Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T51452 | Target Info | |||
| Target Name | GABA(A) receptor alpha-2 (GABRA2) | ||||
| Synonyms |
GABRA2; GABA-A receptor alpha 2; GABA(A)Gamma-aminobutyric-acid receptor alpha-2 subunit precursor receptor
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| Target Type | Successful Target | ||||
| Gene Name | GABRA2 | ||||
| Biochemical Class | Neurotransmitter receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Flumazenil | Drug Info | Ki = 3.3 nM | [1] | ||
| 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 | [2] | ||
| 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 | [3] | ||
| 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 | [4] | ||
| 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 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) | Flumazenil | Drug Info | Ki = 0.6 nM | [5] | ||
| 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) | Flumazenil | Drug Info | Ki = 0.8 nM | Click to Show More | [5] | |
| 2 | Flumazenil | Drug Info | Ki = 0.8 nM | [5] | ||
| 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) | Flumazenil | Drug Info | Ki = 1.05 nM | [5] | ||
| Co-Target Name | GABA receptor alpha-4 (GABRA4) | Co-Target | ||||
| UniProt ID | GBRA4_HUMAN | |||||
| Gene Name | GABRA4 | |||||
| Synonyms |
Gamma-aminobutyric acid receptor subunit alpha-4; GABA(A) receptor subunit alpha-4
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| Representative Drug(s) | Flumazenil | Drug Info | Ki = 2 nM | [1] | ||
| 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) | Flumazenil | Drug Info | Ki = 8.1 nM | Click to Show More | [1] | |
| 2 | GSK683699 | Drug Info | EC50 = 912.01 nM | [4] | ||
| 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) | Flumazenil | Drug Info | Ki = 148 nM | [5] | ||
| 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 | [6] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312. | ||||
| 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 | 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 5 | Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines a... J Med Chem. 1998 Oct 8;41(21):4130-42. | ||||
| REF 6 | 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. | ||||
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