Therapeutic Targets Database
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TTD Target ID: TTDS00428

Target Information
NameGamma-aminobutyric acid receptor subunit gamma-2    
Type of targetSuccessful target    
SynonymsGABA(A) receptor subunit gamma-2    
GABRG2    
DiseaseBrain injury[1][2]
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP18507
SequenceMSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2E,4S)-4-ammoniopent-2-enoate[3]
(4R)-4-ammoniopentanoate[3]
(4S)-4-ammoniopentanoate[3]
(9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine[4]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid[5]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one[6]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one[7]
1- (4-chlorophenyl)-4-phenyl-1H-imidazole[8]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one[6]
2- (1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide[5]
2- (4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one[8]
2- (9-Benzyl-9H-purin-6-ylamino)-ethanol[4]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline[9]
2-Oxa-spiro[4.4]nonan-1-one[6]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline[9]
3,3-Diethyl-dihydro-furan-2-one[6]
3,3-Diisopropyl-dihydro-furan-2-one[6]
3- (benzyloxy)-9H-pyrido[3,4-b]indole[10]
3- (hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole[10]
3- (isopentyloxy)-9H-pyrido[3,4-b]indole[10]
3-Ethoxy-9H-beta-carboline[11]
3-Ethyl-3-isopropyl-dihydro-furan-2-one[6]
3-Ethyl-3-methyl-dihydro-furan-2-one[6]
3-Isopropyl-3-methyl-dihydro-furan-2-one[6]
3-Isothiocyanato-9H-beta-carboline[12]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one[7]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one[7]
3-Methyl-9H-beta-carboline[13]
3-amino-3-demethoxythiocolchicine[14]
3-butoxy-9H-pyrido[3,4-b]indole[10]
3-butoxycarbonyl-4-quinolone[15]
3-butoxycarbonyl-6-ethyl-4-quinolone[15]
3-butylaminocarbonyl-6-ethyl-4-quinolone[15]
3-carboxy-6-ethyl-4-quinolone[15]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone[15]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine[14]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine[14]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine[14]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine[14]
3-demethoxy-3D-glucopyranosylaminothiocolchicine[14]
3-ethoxy-9H-pyrido[3,4-b]indole[10]
3-ethoxycarbonyl-4-quinolone[15]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone[15]
3-ethoxycarbonyl-6-propyl-4-quinolone[15]
3-isobutoxy-9H-pyrido[3,4-b]indole[10]
3-propoxy-9H-pyrido[3,4-b]indole[10]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one[6]
4- (2-aminoethyl)-1,2,5-oxadiazol-3-ol[16]
4- (4-chlorophenyl)-1-pyrid-2-yl-pyrazole[8]
4- (biphenyl-3-yl)-5-[17]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol[18]
4-Methyl-5- (4-piperidyl)isothiazol-3-ol[19]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol[18]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol[18]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol[18]
4-benzyl-5- (4-piperidyl)isothiazol-3-ol[19]
5- (4-piperidyl)-4-propylisothiazol-3-ol[19]
5- (piperidin-4-yl)isothiazol-3-ol[19]
5-Piperidin-4-yl-isoxazol-3-ol[18]
5-[ (1R)-1-ammonioethyl]isoxazol-3-olate[3]
5-[ (1S)-1-ammonioethyl]isoxazol-3-olate[3]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one[6]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one[6]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one[6]
6-Nitro-2- (3-nitro-phenyl)-chromen-4-one[20]
6-Nitro-2- (4-nitro-phenyl)-chromen-4-one[20]
6-benzyl-3-ethoxycarbonyl-4-quinolone[15]
6-benzyl-3-propoxycarbonyl-4-quinolone[15]
6-benzyl-3-propylaminocarbonyl-4-quinolone[15]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone[15]
6-bromo-3-ethoxycarbonyl-4-quinolone[15]
6-ethyl-3- (2-ethylbutoxycarbonyl)-4-quinolone[15]
6-ethyl-3- (2-methylbutoxycarbonyl)-4-quinolone[15]
6-ethyl-3- (3-methylbutoxycarbonyl)-4-quinolone[15]
6-ethyl-3- (3-pentoxycarbonyl)-4-quinolone[15]
6-ethyl-3-i-propoxycarbonyl-4-quinolone[15]
6-ethyl-3-pentoxycarbonyl-4-quinolone[15]
6-ethyl-3-propoxycarbonyl-4-quinolone[15]
6-ethyl-3-propylaminocarbonyl-4-quinolone[15]
9H-beta-Carboline-3-carboxylic acid butyl ester[21]
9H-beta-Carboline-3-carboxylic acid ethyl ester[21]
9H-beta-Carboline-3-carboxylic acid propyl ester[21]
ALLOPREGNANOLONE[22]
AMENTOFLAVONE[23]
BETA-CCM[21]
CGS-13767[24]
CGS-17867A[25]
CGS-8216[24]
CGS-9895[26]
CGS-9896[8]
CI-218872[13]
ELTANOLONE[22]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate[10]
GABAZINE[19]
GABAZINE[18]
GAMMA-AMINO-BUTANOIC ACID[14]
GNF-PF-3645[15]
GNF-PF-4421[15]
L-655708,   NCGC00025115-02[27]
N- (p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide[28]
N-Indan-1-yl-2- (1H-indol-3-yl)-2-oxo-acetamide[29]
N-benzyl-2- (1H-indol-3-yl)-2-oxoacetamide[28]
N-benzyl-2- (5-nitro-1H-indol-3-yl)-2-oxoacetamide[28]
N-butyl-2- (1H-indol-3-yl)-2-oxoacetamide[28]
N-butyl-2- (5-nitro-1H-indol-3-yl)-2-oxoacetamide[28]
PNU-91571[30]
RO-145974[31]
RO-145975[31]
RO-147437[31]
RO-194603[31]
RY-066[32]
Ro-151310[31]
Ro-154513[33]
Ro-4882224[34]
Ro-4938581[34]
THIOCOLCHICOSIDE[14]
TPA-023[35]
U-78875[36]
U-89267[33]
ZK-93423[37]
beta-Carboline-3-carboxylic acid t-butyl ester[10]
ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate[10]
ridine-5-carboxylic acid ethyl ester[38]
sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Neuroprotection of ethanol against cerebral ischemia/reperfusion induced brain injury through GABA receptor activation. Brain Res. 2009 Jun 18;1276:151-8. Epub 2009 May 3. To Reference
Ref 2How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 3J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. To Reference
Ref 4J Med Chem. 1989 May;32(5):1020-4.Benzodiazepine receptor binding activity of 6,9-disubstituted purines. To Reference
Ref 5J Med Chem. 1992 Jun 12;35(12):2214-20.Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. To Reference
Ref 6J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones. To Reference
Ref 7J Med Chem. 1988 Jan;31(1):1-3.Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands. To Reference
Ref 8J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. To Reference
Ref 9J Med Chem. 1996 Jul 5;39(14):2844-51.Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. To Reference
Ref 10Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse. To Reference
Ref 11J Med Chem. 1998 Jul 2;41(14):2537-52.Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors. To Reference
Ref 12J Med Chem. 1990 Sep;33(9):2343-57.Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site. To Reference
Ref 13J Med Chem. 1994 Dec 23;37(26):4576-80.Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. To Reference
Ref 14J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. To Reference
Ref 15J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling. To Reference
Ref 16J Med Chem. 2006 Jul 13;49(14):4442-6.Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds. To Reference
Ref 17J Med Chem. 2010 Apr 22;53(8):3417-21.Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships. To Reference
Ref 18J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. To Reference
Ref 19J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. To Reference
Ref 20Bioorg. Med. Chem. Lett. 5(22):2717-2720 (1995) To Reference
Ref 21J Med Chem. 1983 Apr;26(4):499-503.beta-Carbolines as benzodiazepine receptor ligands. 1. Synthesis and benzodiazepine receptor interaction of esters of beta-carboline-3-carboxylic acid. To Reference
Ref 22J Med Chem. 2005 Apr 21;48(8):3051-9.Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one. To Reference
Ref 23Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. To Reference
Ref 24J Med Chem. 1991 Jan;34(1):281-90.Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. To Reference
Ref 25Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. To Reference
Ref 26J Med Chem. 1987 Oct;30(10):1737-42.1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. To Reference
Ref 27J Med Chem. 2004 Mar 25;47(7):1807-22.3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1. To Reference
Ref 28J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands. To Reference
Ref 29J Med Chem. 2001 Jul 5;44(14):2286-97.Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships. To Reference
Ref 30J Med Chem. 1996 Nov 8;39(23):4654-66.High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines. To Reference
Ref 31J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors. To Reference
Ref 32J Med Chem. 1998 Oct 8;41(21):4130-42.Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis. To Reference
Ref 33J Med Chem. 1994 Mar 18;37(6):758-68.Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. To Reference
Ref 34Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. Epub 2009 Aug 15.The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction. To Reference
Ref 35J Med Chem. 2005 Nov 17;48(23):7089-92.7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. To Reference
Ref 36J Med Chem. 1996 Sep 13;39(19):3820-36.3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex. To Reference
Ref 37J Med Chem. 1990 Mar;33(3):1062-9.Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester. To Reference
Ref 38J Med Chem. 1989 Dec;32(12):2561-73.Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. To Reference



 

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