Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T51487 Target Info
Target Name GABA(A) receptor alpha-1 (GABRA1)
Synonyms
Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1
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Target Type Successful Target
Gene Name GABRA1
Biochemical Class Ligand-gated ion channel
UniProt ID
GBRA1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Gamma-aminobutyric acid B receptor (GABBR) Successful Target
UniProt ID GABR1_HUMAN; GABR2_HUMAN
Gene Name GABBR1; GABBR2
Synonyms
Gamma-aminobutyric acid type B receptor; GPRC3; GABABR; GABA-BR; GABA-B-R; GABA-B receptor
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Representative Drug(s) GSK683699 Drug Info IC50 = 25 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) Zolpidem Drug Info Ki = 400 nM [2]
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) Zolpidem Drug Info EC50 = 737 nM [3]
Co-Target Name GABA transporter-3 (SLC6A11) Clinical trial Target
UniProt ID S6A11_HUMAN
Gene Name SLC6A11
Synonyms
Solute carrier family 6 member 11; Sodium- and chloride-dependent GABA transporter 3; GAT3; GAT-3; GABT3
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Representative Drug(s) GSK683699 Drug Info IC50 = 1000 nM [4]
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) GSK683699 Drug Info EC50 = 269.15 nM [5]
Co-Target Name Na(+)/Cl(-) betaine/GABA transporter (SLC6A12) Literature-reported Target
UniProt ID S6A12_HUMAN
Gene Name SLC6A12
Synonyms
Solute carrier family 6 member 12; Sodium- and chloride-dependent betaine transporter; BGT-1
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Representative Drug(s) GSK683699 Drug Info IC50 = 851.14 nM [4]
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) ZK-93423 Drug Info Ki = 4.2 nM Click to Show More [6]
2 Zolpidem Drug Info Ki = 103 nM [9]
Co-Target Name GABA A receptor alpha-5/beta-3/gamma-2 (GABRA5/GABRB3/GABRG2) Co-Target
UniProt ID GBRA5_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA5-GABRB3-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki = 4.5 nM [7]
Co-Target Name GABA A receptor alpha-3/beta-3/gamma-2 (GABRA3/GABRB3/GABRG2) Co-Target
UniProt ID GBRA3_HUMAN-GBRB3_HUMAN-GBRG2_HUMAN
Gene Name GABRA3-GABRB3-GABRG2
Representative Drug(s) ZK-93423 Drug Info Ki = 6 nM Click to Show More [6]
2 Zolpidem Drug Info Ki = 246 nM [9]
3 Zaleplon Drug Info EC50 ~ 1000 nM [14]
Co-Target Name GABA-A receptor alpha-4/beta-3/delta (GABRA4/GABRB3/GABRD) Co-Target
UniProt ID GBRA4_HUMAN-GBRB3_HUMAN-GBRD_HUMAN
Gene Name GABRA4-GABRB3-GABRD
Representative Drug(s) Allopregnanolone Drug Info EC50 = 75.5 nM [8]
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) Zolpidem Drug Info EC50 = 180 nM Click to Show More [10]
2 GSK683699 Drug Info EC50 = 650 nM [12]
Co-Target Name GABA A receptor alpha-5/beta-2/gamma-2 (GABRA5/GABRB2/GABRD2) Co-Target
UniProt ID GBRA5_HUMAN-GBRB2_HUMAN-GBRG2_HUMAN
Gene Name GABRA5-GABRB2-GABRG2
Representative Drug(s) GSK683699 Drug Info EC50 = 230 nM [11]
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) GSK683699 Drug Info EC50 = 912.01 nM Click to Show More [5]
2 Zolpidem Drug Info Ki = 975 nM [13]
Co-Target Name GABA A receptor alpha-5/beta-3/gamma-3 (GABRA5/GABRB3/GABRD3) Co-Target
UniProt ID GBRA5_HUMAN-GBRB3_HUMAN-GBRG3_HUMAN
Gene Name GABRA5-GABRB3-GABRG3
Representative Drug(s) Zaleplon Drug Info EC50 ~ 1000 nM [14]
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) ZK-93423 Drug Info Ki ~ 1000 nM [7]
References  Top
REF 1 Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.
REF 2 Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases. Eur J Med Chem. 2019 Nov 1;181:111569.
REF 3 Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor. J Med Chem. 2002 Nov 7;45(23):5043-51.
REF 4 Structure-Activity Relationship, Pharmacological Characterization, and Molecular Modeling of Noncompetitive Inhibitors of the Betaine/-Aminobutyric Acid Transporter 1 (BGT1). J Med Chem. 2017 Nov 9;60(21):8834-8846.
REF 5 Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as -aminobutyric acid(a) receptor agonists. J Med Chem. 2013 Feb 14;56(3):993-1006.
REF 6 Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
REF 7 Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. J Med Chem. 2000 Jan 13;43(1):71-95.
REF 8 Neuroactive Steroids. 2. 3alpha-Hydroxy-3beta-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5beta-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (gamma-Aminobutyric Acid)?A?Receptor. J Med Chem. 2017 Sep 28;60(18):7810-7819.
REF 9 Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. J Med Chem. 2005 Mar 10;48(5):1367-83.
REF 10 Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new se... J Med Chem. 1997 Sep 12;40(19):3109-18.
REF 11 Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at gamma-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters. J Med Chem. 2019 Jun 27;62(12):5797-5809.
REF 12 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 13 Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different. J Med Chem. 2008 Nov 27;51(22):7243-52.
REF 14 Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem. 2013 Feb 14;56(3):593-624.

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