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TargetGABA receptor alpha-3/beta-3/gamma-2 subunit
LigandBDBM50162180
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303659
Ki 1.1±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-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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BDBM50162180
n/a
NameBDBM50162180
Synonyms:9-(3-ethoxy-2-pyridyloxy)-6-phenyl-4,5,7,8-tetraazatetracyclo[9.2.2.02,10.03,7]pentadeca-2(10),3,5,8-tetraene | CHEMBL179414
TypeSmall organic molecule
Emp. Form.C25H25N5O2
Mol. Mass.427.4983
SMILESCCOc1cccnc1COc1nn2c(nnc2c2C3CCC(CC3)c12)-c1ccccc1 |(-3.36,-6.04,;-3.36,-4.5,;-2,-3.74,;-.67,-4.51,;-.67,-6.04,;.66,-6.81,;2,-6.04,;1.97,-4.51,;.66,-3.75,;.66,-2.22,;-.67,-1.45,;-.67,.09,;.64,.86,;.64,2.41,;1.81,3.48,;1.18,4.83,;-.34,4.69,;-.67,3.18,;-2,2.4,;-3.36,3.09,;-2.7,1.64,;-4.29,1.64,;-3.34,.09,;-4.67,.86,;-4.67,2.4,;-2,.86,;3.33,3.17,;4.33,4.34,;5.85,4.04,;6.34,2.57,;5.34,1.42,;3.82,1.72,)|
Structure
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