Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T28722 | Target Info | |||
| Target Name | GABA(A) receptor gamma-3 (GABRG3) | ||||
| Synonyms |
GABRG3
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| Target Type | Successful Target | ||||
| Gene Name | GABRG3 | ||||
| Biochemical Class | Ligand-gated ion channel | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Steroid 11-beta-hydroxylase (CYP11B1) | Successful Target | ||||
| UniProt ID | C11B1_HUMAN | |||||
| Gene Name | CYP11B1 | |||||
| Synonyms |
S11BH; P450C11; P-450c11; CYPXIB1; CYP11B1
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| Representative Drug(s) | Etomidate | Drug Info | IC50 = 0.5 nM | [1] | ||
| Co-Target Name | GABA(A) receptor alpha-5 (GABRA5) | Successful Target | ||||
| UniProt ID | GBRA5_HUMAN | |||||
| Gene Name | GABRA5 | |||||
| Synonyms |
GABRA5; GABAA alpha 5; GABA-A alpha-5
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| Representative Drug(s) | SARIPIDEM | Drug Info | IC50 = 2.7 nM | [2] | ||
| 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 | [3] | |
| 2 | Zolpidem | Drug Info | IC50 = 14 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) | Zolpidem | Drug Info | Ki = 400 nM | [4] | ||
| 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) | Zolpidem | Drug Info | EC50 = 737 nM | [5] | ||
| Co-Target Name | Aldosterone synthase (CYP11B2) | Clinical trial Target | ||||
| UniProt ID | C11B2_HUMAN | |||||
| Gene Name | CYP11B2 | |||||
| Synonyms |
Steroid 18hydroxylase; Cytochrome P450C18; Cytochrome P450Aldo; Cytochrome P450 11B2, mitochondrial; CYPXIB2; CYP11B2; Aldosteronesynthesizing enzyme; ALDOS
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| Representative Drug(s) | Etomidate | Drug Info | IC50 = 0.1 nM | [6] | ||
| 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 | [7] | ||
| 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 | [7] | |
| 2 | Flumazenil | Drug Info | Ki = 0.8 nM | [7] | ||
| 3 | SARIPIDEM | Drug Info | IC50 = 1.1 nM | [2] | ||
| 4 | SARIPIDEM | Drug Info | IC50 = 1.1 nM | [2] | ||
| 5 | Zolpidem | Drug Info | Ki = 26.7 nM | [8] | ||
| 6 | Zolpidem | Drug Info | Ki = 26.7 nM | [8] | ||
| 7 | Zolpidem | Drug Info | IC50 = 46.3 nM | [2] | ||
| 8 | Zolpidem | Drug Info | IC50 = 46.3 nM | [2] | ||
| 9 | Allopregnanolone | Drug Info | EC50 = 160 nM | [12] | ||
| 10 | Allopregnanolone | Drug Info | EC50 = 160 nM | [12] | ||
| 11 | Drug Info | EC50 = 260 nM | [12] | |||
| 12 | Drug Info | EC50 = 260 nM | [12] | |||
| 13 | Zuranolone | Drug Info | EC50 = 374 nM | [13] | ||
| 14 | Zuranolone | Drug Info | EC50 = 374 nM | [13] | ||
| 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 | Click to Show More | [8] | |
| 2 | Zolpidem | Drug Info | Ki = 103 nM | [11] | ||
| 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 | Click to Show More | [7] | |
| 2 | Zolpidem | Drug Info | Ki = 246 nM | [11] | ||
| 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 | [3] | ||
| 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 | [3] | |
| 2 | Zolpidem | Drug Info | EC50 = 180 nM | [14] | ||
| 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 | [3] | |
| 2 | Zolpidem | Drug Info | Ki = 975 nM | [3] | ||
| Co-Target Name | GABA A receptor alpha-1/beta-1/gamma-2 (GABRA1/GABRB1/GABRG2) | Co-Target | ||||
| UniProt ID | GBRA1_HUMAN-GBRB1_HUMAN-GBRG2_HUMAN | |||||
| Gene Name | GABRA1-GABRB1-GABRG2 | |||||
| Representative Drug(s) | Zolpidem | Drug Info | Ki = 53 nM | [9] | ||
| 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 | Click to Show More | [10] | |
| 2 | Zuranolone | Drug Info | EC50 = 299 nM | [10] | ||
| 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 | [7] | ||
| Co-Target Name | GABA-A receptor alpha-4/beta-2/delta (GABRA4/GABRB2/GABRD) | Co-Target | ||||
| UniProt ID | GBRA4_HUMAN-GBRB2_HUMAN-GBRD_HUMAN | |||||
| Gene Name | GABRA4-GABRB2-GABRD | |||||
| Representative Drug(s) | Zuranolone | Drug Info | EC50 = 163 nM | [13] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases. J Med Chem. 2014 Jun 26;57(12):5011-22. | ||||
| REF 2 | A conformational study of ligands for omega modulatory sites of GABAa receptors by NOESY NMR spectroscopy and distance geometry. Bioorg Med Chem Lett. 1997 Sep 9;7(17):2277-82. | ||||
| REF 3 | 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 4 | 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 5 | Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor. J Med Chem. 2002 Nov 7;45(23):5043-51. | ||||
| REF 6 | Optimization of the First Selective Steroid-11beta-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases. ACS Med Chem Lett. 2011 Jun 3;2(8):559-64. | ||||
| REF 7 | 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 8 | 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 9 | 4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore mod... J Med Chem. 2006 Apr 20;49(8):2526-33. | ||||
| REF 10 | 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 11 | Discovery of functionally selective 7,8,9,10-tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABA A receptor agonists at the alpha3 subunit. J Med Chem. 2005 Mar 10;48(5):1367-83. | ||||
| REF 12 | Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor. J Med Chem. 1997 Jan 3;40(1):61-72. | ||||
| REF 13 | Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3207-3218. | ||||
| REF 14 | Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new se... J Med Chem. 1997 Sep 12;40(19):3109-18. | ||||
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