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TargetGABA receptor alpha-5/beta-3/gamma-2 subunit
LigandBDBM50162190
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303660
Ki 0.45±n/a nM
Citation Russell MGCarling RWAtack JRBromidge FACook SMHunt PIsted CLucas MMcKernan RMMitchinson AMoore KWNarquizian RMacaulay AJThomas DThompson SAWafford KACastro JL 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 48:1367-83 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
GABA receptor alpha-5/beta-3/gamma-2 subunit
Name:GABA receptor alpha-5/beta-3/gamma-2 subunit
Synonyms:GABA-A receptor; alpha-5/beta-3/gamma-2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 69797
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-5/beta-3/gamma-3
Synonyms:GABA A Alpha5Beta1Gamma2 | GABA A Alpha5Beta3Gamma2 | GABA receptor alpha-5 subunit | GABA(A) receptor subunit alpha-5 (GABAAa5) | Gamma-aminobutyric acid receptor subunit alpha-5 | Gamma-aminobutyric acid receptor subunit alpha-5 (GABAA)
Type:Enzyme
Mol. Mass.:52160.59
Organism:Homo sapiens (Human)
Description:P31644
Residue:462
Sequence:
MDNGMFSGFIMIKNLLLFCISMNLSSHFGFSQMPTSSVKDETNDNITIFTRILDGLLDGY
DNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPL
NNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDF
PMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTS
TGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTM
TTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAA
KIKKKREVILNKSTNAFTTGKMSHPPNIPKEQTPAGTSNTTSVSVKPSEEKTSESKKTYN
SISKIDKMSRIVFPVLFGTFNLVYWATYLNREPVIKGAASPK
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Component 3
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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BDBM50162190
n/a
NameBDBM50162190
Synonyms:1-methyl-1H-2-imidazolyl[6-phenyl-4,5,7,8-tetraazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraen-9-yloxy]methane | CHEMBL366537
TypeSmall organic molecule
Emp. Form.C22H22N6O
Mol. Mass.386.4497
SMILESCn1ccnc1COc1nn2c(nnc2c2C3CCC(CC3)c12)-c1ccccc1 |(2.89,-4.89,;2.58,-3.38,;3.59,-2.24,;2.83,-.91,;1.31,-1.22,;1.17,-2.76,;-.18,-3.53,;-1.49,-2.76,;-1.49,-1.22,;-.19,-.47,;-.19,1.09,;.98,2.15,;.35,3.52,;-1.18,3.35,;-1.49,1.84,;-2.84,1.09,;-4.18,1.77,;-5.5,1.09,;-5.5,-.47,;-4.17,-1.22,;-5.11,.3,;-3.54,.3,;-2.84,-.47,;2.5,1.84,;3.51,3,;5,2.71,;5.51,1.24,;4.49,.09,;2.99,.39,)|
Structure
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