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TargetGABA receptor alpha-2/beta-3/gamma-2 subunit
LigandBDBM50162183
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303657
Ki 1.7±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-2/beta-3/gamma-2 subunit
Name:GABA receptor alpha-2/beta-3/gamma-2 subunit
Synonyms:GABA-A receptor; alpha-2/beta-3/gamma-2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 68716
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:Gamma-aminobutyric acid receptor subunit alpha-2/beta-2
Synonyms:GABA receptor alpha-2 subunit | Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2)
Type:Protein
Mol. Mass.:51338.78
Organism:Homo sapiens (Human)
Description:P47869
Residue:451
Sequence:
MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPG
LGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSC
PLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVM
TAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASV
MIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRM
SRIVFPVLFGTFNLVYWATYLNREPVLGVSP
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BDBM50162183
n/a
NameBDBM50162183
Synonyms:1-benzyl-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 | CHEMBL361114
TypeSmall organic molecule
Emp. Form.C28H26N6O
Mol. Mass.462.5456
SMILESC(Oc1nn2c(nnc2c2C3CCC(CC3)c12)-c1ccccc1)c1nccn1Cc1ccccc1 |(-.27,-2.33,;-1.61,-1.56,;-1.61,-.03,;-.3,.72,;-.3,2.28,;.89,3.33,;.23,4.71,;-1.28,4.55,;-1.61,3.03,;-2.94,2.26,;-4.29,2.96,;-5.6,2.26,;-5.6,.72,;-4.26,-.05,;-5.2,1.49,;-3.63,1.49,;-2.94,.72,;2.39,3.03,;3.39,4.2,;4.9,3.89,;5.4,2.43,;4.39,1.28,;2.87,1.59,;1.05,-1.56,;1.22,-.03,;2.71,.3,;3.5,-1.05,;2.46,-2.2,;2.78,-3.69,;1.64,-4.71,;.19,-4.25,;-.95,-5.3,;-.63,-6.79,;.85,-7.26,;1.97,-6.23,)|
Structure
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