Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T08910 | Target Info | |||
Target Name | GABA(A) receptor gamma-2 (GABRG2) | ||||
Synonyms |
Gamma-aminobutyric acid receptor subunit gamma-2; GABA(A) receptor subunit gamma-2
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Target Type | Successful Target | ||||
Gene Name | GABRG2 | ||||
Biochemical Class | Neurotransmitter receptor | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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 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 | [4] |
References | Top | ||||
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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 | 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. |
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