Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T75440 Target Info
Target Name Translocator protein (TSPO)
Synonyms
Peripheral-type benzodiazepine receptor; Peripheral benzodiazepine receptor; PKBS; PBR; Mitochondrial benzodiazepine receptor; MBR; BZRP
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Target Type Successful Target
Gene Name TSPO
Biochemical Class Cholesterol/porphyrin uptake translocator
UniProt ID
TSPO_HUMAN
Co-Targets of This Target  Top
Co-Target Name Matrix metalloproteinase-2 (MMP-2) Successful Target
UniProt ID MMP2_HUMAN
Gene Name MMP2
Synonyms
TBE-1; Matrix metalloproteinase 2; CLG4A; 72 kDa type IV collagenase; 72 kDa gelatinase
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Representative Drug(s) TLN-4601 Drug Info IC50 = 0.46 ug.mL-1 [1]
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 [2]
2 Diazepam Drug Info Ki = 16 nM [4]
3 Alprazolam Drug Info EC50 = 37 nM [3]
4 Eszopiclone Drug Info Ki = 50.1 nM [2]
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) Alprazolam Drug Info EC50 = 10 nM Click to Show More [3]
2 Diazepam Drug Info Ki = 15 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) Alprazolam Drug Info EC50 = 12 nM Click to Show More [3]
2 Diazepam Drug Info Ki = 17 nM [4]
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) Diazepam Drug Info Ki = 17 nM Click to Show More [4]
2 Alprazolam Drug Info EC50 = 69 nM [3]
Co-Target Name Matrix metalloproteinase-9 (MMP-9) Clinical trial Target
UniProt ID MMP9_HUMAN
Gene Name MMP9
Synonyms
Matrix metalloproteinase 9; GELB; CLG4B; 92 kDa type IV collagenase; 92 kDa gelatinase
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Representative Drug(s) TLN-4601 Drug Info IC50 = 0.6 ug.mL-1 [1]
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) Drug Info Ki = 0.59 nM Click to Show More [5]
2 Flumazenil Drug Info Ki = 0.9 nM [5]
3 Drug Info Ki = 1.1 nM [8]
4 Diazepam Drug Info Ki = 6.6 nM [8]
5 Chlordiazepoxide Drug Info Ki = 392 nM [17]
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 Click to Show More [6]
2 Drug Info Ki = 1.54 nM [5]
3 Drug Info Ki = 2.1 nM [5]
4 Diazepam Drug Info Ki = 11 nM [13]
5 Chlordiazepoxide Drug Info Ki = 320 nM [16]
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 Drug Info Ki = 0.8 nM [5]
3 Flumazenil Drug Info Ki = 0.8 nM [6]
4 Drug Info Ki = 0.8 nM [5]
5 Drug Info EC50 = 1.4 nM [9]
6 Drug Info EC50 = 1.4 nM [9]
7 Drug Info Ki = 2.2 nM [10]
8 Drug Info Ki = 2.2 nM [10]
9 Diazepam Drug Info Ki = 12 nM [8]
10 Diazepam Drug Info Ki = 12 nM [8]
11 Diazepam Drug Info Ki = 13 nM [15]
12 Diazepam Drug Info Ki = 13 nM [15]
13 Chlordiazepoxide Drug Info Ki = 560 nM [16]
14 Chlordiazepoxide Drug Info Ki = 560 nM [16]
Co-Target Name GABA-A receptor anion channel Co-Target
UniProt ID GBRE_HUMAN; GBRP_HUMAN
Gene Name GABRE; GABRP
Representative Drug(s) Flumazenil Drug Info Ki = 0.9 nM Click to Show More [7]
2 Diazepam Drug Info IC50 = 8.1 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 [6]
2 Drug Info Ki = 1.43 nM [5]
3 Drug Info Ki = 4.5 nM [5]
4 Diazepam Drug Info Ki = 15 nM [5]
5 Chlordiazepoxide Drug Info Ki = 275 nM [16]
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 Click to Show More [2]
2 Eszopiclone Drug Info Ki = 102 nM [2]
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 [2]
2 Eszopiclone Drug Info Ki = 114 nM [2]
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 [2]
2 Diazepam Drug Info Ki = 10 nM [12]
3 Eszopiclone Drug Info Ki = 162 nM [2]
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) Diazepam Drug Info Ki = 12 nM [14]
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]
References  Top
REF 1 Anti-invasive and anti-angiogenic activities of naturally occurring dibenzodiazepine BU-4664L and its derivatives. Bioorg Med Chem Lett. 2010 Feb 1;20(3):963-5.
REF 2 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 3 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 4 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 5 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 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 High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives. J Med Chem. 2005 Apr 21;48(8):2936-43.
REF 8 N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit. Bioorg Med Chem Lett. 2000 Jun 19;10(12):1381-4.
REF 9 Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2... J Biol Chem. 2007 Nov 9;282(45):33052-63.
REF 10 Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
REF 11 Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones. J Med Chem. 1982 Sep;25(9):1050-5.
REF 12 High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex. J Med Chem. 1996 Jan 5;39(1):158-75.
REF 13 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 14 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 15 Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety. J Med Chem. 2006 Feb 23;49(4):1235-8.
REF 16 3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels. J Med Chem. 2002 Apr 25;45(9):1887-900.
REF 17 3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors. Bioorg Med Chem Lett. 2004 Jun 7;14(11):2871-5.

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