DGIdb - GRIA2 Gene Record

GRIA2 2891 Druggable Genome

Alternate Names:

2891
GLUTAMATE IONOTROPIC RECEPTOR AMPA TYPE SUBUNIT 2
GRIA2
GLUR2
GLURB
GluA2
GluR-K2
HBGR2
138247
4572
ENSG00000120251
OTTHUMG00000133836
P42262
GluR-B
Glutamate receptor 2
AMPA-selective glutamate receptor 2
GluR-2
Glutamate receptor ionotropic, AMPA 2
GLUTAMATE RECEPTOR 2 PRECURSOR (GLUR-2) (GLUR-B) (GLUR-K2) (GLUTAMATE RECEPTOR IONOTROPIC, AMPA 2). [SOURCE:UNIPROT/SWISSPROT;ACC:P42262]
GRIA2_HUMAN
Glutamate receptor AMPA 2
T42392
NEDLIB

Gene Info:

Human Readable Name	DRUGGABLE GENOME
Target Subclass	Glutamate
Target Subclass	Ligand_gated_ion_channels
Transmembrane Helix Count	3
Target Subclass	Channels
Target Main Class	Receptors
Target Class	Receptors
Target Subclass	TC:1.A.10.1.13
Interpro Short Name	Iontro_glu_rcpt
Interpro Name	Ionotropic glutamate receptor
Interpro Acc	IPR001320
Interpro Type	Domain
Uniprot Status	Swiss-Prot
Uniprot Evidence	1: Evidence at protein level
Gene Biotype	PROTEIN_CODING

(7 More Sources)

Gene Categories: Category Details

ION CHANNEL
EXTERNAL SIDE OF PLASMA MEMBRANE
DRUGGABLE GENOME

Publications:

Yamakura et al., 2001, Anesthetics and ion channels: molecular models and sites of action., Annu. Rev. Pharmacol. Toxicol.
Krasowski et al., 1999, General anaesthetic actions on ligand-gated ion channels., Cell. Mol. Life Sci.
Jin et al., 2010, The interaction of the neuroprotective compounds riluzole and phenobarbital with AMPA-type glutamate receptors: a patch-clamp study., Pharmacology
Denes et al., 2006, Talampanel a non-competitive AMPA-antagonist attenuates caspase-3 dependent apoptosis in mouse brain after transient focal cerebral ischemia., Brain Res. Bull.
Howes et al., 2007, Talampanel., Neurotherapeutics
Langan et al., 2003, Talampanel, a new antiepileptic drug: single- and multiple-dose pharmacokinetics and initial 1-week experience in patients with chronic intractable epilepsy., Epilepsia
Henley et al., 1993, Localisation of glutamate receptor binding sites and mRNAs to the dorsal horn of the rat spinal cord., Neuropharmacology
Li et al., 1995, Functional effects of mutations in the putative agonist binding region of recombinant alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors., Mol. Pharmacol.
Stein et al., 1992, Complex pharmacological properties of recombinant alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate receptor subtypes., Mol. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Cheng Q et al., 2005, Evolution of glutamate interactions during binding to a glutamate receptor., Nat Chem Biol

GLUTAMIC ACID GRIA2

Interaction Score: 7.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7679210 7838123 1279377 17016423 17139284 16408071

Sources:
DTC
PALIRODEN GRIA2

Interaction Score: 2.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
TALAMPANEL GRIA2

Interaction Score: 2.21

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name talampanel

Novel drug target Established target

PMIDs:
16861112 17199027 12581229

Sources:
TdgClinicalTrial
PERAMPANEL GRIA2

Interaction Score: 1.66

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

Direct Interaction yes

Trial Name E2007

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
SECOBARBITAL GRIA2

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
BUTABARBITAL GRIA2

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
HEXOBARBITAL GRIA2

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
BUTETHAL GRIA2

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
THIOPENTAL GRIA2

Interaction Score: 0.8

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
MEPHOBARBITAL GRIA2

Interaction Score: 0.74

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
MIBAMPATOR GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZONAMPANEL GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CX1739 GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MK-8777 GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PF-04958242 GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
FARAMPATOR GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions
SELURAMPANEL GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name BGG-492

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
BECAMPANEL GRIA2

Interaction Score: 0.55

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
ChemblInteractions
TEZAMPANEL GRIA2

Interaction Score: 0.49

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name tezampanel, NGX424,NGX426

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions
DASOLAMPANEL GRIA2

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PENTOBARBITAL GRIA2

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
METHARBITAL GRIA2

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
TALBUTAL GRIA2

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
BUTALBITAL GRIA2

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
PHENOBARBITAL GRIA2

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
20051697 11264449 10487207

Sources:
TdgClinicalTrial TEND
PRIMIDONE GRIA2

Interaction Score: 0.28

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND
IRAMPANEL GRIA2

Interaction Score: 0.16

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
ChemblInteractions
TOPIRAMATE GRIA2

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Ensembl: ENSG00000120251
- Version: 101_38
Alternate Names:

GRIA2 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TEND: P42262
- Version: 01-August-2011
Alternate Names:

GRIA2_HUMAN Uniprot Id

GRIA2 Gene Symbol

2891 Entrez Gene Id

Gene Info:

Target Subclass Glutamate

Target Subclass Ligand_gated_ion_channels

Transmembrane Helix Count 3

Publications:
TdgClinicalTrial: P42262
- Version: January-2014
Alternate Names:

GRIA2 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass TC:1.A.10.1.13

Publications:

RussLampel: ENSG00000120251

Version: 26-July-2011

Alternate Names:

GRIA2 Display Id

ENSG00000120251 Ensembl Gene Id

GLUTAMATE RECEPTOR 2 PRECURSOR (GLUR-2) (GLUR-B) (GLUR-K2) (GLUTAMATE RECEPTOR IONOTROPIC, AMPA 2). [SOURCE:UNIPROT/SWISSPROT;ACC:P42262] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:

HopkinsGroom: P42262
- Version: 11-September-2012
Alternate Names:

2891 Entrez Gene Id

GLUTAMATE RECEPTOR 2 Uniprot Protein Name

GRIA2 Uniprot Gene Name

Gene Info:

Human Readable Name DRUGGABLE GENOME

Interpro Short Name Iontro_glu_rcpt

Interpro Name Ionotropic glutamate receptor

Gene Categories:

DRUGGABLE GENOME

Publications:
DTC: GRIA2
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Cheng Q et al., 2005, Evolution of glutamate interactions during binding to a glutamate receptor., Nat Chem Biol
ChemblInteractions: GLUR2
- Version: chembl_23
Alternate Names:

GLUR2 GENE_SYMBOL

GRIA2 GENE_SYMBOL

Glutamate receptor 2 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000120251
- Version: 31-May-2017
Alternate Names:

ENSG00000120251 Gene Symbol

GRIA2 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
GO: GRIA2
- Version: 01-February-2022
Alternate Names:

GLUR2 GO Gene Synonym

Gene Info:

Gene Categories:

EXTERNAL SIDE OF PLASMA MEMBRANE

Publications:
TTD: Glutamate receptor AMPA 2
- Version: 2020.06.01
Alternate Names:

GRIA2 TTD Gene Abbreviation

T42392 TTD Target ID

Gene Info:

Publications:
Pharos: GRIA2
- Version: 01-February-2022
Alternate Names:

Glutamate receptor 2 Gene Name

P42262 UniProt ID

Gene Info:

Gene Categories:

ION CHANNEL

Publications:

Mechanism of Interaction	Glutamate receptor ionotropic AMPA antagonist
Direct Interaction	yes
Trial Name	E2007

Mechanism of Interaction	Glutamate receptor ionotropic AMPA positive allosteric modulator
Direct Interaction	yes

Novel drug target	Established target
Trial Name	BGG-492
Mechanism of Interaction	Glutamate receptor ionotropic AMPA antagonist

Trial Name	tezampanel, NGX424,NGX426
Novel drug target	Established target
Direct Interaction	yes

GRIA2	Display Id
ENSG00000120251	Ensembl Gene Id
GLUTAMATE RECEPTOR 2 PRECURSOR (GLUR-2) (GLUR-B) (GLUR-K2) (GLUTAMATE RECEPTOR IONOTROPIC, AMPA 2). [SOURCE:UNIPROT/SWISSPROT;ACC:P42262]	Description

2891	Entrez Gene Id
GLUTAMATE RECEPTOR 2	Uniprot Protein Name
GRIA2	Uniprot Gene Name

GRIA2 Gene Record

GRIA2 2891 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7679210 7838123 1279377 17016423 17139284 16408071

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info: Trial Name talampanel Novel drug target Established target

PMIDs: 16861112 17199027 12581229

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist Direct Interaction yes Trial Name E2007

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11264449 10487207

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name BGG-492 Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name tezampanel, NGX424,NGX426 Novel drug target Established target Direct Interaction yes

Interaction Types & Directionality:

n/a

PMIDs:
7679210 7838123 1279377 17016423 17139284 16408071

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name talampanel

Novel drug target Established target

PMIDs:
16861112 17199027 12581229

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

Direct Interaction yes

Trial Name E2007

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11264449 10487207

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name BGG-492

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name tezampanel, NGX424,NGX426

Novel drug target Established target

Direct Interaction yes

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Glutamate receptor ionotropic AMPA antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target