Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T38200 Target Info
Target Name GABA transporter-3 (SLC6A11)
Synonyms
Solute carrier family 6 member 11; Sodium- and chloride-dependent GABA transporter 3; GAT3; GAT-3; GABT3
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Target Type Clinical trial Target
Gene Name SLC6A11
UniProt ID
S6A11_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 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 [2]
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 [3]
Co-Target Name GABA-A receptor anion channel Co-Target
UniProt ID GBRE_HUMAN; GBRP_HUMAN
Gene Name GABRE; GABRP
Representative Drug(s) GSK683699 Drug Info IC50 = 25 nM [4]
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 [5]
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) GSK683699 Drug Info EC50 = 650 nM [6]
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 [2]
Co-Target Name GABA-A receptor; agonist GABA site Co-Target
UniProt ID GBRA1_HUMAN; GBRA2_HUMAN; GBRA3_HUMAN; GBRA4_HUMAN; GBRA5_HUMAN; GBRA6_HUMAN; GBRB1_HUMAN; GBRB2_HUMAN; GBRB3_HUMAN
Gene Name NO-GeName
Representative Drug(s) GSK683699 Drug Info EC50 = 990 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 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 3 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 4 Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists. J Med Chem. 1992 Oct 30;35(22):4092-7.
REF 5 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 6 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 7 p-(4-Azipentyl)propofol: a potent photoreactive general anesthetic derivative of propofol. J Med Chem. 2011 Dec 8;54(23):8124-35.

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