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TargetGABA receptor alpha-5/beta-3/gamma-2 subunit
LigandBDBM50162197
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303660
Ki 0.84±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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BDBM50162197
n/a
NameBDBM50162197
Synonyms:3,6-dimethyl-2-pyridyl 6-phenyl-4,5,7,8-tetraazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraen-9-yl ether | CHEMBL369035
TypeSmall organic molecule
Emp. Form.C25H25N5O
Mol. Mass.411.4989
SMILESCc1ccc(C)c(COc2nn3c(nnc3c3C4CCC(CC4)c23)-c2ccccc2)n1 |(3.01,-6.91,;1.66,-6.16,;.33,-6.93,;-1,-6.16,;-1,-4.62,;-2.33,-3.83,;.33,-3.87,;.33,-2.33,;-1,-1.56,;-1,-.02,;.33,.74,;.33,2.29,;1.49,3.35,;.85,4.71,;-.67,4.57,;-1,3.07,;-2.33,2.28,;-3.68,2.96,;-3.03,1.52,;-4.6,1.52,;-3.66,-.03,;-4.99,.74,;-4.99,2.28,;-2.33,.74,;3.01,3.05,;4,4.2,;5.51,3.91,;6,2.45,;5,1.28,;3.5,1.59,;1.64,-4.62,)|
Structure
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