Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T64382 | Target Info | |||
| Target Name | Gamma-aminobutyric acid receptor (GAR) | ||||
| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Translocator protein (TSPO) | Successful Target | ||||
| UniProt ID | TSPO_HUMAN | |||||
| Gene Name | TSPO | |||||
| Synonyms |
Peripheral-type benzodiazepine receptor; Peripheral benzodiazepine receptor; PKBS; PBR; Mitochondrial benzodiazepine receptor; MBR; BZRP
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| Representative Drug(s) | Alpidem | Drug Info | Ki = 0.5 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 | 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-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) | ZK-93423 | Drug Info | Ki = 4.5 nM | [3] | ||
| 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] | ||
| 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-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) | ZK-93423 | Drug Info | Ki ~ 1000 nM | [3] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases. Eur J Med Chem. 2019 Nov 1;181:111569. | ||||
| 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 | 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 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. | ||||
| 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. | ||||
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