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TargetGABA receptor alpha-3/beta-3/gamma-2 subunit
LigandBDBM50185514
Substrate/Competitorn/a
Meas. Tech.ChEMBL_373310
Ki 0.36±n/a nM
Citation Carling RWRussell MGMoore KWMitchinson AGuiblin ASmith AWafford KAMarshall GAtack JRStreet LJ 2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists. Bioorg Med Chem Lett 16:3550-4 (2006) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
GABA receptor alpha-3/beta-3/gamma-2 subunit
Name:GABA receptor alpha-3/beta-3/gamma-2 subunit
Synonyms:GABA-A receptor; alpha-3/beta-3/gamma-2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 68410
Components:This complex has 3 components.
Component 1
Name:GABA A receptor alpha-2/beta-2/gamma-2
Synonyms:GABA(A) receptor subunit gamma-2 | Gamma-aminobutyric acid receptor subunit gamma-2
Type:PROTEIN
Mol. Mass.:54172.74
Organism:Homo sapiens (Human)
Description:EBI_217
Residue:467
Sequence:
MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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Component 2
Name:Gamma-aminobutyric acid receptor subunit alpha-3/beta-3
Synonyms:GABA receptor beta-3 subunit | GABA-A receptor | agonist GABA site
Type:PROTEIN
Mol. Mass.:54130.51
Organism:Homo sapiens (Human)
Description:ChEMBL_448071
Residue:473
Sequence:
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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Component 3
Name:GABA A receptor alpha-3/beta-2/gamma-2
Synonyms:GABA A Alpha3Beta3Gamma2 | GABA C | GABA receptor alpha-3 subunit | GABA-A receptor | Gamma-aminobutyric acid receptor subunit alpha-3 | agonist GABA site
Type:Enzyme Catalytic Domain
Mol. Mass.:55175.47
Organism:Homo sapiens (Human)
Description:GABA A Alpha3Beta1Gamma2 0 HUMAN::P34903
Residue:492
Sequence:
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
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BDBM50185514
n/a
NameBDBM50185514
Synonyms:7-cyclopropyl-3-(2-fluorophenyl)-2-((2-methyl-2H-1,2,4-triazol-3-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazine | CHEMBL208794
TypeSmall organic molecule
Emp. Form.C18H16FN7O
Mol. Mass.365.3643
SMILESCn1ncnc1COc1nn2c(nncc2c1-c1ccccc1F)C1CC1 |(25.8,-32.62,;24.27,-32.39,;23.2,-33.5,;21.82,-32.82,;22.03,-31.3,;23.56,-31.03,;24.33,-29.7,;23.57,-28.36,;24.34,-27.03,;25.88,-26.87,;26.21,-25.37,;27.55,-24.59,;27.54,-23.04,;26.2,-22.28,;24.88,-23.05,;24.87,-24.59,;23.72,-25.62,;22.39,-24.85,;22.39,-23.32,;21.06,-22.55,;19.72,-23.33,;19.73,-24.87,;21.07,-25.63,;21.08,-27.17,;28.88,-25.36,;29.65,-26.69,;30.42,-25.35,)|
Structure
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