Therapeutic Targets Database
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TTD Target ID: TTDS00410

Target Information
NameGamma-aminobutyric acid receptor subunit beta-2    
Type of targetSuccessful target    
SynonymsGABA(A) receptor subunit beta-2    
GABRB2    
DiseaseInsomnia
[ICD9: 307.41, 307.42, 327.0, 780.51, 780.52   ICD10: F51.0, G47.0]
[1][2]
Drug(s)EthchlorvynolApprovedInsomnia[3]
BioChemical ClassChloride channel    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP47870
SequenceMWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKM DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2E,4S)-4-ammoniopent-2-enoate[4]
(4R)-4-ammoniopentanoate[4]
(4S)-4-ammoniopentanoate[4]
(9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine[5]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one[6]
1- (4-chlorophenyl)-4-phenyl-1H-imidazole[7]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one[6]
2- (4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one[7]
2- (9-Benzyl-9H-purin-6-ylamino)-ethanol[5]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline[8]
2-Oxa-spiro[4.4]nonan-1-one[6]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline[8]
3,3-Diethyl-dihydro-furan-2-one[6]
3,3-Diisopropyl-dihydro-furan-2-one[6]
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[9]
3-Methyl-9H-beta-carboline[10]
3-amino-3-demethoxythiocolchicine[11]
3-butoxycarbonyl-4-quinolone[12]
3-butoxycarbonyl-6-ethyl-4-quinolone[12]
3-butylaminocarbonyl-6-ethyl-4-quinolone[12]
3-carboxy-6-ethyl-4-quinolone[12]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone[12]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine[11]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine[11]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine[11]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine[11]
3-demethoxy-3D-glucopyranosylaminothiocolchicine[11]
3-ethoxycarbonyl-4-quinolone[12]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone[12]
3-ethoxycarbonyl-6-propyl-4-quinolone[12]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one[6]
4- (2-aminoethyl)-1,2,5-oxadiazol-3-ol[13]
4- (4-chlorophenyl)-1-pyrid-2-yl-pyrazole[7]
4- (biphenyl-3-yl)-5-[14]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol[15]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol[15]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol[15]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol[15]
5-Piperidin-4-yl-isoxazol-3-ol[15]
5-[ (1R)-1-ammonioethyl]isoxazol-3-olate[4]
5-[ (1S)-1-ammonioethyl]isoxazol-3-olate[4]
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-benzyl-3-ethoxycarbonyl-4-quinolone[12]
6-benzyl-3-propoxycarbonyl-4-quinolone[12]
6-benzyl-3-propylaminocarbonyl-4-quinolone[12]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone[12]
6-bromo-3-ethoxycarbonyl-4-quinolone[12]
6-ethyl-3- (2-ethylbutoxycarbonyl)-4-quinolone[12]
6-ethyl-3- (2-methylbutoxycarbonyl)-4-quinolone[12]
6-ethyl-3- (3-methylbutoxycarbonyl)-4-quinolone[12]
6-ethyl-3- (3-pentoxycarbonyl)-4-quinolone[12]
6-ethyl-3-i-propoxycarbonyl-4-quinolone[12]
6-ethyl-3-pentoxycarbonyl-4-quinolone[12]
6-ethyl-3-propoxycarbonyl-4-quinolone[12]
6-ethyl-3-propylaminocarbonyl-4-quinolone[12]
ALLOPREGNANOLONE[16]
AMENTOFLAVONE[17]
BETA-CCM[10]
CGS-13767[18]
CGS-8216[19]
CGS-9896[7]
CI-218872[10]
ELTANOLONE[16]
GABAZINE[15]
GAMMA-AMINO-BUTANOIC ACID[11]
GNF-PF-3645[12]
GNF-PF-4421[12]
N- (p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide[20]
N-Indan-1-yl-2- (1H-indol-3-yl)-2-oxo-acetamide[21]
N-benzyl-2- (1H-indol-3-yl)-2-oxoacetamide[20]
N-benzyl-2- (5-nitro-1H-indol-3-yl)-2-oxoacetamide[20]
N-butyl-2- (1H-indol-3-yl)-2-oxoacetamide[20]
N-butyl-2- (5-nitro-1H-indol-3-yl)-2-oxoacetamide[20]
PNU-91571[22]
RO-145974[23]
RO-145975[23]
RO-147437[23]
RO-194603[23]
Ro-151310[23]
Ro-154513[23]
THIOCOLCHICOSIDE[11]
U-78875[22]
U-89267[24]
ZK-93423[25]
ridine-5-carboxylic acid ethyl ester[26]
AntagonistEthchlorvynol[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Hypnotic drugs. Med Lett Drugs Ther. 2000 Aug 7;42(1084):71-2. To Reference
Ref 2The treatment of sleep disorders. S Afr Med J. 1992 May 2;Suppl:1-8. To Reference
Ref 3DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. To Reference
Ref 4J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. To Reference
Ref 5J Med Chem. 1989 May;32(5):1020-4.Benzodiazepine receptor binding activity of 6,9-disubstituted purines. 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. 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 8J 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 9J 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 10J 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 11J 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 12J 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 13J 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 14J 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 15J 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 16J 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 17Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. To Reference
Ref 18J 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 19Bioorg Med Chem Lett. 2000 Dec 18;10(24):2723-6.Substituted 3-(2-benzoxazyl)-benzimidazol-2-(1H)-ones: a new class of GABA(A) brain receptor ligands. To Reference
Ref 20J 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 21J 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 22J 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 23J 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 24J 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 25J 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 26J 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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