Details of the Target

General Information of Target

Target ID LDTP05459
Target Name Glutamate receptor ionotropic, NMDA 1 (GRIN1)
Gene Name GRIN1
Gene ID 2902
Synonyms
NMDAR1; Glutamate receptor ionotropic, NMDA 1; GluN1; Glutamate [NMDA] receptor subunit zeta-1; N-methyl-D-aspartate receptor subunit NR1; NMD-R1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTMRLLTLALLFSCSVARAACDPKIVNIGAVLSTRKHEQMFREAVNQANKRHGSWKIQL
NATSVTHKPNAIQMALSVCEDLISSQVYAILVSHPPTPNDHFTPTPVSYTAGFYRIPVLG
LTTRMSIYSDKSIHLSFLRTVPPYSHQSSVWFEMMRVYSWNHIILLVSDDHEGRAAQKRL
ETLLEERESKAEKVLQFDPGTKNVTALLMEAKELEARVIILSASEDDAATVYRAAAMLNM
TGSGYVWLVGEREISGNALRYAPDGILGLQLINGKNESAHISDAVGVVAQAVHELLEKEN
ITDPPRGCVGNTNIWKTGPLFKRVLMSSKYADGVTGRVEFNEDGDRKFANYSIMNLQNRK
LVQVGIYNGTHVIPNDRKIIWPGGETEKPRGYQMSTRLKIVTIHQEPFVYVKPTLSDGTC
KEEFTVNGDPVKKVICTGPNDTSPGSPRHTVPQCCYGFCIDLLIKLARTMNFTYEVHLVA
DGKFGTQERVNNSNKKEWNGMMGELLSGQADMIVAPLTINNERAQYIEFSKPFKYQGLTI
LVKKEIPRSTLDSFMQPFQSTLWLLVGLSVHVVAVMLYLLDRFSPFGRFKVNSEEEEEDA
LTLSSAMWFSWGVLLNSGIGEGAPRSFSARILGMVWAGFAMIIVASYTANLAAFLVLDRP
EERITGINDPRLRNPSDKFIYATVKQSSVDIYFRRQVELSTMYRHMEKHNYESAAEAIQA
VRDNKLHAFIWDSAVLEFEASQKCDLVTTGELFFRSGFGIGMRKDSPWKQNVSLSILKSH
ENGFMEDLDKTWVRYQECDSRSNAPATLTFENMAGVFMLVAGGIVAGIFLIFIEIAYKRH
KDARRKQMQLAFAAVNVWRKNLQDRKSGRAEPDPKKKATFRAITSTLASSFKRRRSSKDT
STGGGRGALQNQKDTVLPRRAIEREEGQLQLCSRHRES
Target Type
Successful
Target Bioclass
Transporter and channel
Family
Glutamate-gated ion channel (TC 1.A.10.1) family, NR1/GRIN1 subfamily
Subcellular location
Cell membrane
Function
Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+). Sensitivity to glutamate and channel kinetics depend on the subunit composition.
TTD ID
T62276
Uniprot ID
Q05586
DrugMap ID
TTLD29N
Ensemble ID
ENST00000371546.8
HGNC ID
HGNC:4584
ChEMBL ID
CHEMBL2015

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT116 SNV: p.A235D; p.T302A .
HKGZCC SNV: p.A234T .
KYSE510 SNV: p.P660S .
LNCaP clone FGC SNV: p.S352N .
NCIH2291 SNV: p.R468W .
OV90 SNV: p.A524P .
PF382 SNV: p.A515V .
RKO SNV: p.I464V .
RL952 Deletion: p.F754SfsTer7 .
SUPT1 SNV: p.R233H .
SW480 SNV: p.V218I .
SW620 SNV: p.V218I .
TE4 SNV: p.C22F; p.R52Q .
TOV21G SNV: p.E716Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Acrolein
 Probe Info  		N.A.  LDD0226  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0109  NEM HeLa N.A.  LDD0226  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Glutamate receptor ionotropic, NMDA 2B (GRIN2B) Glutamate-gated ion channel family Q13224
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
RNA-binding protein FUS (FUS) RRM TET family P35637

The Drug(s) Related To This Target

Approved
Click To Hide/Show 21 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acamprosate Small molecular drug DB00659
Acetylcysteine Small molecular drug DB06151
Aripiprazole Small molecular drug DB01238
Atomoxetine Small molecular drug DB00289
Cycloserine Small molecular drug D02WFK
Dextropropoxyphene Small molecular drug DB00647
Donepezil Small molecular drug DB00843
Enflurane Small molecular drug DB00228
Glutamic Acid Small molecular drug DB00142
Memantine Small molecular drug DB01043
Meperidine Small molecular drug DB00454
Methadone Small molecular drug DB00333
Milnacipran Small molecular drug DB04896
Orphenadrine Small molecular drug DB01173
Pentobarbital Small molecular drug DB00312
Phenobarbital Small molecular drug DB01174
Prasterone Small molecular drug DB01708
Secobarbital Small molecular drug DB00418
Tramadol Small molecular drug DB00193
Esketamine . DB11823
Fluciclovine (18f) . DB13146
Phase 4
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
D-serine Small molecular drug D02UDJ
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Eliprodil Small molecular drug D0S8CI
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Nbqx Small molecular drug D02VKC
Investigative
Click To Hide/Show 95 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(+)-ha966 Small molecular drug D08TAN
(D)-ala-pro-glu Small molecular drug D0S5OQ
(R)-2-amino-5-phosphono-pentanoic Acid Small molecular drug D09ISB
(R)-2-amino-7-phosphono-heptanoic Acid Small molecular drug D01LDO
(Rs)-(Tetrazol-5-yl)Glycine Small molecular drug D0FW8K
1,3-ditolylguanidine Small molecular drug D02WJT
2-(4-phenoxy-benzyl)-1h-benzoimidazole Small molecular drug D04ZFH
2-(4-phenoxy-benzyl)-3h-benzoimidazol-4-ol Small molecular drug D0T0GA
2-(4-phenoxy-benzyl)-3h-benzoimidazol-5-ol Small molecular drug D05IGJ
2-(4-phenoxy-benzyl)-3h-benzoimidazol-5-ylamine Small molecular drug D01BQD
2-methylamino-succinic Acid(Nmda) Small molecular drug D06GKL
2-pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Small molecular drug D0B4DP
3-benzoyl-7-chloro-4-hydroxy-1h-quinolin-2-one Small molecular drug D0Q6QW
3-carbamoyl-6-chloro-1h-indole-2-carboxylic Acid Small molecular drug D0X7BP
3-hydroxy-1h-benzo[B]Azepine-2,5-dione Small molecular drug D0S5RV
3-hydroxy-6-methyl-1h-benzo[B]Azepine-2,5-dione Small molecular drug D0L4QC
3-hydroxy-7-nitro-1h-benzo[B]Azepine-2,5-dione Small molecular drug D01MSM
3-hydroxy-8-methyl-1h-benzo[B]Azepine-2,5-dione Small molecular drug D01XWL
3-phenyl-4-hydroxyquinolin-2(1h)-one Small molecular drug D0W0VK
4,5,7-trichloro-3-hydroxy-1h-quinolin-2-one Small molecular drug D0H7PR
4,6-dichloro-1h-indole-2-carboxylic Acid Small molecular drug D03GBO
4-(3,4-dihydro-1h-isoquinolin-2-yl)-quinoline Small molecular drug D0K9NW
4-benzyl-1-(2-phenoxy-ethyl)-piperidine Small molecular drug D0J8PY
4-bromo-3-hydroxy-1h-quinolin-2-one Small molecular drug D00KGK
4-bromo-5,7-dichloro-3-hydroxy-1h-quinolin-2-one Small molecular drug D0D5HM
4-hydroxy-5-phenylthieno[2,3-b]Pyridin-6(7h)-one Small molecular drug D0Q8NW
4-[2-(3-phenyl-propylamino)-ethyl]-phenol Small molecular drug D07RFM
4-[2-(4-benzyl-piperidin-1-yl)-ethoxy]-phenol Small molecular drug D09BZV
4-[2-(4-phenyl-butoxy)-ethyl]-phenol Small molecular drug D06NIS
4-[2-(4-phenyl-butylamino)-ethyl]-phenol Small molecular drug D0W0HN
4-[2-(4-phenyl-piperidin-1-yl)-ethoxy]-phenol Small molecular drug D0Q8PE
4-[2-(5-phenyl-pentylamino)-ethyl]-phenol Small molecular drug D03CAE
4-[2-(6-phenyl-hexylamino)-ethyl]-phenol Small molecular drug D06QXT
4-[3-(4-phenyl-butylamino)-propyl]-phenol Small molecular drug D05WZA
4-[3-(5-phenyl-pentylamino)-propyl]-phenol Small molecular drug D0A5ET
4-{2-[Ethyl-(4-phenyl-butyl)-amino]-ethyl}-phenol Small molecular drug D0V5IZ
5,6,7-trichloro-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D0D4IG
5,7-dibromo-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D07DHN
5,7-dichloro-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D06NYB
5,7-dichloro-4-hydroxy-3-phenyl-1h-quinolin-2-one Small molecular drug D0L7RU
5,7-dichlorokynurenic Acid Small molecular drug D04DHB
5,7-dinitro-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D0P4RL
57-dichlorokynurenic Acid Small molecular drug DB01931
6,7-dichloro-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D0S6TW
6,7-dichloro-3-hydroxy-1h-quinazoline-2,4-dione Small molecular drug D06SZG
6-chloro-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D07QBQ
6-methoxy-2-(4-phenoxy-benzyl)-1h-benzoimidazole Small molecular drug D00HET
6-nitro-1,4-dihydro-quinoxaline-2,3-dione Small molecular drug D0J3EZ
6-nitro-2-(4-phenoxy-benzyl)-1h-benzoimidazole Small molecular drug D0P1YK
7-chloro-3-hydroxyquinazoline-2,4-dione Small molecular drug D05VVC
8-bromo-3-hydroxy-1h-benzo[B]Azepine-2,5-dione Small molecular drug D04ZJL
8-chloro-3-hydroxy-1h-benzo[B]Azepine-2,5-dione Small molecular drug D0V1PE
8-ethyl-3-hydroxy-1h-benzo[B]Azepine-2,5-dione Small molecular drug D08FBB
8-fluoro-3-hydroxy-1h-benzo[B]Azepine-2,5-dione Small molecular drug D0LE0E
Agmatine Small molecular drug DB08838
Ala-pro-glu Small molecular drug D03NWI
Ap-7 Small molecular drug D0OZ2F
Benzyl 4-aminobutyl(3-aminopropyl)Carbamate Small molecular drug D0U8ZQ
Cgp61594 Small molecular drug D0F5ZW
Cns-5161 Small molecular drug DB05824
Cycloleucine Small molecular drug D0P0GT
D-aspartic Acid Small molecular drug D08CAB
Dnqx Small molecular drug D05KQC
Gly-amp-glu Small molecular drug D0T7TB
Gly-b7pro-glu Small molecular drug D0ZL5U
Gly-hyp-glu Small molecular drug D0P3MF
Gly-pip-glu Small molecular drug D0BC2N
H-gly-d-dmp-glu-oh Small molecular drug D07OBI
H-gly-dmp-glu-oh Small molecular drug D01JHR
Homoquinolinic Acid Small molecular drug D0B5ZA
Ifenprodil Small molecular drug DB08954
Ketobemidone Small molecular drug DB06738
L-aspartic Acid Small molecular drug D0OT9B
N,N'-bis-(4-butoxy-phenyl)-guanidine Small molecular drug D0E9KB
N,N'-bis-(4-butyl-phenyl)-guanidine Small molecular drug D0S3TY
N,N'-bis-(4-ethyl-phenyl)-guanidine Small molecular drug D04JJL
N,N'-bis-(4-hexyl-phenyl)-guanidine Small molecular drug D0ZD4F
N,N'-bis-(4-isopropyl-phenyl)-guanidine Small molecular drug D06RFW
N,N'-bis-(4-sec-butyl-phenyl)-guanidine Small molecular drug D0U8BM
N-(2-methoxybenzyl)Cinnamamidine Small molecular drug D0K7EZ
Nle-pro-glu Small molecular drug D03LWV
Phe-pro-glu Small molecular drug D05RRK
Phencyclidine Small molecular drug D0Q5PC
Phenethyl-(3-phenyl-propyl)-amine Small molecular drug D0T1GZ
Phenethyl-(4-phenyl-butyl)-amine Small molecular drug D0J1AE
Rpr-118723 Small molecular drug D03PGF
Transtorine Small molecular drug D01SHB
[3h]Cgp39653 Small molecular drug D08UDC
[3h]Cgs19755 Small molecular drug D0KO6Y
[3h]Cpp Small molecular drug D00ZKW
[3h]Dizocilpine Small molecular drug D0D2ZH
[3h]Mdl105519 Small molecular drug D07COG
4-benzyl-1-phenethyl-piperidine Hydrochloride . D0QV0K
4-chloro-3-hydroxy-1h-quinolin-2-one . D0H5JV
5,7-dichloro-3-hydroxy-1h-quinazoline-2,4-dione . D0FU0K
Discontinued
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Am-92016 Small molecular drug D03KGJ
Dizocilpine Small molecular drug D02KLW
L-687414 Small molecular drug D0UB6U
L-689560 Small molecular drug D03UNN
L-695902 Small molecular drug D03WYF
L-698532 Small molecular drug D03CNT
L-698544 Small molecular drug D0AZ5V
L-701324 Small molecular drug D0M1WN
Mdl-105519 Small molecular drug D0X5PX
Rpr-104632 Small molecular drug D01PWK
Spermine Small molecular drug D0LD9S
Ym-90k Small molecular drug D02TTF

References

1 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.