Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T62184 | Target Info | |||
| Target Name | GABA transporter GAT-1 (SLC6A1) | ||||
| Synonyms |
Solute carrier family 6 member 1; Sodium- and chloride-dependent GABA transporter 1; GAT1; GAT-1; GABT1; GABATR; GABA transporter 1
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| Target Type | Successful Target | ||||
| Gene Name | SLC6A1 | ||||
| Biochemical Class | Neurotransmitter:sodium symporter | ||||
| UniProt ID | |||||
| 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 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 | [2] | ||
| 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 | [3] | ||
| 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 | [2] | ||
| 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 | [3] | ||
| 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 | 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 3 | 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 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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