Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T54128 Target Info
Target Name Glutamate receptor AMPA (GRIA)
Synonyms
Glutamate receptor ionotropic, AMPA; Glutamate receptor; AMPA selective glutamate receptor; AMPA receptor
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Target Type Successful Target
Gene Name NO-GeName
Biochemical Class Chloride channel
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name GABA(A) receptor alpha-2 (GABRA2) Successful Target
UniProt ID GBRA2_HUMAN
Gene Name GABRA2
Synonyms
GABRA2; GABA-A receptor alpha 2; GABA(A)Gamma-aminobutyric-acid receptor alpha-2 subunit precursor receptor
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Representative Drug(s) AZD7325 Drug Info Ki = 0.3 nM [1]
Co-Target Name GABA(A) receptor alpha-1 (GABRA1) Successful Target
UniProt ID GBRA1_HUMAN
Gene Name GABRA1
Synonyms
Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1
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Representative Drug(s) AZD7325 Drug Info Ki = 0.5 nM [1]
Co-Target Name GABA(A) receptor alpha-3 (GABRA3) Successful Target
UniProt ID GBRA3_HUMAN
Gene Name GABRA3
Synonyms
Gamma-aminobutyric acid receptor subunit alpha-3; GABA-A receptor alpha 3; GABA(A)Gamma-aminobutyric-acid receptor alpha-3 subunit precursor receptor; GABA(A) receptor subunit alpha-3
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Representative Drug(s) AZD7325 Drug Info Ki = 1.3 nM [1]
Co-Target Name GABA(A) receptor alpha-5 (GABRA5) Successful Target
UniProt ID GBRA5_HUMAN
Gene Name GABRA5
Synonyms
GABRA5; GABAA alpha 5; GABA-A alpha-5
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Representative Drug(s) AZD7325 Drug Info Ki = 230 nM [1]
Co-Target Name GABA(A) receptor rho1 (GABRR1) Literature-reported Target
UniProt ID GBRR1_HUMAN
Gene Name GABRR1
Synonyms
Gamma-aminobutyric acid receptor subunit rho-1; GABA(C) receptor1; GABA(A) receptor subunit rho-1
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Representative Drug(s) Lindane Drug Info IC50 = 91 nM Click to Show More [2]
2 Drug Info EC50 = 691.83 nM [3]
Co-Target Name GABA A receptor alpha-2/beta-3/gamma-2 (GABRA2/GABRB3/GABRG2) Co-Target
UniProt ID GBRA2_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA2-GABRB3-GABRG2
Representative Drug(s) AZD7325 Drug Info Ki = 0.309 nM [4]
Co-Target Name GABA receptor beta-3 (GABRB3) Co-Target
UniProt ID GBRB3_HUMAN
Gene Name GABRB3
Synonyms
Gamma-aminobutyric acid receptor subunit beta-3; GABA(A) receptor subunit beta-3
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Representative Drug(s) Lindane Drug Info IC50 = 0.9 nM [2]
Co-Target Name GABA-A receptor alpha-6/beta-3 (GABRA6/GABRB3) Co-Target
UniProt ID GBRB3_HUMAN-GBRA6_HUMAN
Gene Name GABRB3-GABRA6
Representative Drug(s) Lindane Drug Info IC50 = 1.3 nM [2]
Co-Target Name GABA-A receptor anion channel Co-Target
UniProt ID GBRE_HUMAN; GBRP_HUMAN
Gene Name GABRE; GABRP
Representative Drug(s) Drug Info IC50 = 2 nM Click to Show More [5]
2 Artemisinin SP Drug Info Ki = 54.95 nM [3]
Co-Target Name GABA A receptor alpha-6/beta-3/gamma-2 (GABRA6/GABRB3/GABRG2) Co-Target
UniProt ID GBRA6_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA6-GABRB3-GABRG2
Representative Drug(s) Lindane Drug Info IC50 = 4.9 nM [2]
Co-Target Name GABA-A receptor alpha-1/beta-3 (GABRA1/GABRB3) Co-Target
UniProt ID GBRA1_HUMAN-GBRB3_HUMAN
Gene Name GABRA1-GABRB3
Representative Drug(s) Lindane Drug Info IC50 = 12 nM [2]
Co-Target Name GABA A receptor alpha-1/beta-2/gamma-2 (GABRA1/GABRB2/GABRG2) Co-Target
UniProt ID GBRA1_HUMAN-GBRB2_HUMAN-GBRG2_HUMAN
Gene Name GABRA1-GABRB2-GABRG2
Representative Drug(s) Lindane Drug Info IC50 = 21 nM Click to Show More [2]
2 Lindane Drug Info IC50 = 21 nM [2]
3 Drug Info EC50 = 537.03 nM [3]
4 Drug Info EC50 = 537.03 nM [3]
Co-Target Name GABA-A receptor alpha-1/beta-1 (GABRA1/GABRB1) Co-Target
UniProt ID GBRA1_HUMAN-GBRB1_HUMAN
Gene Name GABRA1-GABRB1
Representative Drug(s) Lindane Drug Info IC50 = 112 nM [2]
Co-Target Name GABA A receptor alpha-3/beta-2/gamma-2 (GABRA3/GABRB2/GABRG2) Co-Target
UniProt ID GBRA3_HUMAN-GBRB2_HUMAN-GBRG2_HUMAN
Gene Name GABRA3-GABRB2-GABRG2
Representative Drug(s) Drug Info EC50 = 210 nM [3]
Co-Target Name GABA A receptor alpha-2/beta-2/gamma-2 (GABRA2/GABRB2/GABRG2) Co-Target
UniProt ID GBRA2_HUMAN-GBRB2_HUMAN-GBRG2_HUMAN
Gene Name GABRA2-GABRB2-GABRG2
Representative Drug(s) Drug Info EC50 = 407.38 nM [3]
References  Top
REF 1 Subtype Selective gamma-Aminobutyric Acid Type A Receptor (GABA A R) Modulators Acting at the Benzodiazepine Binding Site: An Update. J Med Chem. 2020 Apr 9;63(7):3425-3446.
REF 2 Insecticide interactions with gamma-aminobutyric acid and nicotinic receptors: predictive aspects of structural models. 2008;33(1):4-8.
REF 3 Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists. Eur J Med Chem. 2014 Sep 12;84:404-16.
REF 4 Development and SAR of functionally selective allosteric modulators of GABAA receptors. Bioorg Med Chem. 2011 May 1;19(9):2927-38.
REF 5 Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists. J Med Chem. 1992 Oct 30;35(22):4092-7.

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