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TargetGABA receptor alpha-5/beta-3/gamma-2 subunit
LigandBDBM50162223
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303660
Ki 0.54±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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BDBM50162223
n/a
NameBDBM50162223
Synonyms:2-[6-phenyl-4,5,7,8-tetraazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraen-9-yloxy]-3-pyridyl cyanide | CHEMBL179475
TypeSmall organic molecule
Emp. Form.C24H20N6O
Mol. Mass.408.4552
SMILESN#Cc1cccnc1COc1nn2c(nnc2c2C3CCC(CC3)c12)-c1ccccc1 |(-3.45,-3.2,;-2.12,-3.97,;-.79,-4.74,;-.79,-6.28,;.54,-7.06,;1.87,-6.28,;1.87,-4.74,;.54,-3.99,;.54,-2.46,;-.79,-1.68,;-.79,-.15,;.54,.61,;.54,2.17,;1.7,3.22,;1.07,4.59,;-.46,4.43,;-.79,2.93,;-2.12,2.15,;-3.45,2.84,;-2.82,1.39,;-4.39,1.39,;-3.45,-.15,;-4.78,.61,;-4.78,2.15,;-2.12,.61,;3.22,2.92,;3.71,1.46,;5.21,1.16,;6.23,2.33,;5.73,3.78,;4.21,4.08,)|
Structure
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