Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T26368 Target Info
Target Name GABA(A) receptor alpha-5 (GABRA5)
Synonyms
GABRA5; GABAA alpha 5; GABA-A alpha-5
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Target Type Successful Target
Gene Name GABRA5
Biochemical Class Ligand-gated ion channel
UniProt ID
GBRA5_HUMAN
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 Click to Show More [1]
2 Basmisanil Drug Info Ki = 985 nM [3]
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(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) Basmisanil Drug Info Ki = 489 nM [3]
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) Basmisanil Drug Info Ki = 502 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-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 [6]
2 Flumazenil Drug Info Ki = 0.8 nM [6]
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) Flumazenil Drug Info Ki = 0.9 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) Flumazenil Drug Info Ki = 1.05 nM [6]
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-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) Flumazenil Drug Info Ki = 5.7 nM Click to Show More [1]
2 GSK683699 Drug Info EC50 = 650 nM [9]
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 [5]
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 [6]
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 [8]
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 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 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 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 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 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 9 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.

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