer with GRIN1 to create an excitatory glycine receptor. Variations in this gene have been proposed to be linked to schizophrenia.
Source: NCBI Gene 116444 — RefSeq curated summary.
At a glance
- GWAS associations: 3
- Clinical variants (ClinVar): 274 total
- Druggable target: yes — 22 molecules with ChEMBL bioactivity
- Dosage sensitivity (ClinGen): haploinsufficiency dosage sensitivity unlikely, triplosensitivity no evidence
- MANE Select transcript:
NM_138690
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:16768 |
| Approved symbol | GRIN3B |
| Name | glutamate ionotropic receptor NMDA type subunit 3B |
| Location | 19p13.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | GluN3B |
| Ensembl gene | ENSG00000116032 |
| Ensembl biotype | protein_coding |
| OMIM | 606651 |
| Entrez | 116444 |
Gene structure
Transcript identifiers
Ensembl transcripts: 2 — 1 protein_coding, 1 protein_coding_CDS_not_defined
ENST00000234389, ENST00000588335
RefSeq mRNA: 1 — MANE Select: NM_138690
NM_138690
CCDS: CCDS32861
Canonical transcript exons
ENST00000234389 — 9 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000769054 | 1000419 | 1000863 |
| ENSE00000769056 | 1003130 | 1003722 |
| ENSE00000769058 | 1004521 | 1005553 |
| ENSE00000769060 | 1007628 | 1007773 |
| ENSE00000769062 | 1007856 | 1007971 |
| ENSE00000769063 | 1008140 | 1008291 |
| ENSE00000769064 | 1008618 | 1008782 |
| ENSE00000769065 | 1008857 | 1008927 |
| ENSE00001492453 | 1009173 | 1009732 |
Expression profiles
Bgee: expression breadth ubiquitous, 144 present calls, max score 86.86.
Top tissues by expression
245 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| right uterine tube | UBERON:0001302 | 86.86 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 79.42 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 79.21 | silver quality |
| bronchial epithelial cell | CL:0002328 | 74.19 | gold quality |
| bronchus | UBERON:0002185 | 73.26 | gold quality |
| stromal cell of endometrium | CL:0002255 | 64.15 | gold quality |
| metanephros cortex | UBERON:0010533 | 64.01 | gold quality |
| right lung | UBERON:0002167 | 63.57 | gold quality |
| endocervix | UBERON:0000458 | 63.55 | gold quality |
| granulocyte | CL:0000094 | 63.12 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 62.89 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 62.73 | gold quality |
| spleen | UBERON:0002106 | 62.61 | gold quality |
| adenohypophysis | UBERON:0002196 | 62.61 | gold quality |
| pituitary gland | UBERON:0000007 | 62.48 | gold quality |
| tibial nerve | UBERON:0001323 | 62.47 | gold quality |
| mucosa of paranasal sinus | UBERON:0005030 | 61.61 | gold quality |
| nasal cavity mucosa | UBERON:0001826 | 61.46 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 60.94 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 60.85 | gold quality |
| left uterine tube | UBERON:0001303 | 60.53 | gold quality |
| thyroid gland | UBERON:0002046 | 60.50 | gold quality |
| ganglionic eminence | UBERON:0004023 | 60.19 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 60.16 | gold quality |
| cerebellar cortex | UBERON:0002129 | 60.03 | gold quality |
| ectocervix | UBERON:0012249 | 59.63 | gold quality |
| ventricular zone | UBERON:0003053 | 59.53 | gold quality |
| cerebellum | UBERON:0002037 | 58.87 | gold quality |
| cortex of kidney | UBERON:0001225 | 58.68 | gold quality |
| cortical plate | UBERON:0005343 | 58.33 | silver quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.52 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
11 targeting GRIN3B, 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-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-4482-3P | 99.98 | 72.50 | 3147 |
| HSA-LET-7C-3P | 99.95 | 73.42 | 2862 |
| HSA-MIR-6499-3P | 99.90 | 66.38 | 1212 |
| HSA-MIR-3177-5P | 99.65 | 70.38 | 1174 |
| HSA-MIR-6758-3P | 99.57 | 67.55 | 1078 |
| HSA-MIR-548G-3P | 99.48 | 68.67 | 2159 |
| HSA-MIR-548AV-3P | 99.43 | 68.50 | 1721 |
| HSA-MIR-138-2-3P | 98.91 | 68.33 | 1643 |
| HSA-MIR-6516-5P | 98.42 | 70.19 | 1551 |
| HSA-MIR-191-3P | 83.90 | 61.25 | 44 |
Functional genomics
ClinGen dosage: haploinsufficiency 40 (dosage sensitivity unlikely), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map
Literature-anchored findings (GeneRIF, showing 8)
- NR3B mRNA expression in the human hippocampal formation (CA1-CA4 and dentate gyrus) and adjacent neocortex may have implications for understanding the role of NMDA receptors for physiological and pathological processes in these forebrain regions. (PMID:15722182)
- cross-talk between NR3B and NR4A receptors is a mechanism modulating the transcriptional activities of these orphan nuclear receptors (PMID:17543277)
- We tested whether genetic dysfunction of GRIN3B is implicated in the pathogenesis of amyotrophic lateral sclerosis (ALS). (PMID:17687115)
- These observations suggest that the genetic variation of the NR3B subunit of the NMDA receptor is not a risk factor for Alzheimer’s dis pathogenesis (PMID:20016182)
- our findings suggest that the over-expression of NR3B subunit of NMDA receptor is a long lasting result of chronic opioid abuse. (PMID:20153313)
- Rs2240158 of GRIN3B was significantly associated with mismatch negativity in healthy subjects. (PMID:24814139)
- Authors investigated the significance of a common human genetic variation of the NMDAR NR3B subunit (PMID:25768306)
- GRIN3B missense mutation is an inherited risk factor for schizophrenia. (PMID:28132660)
Cross-species orthologs
43 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | grin3ba | ENSDARG00000005364 |
| danio_rerio | grin3bb | ENSDARG00000098667 |
| mus_musculus | Grin3b | ENSMUSG00000035745 |
| rattus_norvegicus | Grin3b | ENSRNOG00000012562 |
| 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), GRIA2 (ENSG00000120251), GRIA3 (ENSG00000125675), GRIK4 (ENSG00000149403), GRID2 (ENSG00000152208), GRIA4 (ENSG00000152578), GRIA1 (ENSG00000155511), GRIN2C (ENSG00000161509), GRIK3 (ENSG00000163873), GRIK2 (ENSG00000164418), GRIK1 (ENSG00000171189), GRIN1 (ENSG00000176884), GRID1 (ENSG00000182771), GRIN2A (ENSG00000183454), GRIN3A (ENSG00000198785), GRIN2B (ENSG00000273079)
Protein
Protein identifiers
Glutamate receptor ionotropic, NMDA 3B — O60391 (reviewed: O60391)
Alternative names: N-methyl-D-aspartate receptor subtype 3B
All UniProt accessions (1): O60391
UniProt curated annotations — full annotation on UniProt →
Function. Component of a non-conventional N-methyl-D-aspartate (NMDA) receptors (NMDARs) that function as heterotetrameric, ligand-gated cation channels with low calcium permeability and low voltage-dependent block by Mg(2+). Forms glutamatergic receptor complexes with GluN1 and GluN2 subunits which are activated by glycine binding to the GluN1 and GluN3 subunits and L-glutamate binding to GluN2 subunits. Forms excitatory glycinergic receptor complexes with GluN1 alone which are activated by glycine binding to the GluN1 and GluN3 subunits. GluN3B subunit also binds D-serine and, in the absence of glycine, activates glycinergic receptor complexes, but with lower efficacy than glycine. Each GluN3 subunit confers differential attributes to channel properties, including activation, deactivation and desensitization kinetics, pH sensitivity, Ca2(+) permeability, and binding to allosteric modulators.
Subunit / interactions. Forms heterotetrameric channels that contain at least two GluN1 subunits and at least a combination of one GluN2 and one GluN3 subunits (in vitro). Forms heterotetrameric channels composed of two GluN1/zeta subunits (GRIN1), and two identical GluN3 subunits (GRIN3A or GRIN3B) (in vitro). Does not form functional homomeric channels.
Subcellular location. Cell membrane. Postsynaptic cell membrane.
Similarity. Belongs to the glutamate-gated ion channel (TC 1.A.10.1) family. NR3B/GRIN3B subfamily.
RefSeq proteins (1): NP_619635* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001320 | Iontro_rcpt_C | Domain |
| IPR001508 | Iono_Glu_rcpt_met | Family |
| IPR015683 | Ionotropic_Glu_rcpt | Family |
| IPR019594 | Glu/Gly-bd | Domain |
| IPR028082 | Peripla_BP_I | Homologous_superfamily |
Pfam: PF00060, PF10613
Catalyzed reactions (Rhea), 2 shown:
- Ca(2+)(in) = Ca(2+)(out) (RHEA:29671)
- Na(+)(in) = Na(+)(out) (RHEA:34963)
UniProt features (58 total): sequence variant 26, binding site 10, topological domain 5, glycosylation site 5, region of interest 3, transmembrane region 3, disulfide bond 2, signal peptide 1, chain 1, compositionally biased region 1, intramembrane region 1
Structure
Experimental structures (PDB)
0 structures.
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O60391-F1 | 75.35 | 0.23 |
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 (10): 531; 533; 533; 538; 538; 701; 701; 702; 745; 745
Disulfide bonds (2): 439–475, 445–476
Glycosylation sites (5): 69, 344, 451, 465, 786
Function
Pathways and Gene Ontology
Reactome pathways
1 pathways
| ID | Pathway |
|---|---|
| R-HSA-9609736 | Assembly and cell surface presentation of NMDA receptors |
MSigDB gene sets: 117 (showing top):
GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GOMF_GLUTAMATE_GATED_RECEPTOR_ACTIVITY, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_REGULATION_OF_SYNAPTIC_PLASTICITY, GOBP_REGULATION_OF_POSTSYNAPTIC_MEMBRANE_POTENTIAL, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_ESTABLISHMENT_OF_PROTEIN_LOCALIZATION_TO_MEMBRANE, GOBP_SYNAPTIC_SIGNALING, GOBP_MEMBRANE_ORGANIZATION, GOBP_SYNAPTIC_TRANSMISSION_GLUTAMATERGIC, REACTOME_TRANSMISSION_ACROSS_CHEMICAL_SYNAPSES, GOBP_LOCALIZATION_WITHIN_MEMBRANE, GOBP_REGULATION_OF_TRANSPORT
GO Biological Process (12): ionotropic glutamate receptor signaling pathway (GO:0035235), synaptic transmission, glutamatergic (GO:0035249), regulation of synaptic plasticity (GO:0048167), modulation of chemical synaptic transmission (GO:0050804), protein insertion into membrane (GO:0051205), regulation of calcium ion transport (GO:0051924), monoatomic cation transmembrane transport (GO:0098655), monoatomic ion transport (GO:0006811), monoatomic ion transmembrane transport (GO:0034220), regulation of postsynaptic membrane potential (GO:0060078), calcium ion transmembrane transport (GO:0070588), regulation of presynaptic membrane potential (GO:0099505)
GO Molecular Function (12): monoatomic cation channel activity (GO:0005261), calcium channel activity (GO:0005262), glutamate receptor activity (GO:0008066), glycine binding (GO:0016594), neurotransmitter receptor activity (GO:0030594), ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential (GO:0099507), glycine-gated cation channel activity (GO:0160212), transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential (GO:1904315), NMDA glutamate receptor activity (GO:0004972), monoatomic ion channel activity (GO:0005216), ligand-gated monoatomic ion channel activity (GO:0015276), signaling receptor activity (GO:0038023)
GO Cellular Component (10): plasma membrane (GO:0005886), NMDA selective glutamate receptor complex (GO:0017146), presynaptic membrane (GO:0042734), neuronal cell body (GO:0043025), postsynaptic density membrane (GO:0098839), neurotransmitter receptor complex (GO:0098878), membrane (GO:0016020), monoatomic ion channel complex (GO:0034702), synapse (GO:0045202), postsynaptic membrane (GO:0045211)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Activation of NMDA receptors and postsynaptic events | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| glutamate-gated receptor activity | 2 |
| chemical synaptic transmission | 2 |
| calcium ion transport | 2 |
| regulation of membrane potential | 2 |
| monoatomic ion channel activity | 2 |
| transmitter-gated monoatomic ion channel activity | 2 |
| synaptic membrane | 2 |
| glutamate receptor signaling pathway | 1 |
| ligand-gated ion channel signaling pathway | 1 |
| modulation of chemical synaptic transmission | 1 |
| regulation of biological quality | 1 |
| regulation of trans-synaptic signaling | 1 |
| intracellular protein localization | 1 |
| membrane organization | 1 |
| establishment of protein localization to membrane | 1 |
| regulation of metal ion transport | 1 |
| monoatomic cation transport | 1 |
| monoatomic ion transmembrane transport | 1 |
| transport | 1 |
| monoatomic ion transport | 1 |
| transmembrane transport | 1 |
| monoatomic cation transmembrane transport | 1 |
| monoatomic cation transmembrane transporter activity | 1 |
| monoatomic cation channel activity | 1 |
| calcium ion transmembrane transporter activity | 1 |
| transmembrane signaling receptor activity | 1 |
| glutamate binding | 1 |
| amino acid binding | 1 |
| carboxylic acid binding | 1 |
| cation binding | 1 |
| signaling receptor activity | 1 |
| ligand-gated monoatomic ion channel activity | 1 |
| presynaptic membrane | 1 |
| regulation of presynaptic membrane potential | 1 |
| ligand-gated monoatomic cation channel activity | 1 |
| regulation of postsynaptic membrane potential | 1 |
| voltage-gated monoatomic ion channel activity | 1 |
| monoatomic ion transmembrane transporter activity | 1 |
| channel activity | 1 |
| ligand-gated channel activity | 1 |
Protein interactions and networks
STRING
880 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| GRIN3B | GRIN1 | P35437 | 990 |
| GRIN3B | GRIN2D | O15399 | 988 |
| GRIN3B | GRIN2A | Q12879 | 988 |
| GRIN3B | GRIN2B | Q13224 | 985 |
| GRIN3B | GRIN2C | Q14957 | 985 |
| GRIN3B | GRIN3A | Q8TCU5 | 981 |
| GRIN3B | KCND2 | Q9NZV8 | 571 |
| GRIN3B | BDNF | P23560 | 537 |
| GRIN3B | GRM4 | Q14833 | 489 |
| GRIN3B | ESRRG | P62508 | 480 |
| GRIN3B | CACNG2 | Q9Y698 | 466 |
| GRIN3B | GRM1 | Q13255 | 456 |
| GRIN3B | SLC7A1 | P30825 | 447 |
| GRIN3B | GRM8 | O00222 | 445 |
| GRIN3B | GRM6 | O15303 | 445 |
IntAct
3 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| GRIN3B | DAPK3 | psi-mi:“MI:0914”(association) | 0.350 |
| GRIN3B | TPD52L2 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (38): GRIN2A (Affinity Capture-Western), GRIN1 (Affinity Capture-Western), GRIN3B (Affinity Capture-Western), GRIN3B (Affinity Capture-Western), GRIN1 (Affinity Capture-Western), C19orf44 (Affinity Capture-MS), TPD52L1 (Affinity Capture-MS), C9orf16 (Affinity Capture-MS), EDEM2 (Affinity Capture-MS), ABCB9 (Affinity Capture-MS), DAPK3 (Affinity Capture-MS), MXRA7 (Affinity Capture-MS), HSPA5 (Affinity Capture-MS), CGRRF1 (Affinity Capture-MS), GRIN3A (Affinity Capture-MS)
ESM2 similar proteins: A6NGC4, A6NKX4, A6NM10, D3YZZ2, O35595, O46547, O60391, O77808, O95528, P30518, P43119, P46092, P46095, P48044, P48748, Q14626, Q3SYU3, Q3ZAV1, Q4U2R8, Q4W8A3, Q5RF19, Q5U419, Q64385, Q684M3, Q6UXD7, Q6UXT9, Q6YNI2, Q863Y8, Q86SM5, Q8CFZ5, Q8IXF9, Q8WUG5, Q91X56, Q924U0, Q96S37, Q99MF4, Q9BGL8, Q9BZ11, Q9H1Z9, Q9H228
Diamond homologs: A0A1L8F5J9, A2AIR5, O15399, O60391, Q8TCU5, Q8VHN2, Q91ZU9, Q9R1M7, A0A2R8QF68, A7XY94, B1AS29, B7ZSK1, O43424, P0AEQ3, P0AEQ4, P0AEQ5, P22756, P35436, P39086, P42264, Q00959, Q00960, Q00961, Q01097, Q01098, Q01812, Q03391, Q10914, Q12879, Q13003, Q13224, Q14957, Q38PU2, Q38PU4, Q5IS45, Q5R1P3, Q60934, Q61625, Q62645, Q63226
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
274 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 248 |
| Likely benign | 10 |
| Benign | 8 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
1580 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 19:1000887:G:GT | donor_gain | 1.0000 |
| 19:1003129:GAACC:G | acceptor_gain | 1.0000 |
| 19:1005549:CCAAG:C | donor_loss | 1.0000 |
| 19:1005551:AAGG:A | donor_loss | 1.0000 |
| 19:1005552:AGGT:A | donor_loss | 1.0000 |
| 19:1005555:T:A | donor_loss | 1.0000 |
| 19:1007774:G:GG | donor_gain | 1.0000 |
| 19:1007851:A:AG | acceptor_gain | 1.0000 |
| 19:1007852:G:GA | acceptor_gain | 1.0000 |
| 19:1007852:GCA:G | acceptor_gain | 1.0000 |
| 19:1007970:GG:G | donor_gain | 1.0000 |
| 19:1007971:GG:G | donor_gain | 1.0000 |
| 19:1007972:G:GG | donor_gain | 1.0000 |
| 19:1008243:GTG:G | donor_gain | 1.0000 |
| 19:1009171:AGC:A | acceptor_gain | 1.0000 |
| 19:1009172:GC:G | acceptor_gain | 1.0000 |
| 19:1009172:GCG:G | acceptor_gain | 1.0000 |
| 19:1000862:CGGT:C | donor_loss | 0.9900 |
| 19:1000864:G:GG | donor_gain | 0.9900 |
| 19:1000865:T:A | donor_loss | 0.9900 |
| 19:1003124:TCCCA:T | acceptor_loss | 0.9900 |
| 19:1003127:CA:C | acceptor_loss | 0.9900 |
| 19:1003128:A:AG | acceptor_gain | 0.9900 |
| 19:1003129:G:GA | acceptor_gain | 0.9900 |
| 19:1003129:G:GT | acceptor_loss | 0.9900 |
| 19:1003129:GA:G | acceptor_gain | 0.9900 |
| 19:1003129:GAA:G | acceptor_gain | 0.9900 |
| 19:1003129:GAAC:G | acceptor_gain | 0.9900 |
| 19:1004794:T:TA | acceptor_gain | 0.9900 |
| 19:1005554:G:GG | donor_gain | 0.9900 |
AlphaMissense
6604 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 19:1007882:T:C | F742S | 0.997 |
| 19:1007885:T:A | I743N | 0.996 |
| 19:1005131:T:C | F544L | 0.995 |
| 19:1005133:C:A | F544L | 0.995 |
| 19:1005133:C:G | F544L | 0.995 |
| 19:1007891:A:T | D745V | 0.995 |
| 19:1005092:A:C | S531R | 0.994 |
| 19:1005094:C:A | S531R | 0.994 |
| 19:1005094:C:G | S531R | 0.994 |
| 19:1007882:T:G | F742C | 0.994 |
| 19:1007959:T:C | F768L | 0.994 |
| 19:1007961:C:A | F768L | 0.994 |
| 19:1007961:C:G | F768L | 0.994 |
| 19:1007673:A:C | S700R | 0.993 |
| 19:1007675:C:A | S700R | 0.993 |
| 19:1007675:C:G | S700R | 0.993 |
| 19:1007879:C:A | A741D | 0.993 |
| 19:1007960:T:G | F768C | 0.993 |
| 19:1005132:T:C | F544S | 0.992 |
| 19:1007890:G:C | D745H | 0.992 |
| 19:1008246:G:C | W807C | 0.992 |
| 19:1008246:G:T | W807C | 0.992 |
| 19:1005098:A:C | S533R | 0.991 |
| 19:1005100:T:A | S533R | 0.991 |
| 19:1005100:T:G | S533R | 0.991 |
| 19:1007881:T:C | F742L | 0.991 |
| 19:1007883:C:A | F742L | 0.991 |
| 19:1007883:C:G | F742L | 0.991 |
| 19:1007903:T:C | L749P | 0.991 |
| 19:1005132:T:G | F544C | 0.990 |
dbSNP variants (sampled 300 via entrez): RS1000013465 (19:998835 AT>A,ATT), RS1000052882 (19:999889 T>A,C), RS1000058557 (19:1007447 T>TA), RS1000101552 (19:1000024 G>A), RS1000127338 (19:999843 C>A,T), RS1000481993 (19:1009991 C>G), RS1001217364 (19:1009352 T>C), RS1001511400 (19:1002021 C>T), RS1001631342 (19:1008692 C>G,T), RS1001656766 (19:1005576 G>A), RS1001761257 (19:999257 C>A,T), RS1001941197 (19:1004968 G>C), RS1002017434 (19:1007624 G>A), RS1002383281 (19:1008833 A>C,G), RS1002688173 (19:1009917 G>A,T)
Disease associations
OMIM: gene MIM:606651 | disease phenotypes:
GenCC curated gene-disease
Mondo (1): neurodevelopmental disorder (MONDO:0700092)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
3 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001963_1 | Alzheimer’s disease (late onset) | 2.000000e-09 |
| GCST005974_20 | Neutrophil count | 3.000000e-08 |
| GCST006804_167 | Red cell distribution width | 2.000000e-09 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004833 | neutrophil count |
| EFO:0009188 | Red cell distribution width |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D065886 | Neurodevelopmental Disorders | F03.625 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2094124 (PROTEIN COMPLEX GROUP), CHEMBL6066548 (PROTEIN COMPLEX)
Molecules with ChEMBL bioactivity
22 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,350,441 (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 |
|---|---|---|---|
| CHEMBL52440 | DEXTROMETHORPHAN | 4 | 33,223 |
| CHEMBL592 | LEVORPHANOL | 4 | 75,131 |
| CHEMBL660 | AMANTADINE | 4 | 69,750 |
| CHEMBL71 | CHLORPROMAZINE | 4 | 45,827 |
| CHEMBL742 | KETAMINE | 4 | 101,983 |
| CHEMBL807 | MEMANTINE | 4 | 34,597 |
| CHEMBL86715 | PROCYCLIDINE | 4 | 5,456 |
| CHEMBL900 | ORPHENADRINE | 4 | 8,087 |
| CHEMBL575060 | GLUTAMIC ACID | 3 | 929,756 |
| CHEMBL1254766 | DEXTRORPHAN | 2 | 6,521 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2 | 106 |
| CHEMBL17350 | TRAXOPRODIL | 2 | 2,547 |
| CHEMBL182066 | RADIPRODIL | 2 | 126 |
| CHEMBL22207 | RACEMETHORPHAN | 2 | 748 |
| CHEMBL275528 | PHENCYCLIDINE | 2 | 25,537 |
| CHEMBL284237 | DIZOCILPINE | 2 | 5,015 |
| CHEMBL289832 | LICOSTINEL | 2 | 566 |
| CHEMBL334491 | BUDIPINE | 2 | 2,513 |
| CHEMBL39664 | SELFOTEL | 2 | 2,588 |
| CHEMBL452461 | PERZINFOTEL | 2 | 364 |
| CHEMBL467084 | LANICEMINE | 2 | |
| CHEMBL299155 | TRANSTORINE | 1 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
3 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs2240158 | GRIN3B | 0.00 | 0 | ||
| rs2285906 | GRIN3B | 0.00 | 0 | ||
| rs2285907 | GRIN3B | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: lgic — Ionotropic glutamate receptors
ChEMBL bioactivities
439 potent at pChembl≥5 of 567 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.30 | IC50 | 0.5 | nM | CHEMBL276708 |
| 9.10 | IC50 | 0.8 | nM | CHEMBL12513 |
| 9.02 | Ki | 0.96 | nM | CHEMBL39881 |
| 9.00 | IC50 | 1 | nM | CHEMBL12804 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL12242 |
| 8.92 | Ki | 1.2 | nM | DIZOCILPINE |
| 8.85 | Ki | 1.4 | nM | CHEMBL5185347 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL537478 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL274422 |
| 8.82 | IC50 | 1.5 | nM | CHEMBL273662 |
| 8.77 | IC50 | 1.7 | nM | CHEMBL269683 |
| 8.71 | Ki | 1.94 | nM | CNS-5161 |
| 8.70 | IC50 | 2 | nM | CHEMBL536107 |
| 8.70 | Ki | 2 | nM | CHEMBL299294 |
| 8.64 | Ki | 2.3 | nM | CHEMBL39773 |
| 8.59 | Ki | 2.6 | nM | CHEMBL290738 |
| 8.59 | IC50 | 2.6 | nM | CHEMBL450325 |
| 8.52 | Ki | 3 | nM | CHEMBL5208012 |
| 8.52 | IC50 | 3 | nM | CHEMBL552664 |
| 8.52 | Ki | 3 | nM | CHEMBL166935 |
| 8.52 | Ki | 3 | nM | CHEMBL166991 |
| 8.51 | Ki | 3.1 | nM | CHEMBL290649 |
| 8.48 | Ki | 3.3 | nM | CHEMBL5208606 |
| 8.47 | Ki | 3.4 | nM | CHEMBL66626 |
| 8.46 | Ki | 3.5 | nM | CHEMBL50872 |
| 8.42 | Ki | 3.8 | nM | CHEMBL68831 |
| 8.42 | Ki | 3.8 | nM | CHEMBL306899 |
| 8.40 | IC50 | 4 | nM | CHEMBL363010 |
| 8.40 | IC50 | 4 | nM | BESONPRODIL |
| 8.40 | IC50 | 4 | nM | CHEMBL317229 |
| 8.40 | Ki | 4 | nM | CHEMBL354482 |
| 8.40 | Ki | 4 | nM | CHEMBL170552 |
| 8.40 | Ki | 4 | nM | CHEMBL169695 |
| 8.39 | IC50 | 4.1 | nM | CHEMBL557993 |
| 8.36 | Ki | 4.4 | nM | CHEMBL40730 |
| 8.36 | IC50 | 4.4 | nM | CHEMBL61720 |
| 8.35 | Ki | 4.5 | nM | CHEMBL100656 |
| 8.33 | IC50 | 4.7 | nM | CHEMBL297881 |
| 8.31 | Ki | 4.9 | nM | CHEMBL70918 |
| 8.30 | IC50 | 5 | nM | CHEMBL363722 |
| 8.30 | Ki | 5 | nM | CHEMBL166697 |
| 8.29 | Ki | 5.1 | nM | CHEMBL38994 |
| 8.25 | Ki | 5.6 | nM | CHEMBL305195 |
| 8.23 | IC50 | 5.9 | nM | LICOSTINEL |
| 8.22 | IC50 | 6 | nM | RADIPRODIL |
| 8.22 | IC50 | 6 | nM | CHEMBL305195 |
| 8.22 | Ki | 6 | nM | CHEMBL305195 |
| 8.22 | IC50 | 6 | nM | CHEMBL126929 |
| 8.18 | Ki | 6.6 | nM | CHEMBL289607 |
| 8.17 | Ki | 6.8 | nM | DIZOCILPINE |
PubChem BioAssay actives
376 with measured affinity, of 875 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 |
|---|---|---|---|---|
| (2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylphosphonic acid | 144039: Compound was tested in vitro for its inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor by using [3H]CGP-39653 binding assay | ic50 | 0.0005 | uM |
| [7-(4-chlorophenyl)-2,3-dioxo-1,4-dihydroquinoxalin-5-yl]methylphosphonic acid | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0008 | uM |
| (7-fluoro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylphosphonic acid | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0010 | uM |
| 2-[(12S)-7-bromo-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]-N-phenylacetamide | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0010 | uM |
| (1S,9R)-1-methyl-16-azatetracyclo[7.6.1.02,7.010,15]hexadeca-2,4,6,10,12,14-hexaene | 156805: The compound was tested for its ability to block PCP N-methyl-D-aspartate glutamate receptor at the PCP (phencyclidine) binding site in postmortem human frontal cortex. | ki | 0.0012 | uM |
| [hydroxy-(7-nitro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl]phosphonic acid | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0012 | uM |
| 2-[(11S)-7-bromo-11-ethyl-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]acetic acid | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0014 | uM |
| (7-bromo-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylphosphonic acid | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0015 | uM |
| [(2,3-dioxo-1,4-dihydroquinoxalin-5-yl)-hydroxymethyl]phosphonic acid | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0015 | uM |
| [(benzylamino)-(7-nitro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl]phosphonic acid;hydrobromide | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0015 | uM |
| (7-chloro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methylphosphonic acid | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0017 | uM |
| 2-(2-chloro-5-methylsulfanylphenyl)-1-methyl-1-(3-methylsulfanylphenyl)guanidine | 143453: In vitro displacement of [3H]MK-801 from N-methyl-D-aspartate glutamate receptor | ki | 0.0019 | uM |
| [(benzylamino)-(2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl]phosphonic acid;hydrobromide | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0020 | uM |
| 2-[[2-(3,4-dihydro-1H-isoquinolin-2-yl)-4-pyridinyl]amino]ethanol | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0020 | uM |
| 2-[(12S)-7-bromo-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]acetic acid | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0023 | uM |
| 2-(7-bromo-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl)-N-phenylacetamide | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0026 | uM |
| 6,7-dichloro-5-[1-(1,2,4-triazol-4-yl)propyl]-1,4-dihydroquinoxaline-2,3-dione | 1859120: Displacement of [3H]L-689560 from NMDA receptor (unknown origin) | ic50 | 0.0026 | uM |
| 2-[(11S)-7-bromo-11-methyl-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]-N-phenylacetamide | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0030 | uM |
| [(cyclohexylmethylamino)-(7-nitro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl]phosphonic acid;hydrochloride | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0030 | uM |
| 2-(3,4-dihydro-1H-isoquinolin-2-yl)pyridin-4-amine | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0030 | uM |
| 2-(3,4-dihydro-1H-isoquinolin-2-yl)-6-ethylpyridin-4-amine | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0030 | uM |
| 2-[(11S)-7-chloro-11-methyl-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]-N-phenylacetamide | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0031 | uM |
| 2-[(11S)-7-bromo-11-methyl-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]acetic acid | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0033 | uM |
| 4-[3-(4-benzylpiperidin-1-yl)-2-methylpropyl]phenol | 143454: Displacement of [3H]25-6981 from N-methyl-D-aspartate glutamate receptor | ki | 0.0034 | uM |
| 2-[[2-(3,4-dihydro-1H-isoquinolin-2-yl)quinolin-4-yl]amino]ethanol | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0035 | uM |
| 4-[3-(4-benzylpiperidin-1-yl)-1-hydroxypropyl]phenol | 143454: Displacement of [3H]25-6981 from N-methyl-D-aspartate glutamate receptor | ki | 0.0038 | uM |
| 4-[3-(4-benzylpiperidin-1-yl)-2-hydroxypropyl]phenol | 143454: Displacement of [3H]25-6981 from N-methyl-D-aspartate glutamate receptor | ki | 0.0038 | uM |
| 2-(4-benzylpiperidin-1-yl)-2-oxo-N-(2-oxo-1,3-dihydrobenzimidazol-5-yl)acetamide | 241037: Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor | ic50 | 0.0040 | uM |
| 6-[2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethylsulfinyl]-3H-1,3-benzoxazol-2-one | 143455: Inhibition of [3H]Ro-256981 binding to N-methyl-D-aspartate glutamate receptor | ic50 | 0.0040 | uM |
| 1-[2-(4-hydroxyphenoxy)ethyl]-4-[(4-methylphenyl)methyl]piperidin-4-ol | 241037: Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor | ic50 | 0.0040 | uM |
| [4-amino-6-(3,4-dihydro-1H-isoquinolin-2-yl)-2-pyridinyl]methanol | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0040 | uM |
| 2-[[2-(3,4-dihydro-1H-isoquinolin-2-yl)-6-methyl-4-pyridinyl]amino]ethanol | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0040 | uM |
| 2-(3,4-dihydro-1H-isoquinolin-2-yl)-5-methylpyridin-4-amine | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0040 | uM |
| [(furan-2-ylmethylamino)-(7-nitro-2,3-dioxo-1,4-dihydroquinoxalin-5-yl)methyl]phosphonic acid;hydrobromide | 144043: In vitro inhibitory activity at 1 uM concentration against N-methyl-D-aspartate glutamate receptor, using [3H]CGP-39653 binding assay | ic50 | 0.0041 | uM |
| 6,7-dichloro-5-[(1-propylimidazol-4-yl)methyl]-1,4-dihydroquinoxaline-2,3-dione | 1859120: Displacement of [3H]L-689560 from NMDA receptor (unknown origin) | ic50 | 0.0044 | uM |
| 2-[(11S)-7-chloro-11-methyl-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl]acetic acid | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0044 | uM |
| (1S,9R)-10-[(2R)-2-methoxypropyl]-1,13,13-trimethyl-10-azatricyclo[7.3.1.02,7]trideca-2(7),3,5-trien-5-ol | 1960006: Antagonist activity at NMDA receptor (unknown origin) assessed as inhibition constant | ki | 0.0045 | uM |
| 7-chloro-6-methyl-5-nitro-1,4-dihydroquinoxaline-2,3-dione | 143443: Inhibition of [3H]DCKA binding to N-methyl-D-aspartate glutamate receptor | ic50 | 0.0047 | uM |
| 1-[(2R)-2-hydroxy-3-(4-hydroxyphenyl)propyl]-4-[(4-methylphenyl)methyl]piperidin-4-ol | 143454: Displacement of [3H]25-6981 from N-methyl-D-aspartate glutamate receptor | ki | 0.0049 | uM |
| 2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]-2-oxo-N-(2-oxo-1,3-dihydrobenzimidazol-5-yl)acetamide | 241037: Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor | ic50 | 0.0050 | uM |
| 2-(3,4-dihydro-1H-isoquinolin-2-yl)-6-methylpyridin-4-amine | 143451: Binding affinity against NMDA receptor by displacement of [3H]Ro-256981 | ki | 0.0050 | uM |
| 2-(7-chloro-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl)acetic acid | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0051 | uM |
| 4-[(1R,2S)-3-(4-benzylpiperidin-1-yl)-1-hydroxy-2-methylpropyl]phenol | 143454: Displacement of [3H]25-6981 from N-methyl-D-aspartate glutamate receptor | ki | 0.0056 | uM |
| 6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dione | 143443: Inhibition of [3H]DCKA binding to N-methyl-D-aspartate glutamate receptor | ic50 | 0.0059 | uM |
| 2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]-2-oxo-N-(2-oxo-3H-1,3-benzoxazol-6-yl)acetamide | 241037: Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor | ic50 | 0.0060 | uM |
| (4-benzylpiperidin-1-yl)-(4,6-dihydroxy-1H-indol-2-yl)methanone | 143455: Inhibition of [3H]Ro-256981 binding to N-methyl-D-aspartate glutamate receptor | ic50 | 0.0060 | uM |
| 2-(7-chloro-2,3-dioxo-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13)-trien-12-yl)-N-phenylacetamide | 1859114: Displacement of [3H]DCKA from NMDA receptor (unknown origin) | ki | 0.0066 | uM |
| 5,6,7-trichloro-4-hydroxy-3-nitroso-1H-quinolin-2-one | 143443: Inhibition of [3H]DCKA binding to N-methyl-D-aspartate glutamate receptor | ic50 | 0.0070 | uM |
| 1-[(1S,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol | 241037: Inhibition of [3H]-Ro-25-6981 binding to NMDA receptor | ic50 | 0.0070 | uM |
| (1R)-1-(4-chlorophenyl)-2-[(1R)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]ethanol | 238983: Mean inhibitory constant against porcine N-methyl-D-aspartate (NMDA) glutamate receptor; n=3 | ki | 0.0070 | uM |
CTD chemical–gene interactions
24 total (human), top 24 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | decreases expression, increases expression | 3 |
| Estradiol | affects expression, affects cotreatment, increases expression | 2 |
| triphenyl phosphate | affects expression | 1 |
| propionaldehyde | increases expression | 1 |
| ferrous chloride | decreases expression | 1 |
| nutlin 3 | affects cotreatment, increases expression | 1 |
| ICG 001 | increases expression | 1 |
| abrine | decreases expression | 1 |
| bisphenol S | decreases expression | 1 |
| jinfukang | affects cotreatment, increases expression | 1 |
| 4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid | increases expression | 1 |
| Air Pollutants | affects expression, increases abundance | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Camptothecin | increases expression | 1 |
| Cisplatin | affects cotreatment, increases expression | 1 |
| Dactinomycin | affects cotreatment, increases expression | 1 |
| Methotrexate | affects response to substance | 1 |
| Oxygen | increases expression | 1 |
| Ozone | affects expression, increases abundance | 1 |
| Phthalic Acids | increases methylation | 1 |
| Rotenone | increases expression | 1 |
| Tobacco Smoke Pollution | decreases expression | 1 |
| Valproic Acid | increases methylation | 1 |
| Aflatoxin B1 | increases methylation | 1 |
ChEMBL screening assays
182 unique, capped per target: 170 binding, 7 functional, 4 admet, 1 toxicity
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1247908 | Binding | Binding affinity to human recombinant NMDA receptor | Spiroindolones, a potent compound class for the treatment of malaria. — Science |
| CHEMBL2208698 | Functional | Antagonist activity at NMDA receptor (unknwon origin) | Synopsis of some recent tactical application of bioisosteres in drug design. — J Med Chem |
| CHEMBL4680007 | ADMET | Inhibition of NMDA receptor (unknown origin) | Fragment-Based Discovery of Novel Allosteric MEK1 Binders. — ACS Med Chem Lett |
Cellosaurus cell lines
1 cell lines: 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D9FU | Ubigene HEK293 GRIN3B KO | Transformed cell line | Female |
Clinical trials (associated diseases)
202 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT04586348 | PHASE4 | UNKNOWN | Prenatal Iodine Supplementation and Early Childhood Neurodevelopment |
| NCT04873115 | PHASE4 | UNKNOWN | Double-blind, Placebo-controlled, Randomized Clinical Trial Comparing the Efficacy and Safety of Sialanar Plus orAl rehabiLitation Against Placebo Plus Oral Rehabilitation for chIldren and Adolescents With seVere Sialorrhoea and Neurodisabilties, |
| NCT02559102 | PHASE3 | COMPLETED | Dexmedetomidine Sedation Versus General Anaesthesia for Inguinal Hernia Surgery in Infants |
| NCT02757079 | PHASE3 | COMPLETED | Study of the Efficacy and Safety of NPC-15 for Sleep Disorders of Children With Neurodevelopmental Disorders |
| NCT06915480 | PHASE3 | RECRUITING | Reducing Missed Appointments |
| NCT07377032 | PHASE3 | RECRUITING | TAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders |
| NCT02909959 | PHASE2 | COMPLETED | Sulforaphane for the Treatment of Young Men With Autism Spectrum Disorder |
| NCT06081348 | PHASE2 | RECRUITING | Sertraline vs. Placebo in the Treatment of Anxiety in Children and AdoLescents With NeurodevelopMental Disorders |
| NCT06352372 | PHASE2 | COMPLETED | Safety and Efficacy of tPBM for Epileptiform Activity in Autism |
| NCT00503191 | PHASE1 | COMPLETED | NeuroModulation Technique Treatment of Autism |
| NCT04475848 | PHASE1 | COMPLETED | A Study to Investigate the Safety, Tolerability, Pharmacokinetics, Pharmacodynamics and Food Effect of RO6953958 in Healthy Participants |
| NCT06300398 | PHASE1 | COMPLETED | IAMA-6 Oral Dose Study in Healthy Adults |
| NCT01783041 | PHASE2/PHASE3 | COMPLETED | Effect of Early L-Carnitine Supplementation on Neurodevelopmental Outcomes in Very Preterm Infants |
| NCT05767385 | PHASE2/PHASE3 | RECRUITING | Fetal Cerebrovascular Autoregulation in Congenital Heart Disease and Association With Neonatal Neurobehavior |
| NCT05675098 | EARLY_PHASE1 | NOT_YET_RECRUITING | Central Nervous System Stimulants and Physical Function in Children With Cerebral Palsy |
| NCT00783783 | Not specified | COMPLETED | CYP2D6 Pharmacogenetics in Risperidone-Treated Children |
| NCT01778504 | Not specified | RECRUITING | Studying Childhood-onset Behavioral, Psychiatric, and Developmental Disorders |
| NCT01850784 | Not specified | UNKNOWN | High Energy Formula Feeding in Infants With Congenital Heart Disease |
| NCT01922791 | Not specified | COMPLETED | Nutrition and Pregnancy Intervention Study |
| NCT01942525 | Not specified | UNKNOWN | Influence of Intrauterine Growth Restriction on Amplitude-integrated EEG in Preterm Infants |
| NCT02003170 | Not specified | COMPLETED | Etiology and Early Diagnosis of Neurodevelopmental Disorders |
| NCT02118649 | Not specified | ACTIVE_NOT_RECRUITING | Enhancing Behavior and Brain Response to Visual Targets Using a Computer Game |
| NCT02557191 | Not specified | TERMINATED | Biomarkers, Neurodevelopment and Preterm Infants |
| NCT02690675 | Not specified | COMPLETED | Iron Supplement Effect on Child Development |
| NCT02694003 | Not specified | COMPLETED | Better Nights, Better Days for Children With Neurodevelopment Disorders |
| NCT02792894 | Not specified | COMPLETED | Family Networks (FaNs) for Children With Developmental Disorders and Delays |
| NCT02871674 | Not specified | UNKNOWN | Good Night Project: Behavioural Sleep Interventions for Children With ADHD: A Randomised Controlled Trial |
| NCT02887157 | Not specified | COMPLETED | Analyzing Retinal Microanatomy in ROP |
| NCT02898298 | Not specified | COMPLETED | Positive Emotion Regulation Training in Children, Adolescents and Young Adults With and Without Developmental Disorder |
| NCT02912780 | Not specified | UNKNOWN | Introduction of Microsystems in a Level 3 Neonatal Intensive Care Unit |
| NCT03023293 | Not specified | COMPLETED | n-3 PUFAs, Irisin and Maternal Glucose Metabolism From Pregnancy to Postpartum |
| NCT03023644 | Not specified | COMPLETED | Improving Neurodevelopmental Outcomes in Children With Congenital Heart Disease: An Intervention Study |
| NCT03032991 | Not specified | UNKNOWN | Early Biomarkers of Neurodevelopment in Offspring of Diabetic Mothers |
| NCT03088189 | Not specified | TERMINATED | Effect of Parental Peri-conceptional Vitamin B12 Supplementation on Infant Neurocognitive Development in Offspring |
| NCT03096028 | Not specified | COMPLETED | Developmental Origins of Mental Health Disorders |
| NCT03148782 | Not specified | COMPLETED | Brain Plasticity Underlying Acquisition of New Organizational Skills in Children-R61 Phase |
| NCT03172104 | Not specified | COMPLETED | Neurobehavioural Development of Infants Born <30 Weeks Gestational Age Between Birth and Five Years of Age |
| NCT03222375 | Not specified | RECRUITING | SQUED™ Series 28.1 Home-use and Treatment of Autowave Reverberator of Autism |
| NCT03229928 | Not specified | COMPLETED | Clinical Testing of a Real-Time Behavior Measurement Tool: Measuring Outcomes for CHAnge |
| NCT03232489 | Not specified | UNKNOWN | Study for the Evaluation of the Feasibility of Applying Advanced MRI Scanning in Pediatric Clinical Practice |
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.