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TargetGABA receptor alpha-3/beta-3/gamma-2 subunit
LigandBDBM50176773
Substrate/Competitorn/a
Meas. Tech.ChEMBL_430693
Ki 0.14±n/a nM
Citation Carling RWMadin AGuiblin ARussell MGMoore KWMitchinson ASohal BPike ACook SMRagan ICMcKernan RMQuirk KFerris PMarshall GThompson SAWafford KADawson GRAtack JRHarrison TCastro JLStreet LJ 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models. J Med Chem 48:7089-92 (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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BDBM50176773
n/a
NameBDBM50176773
Synonyms:7-tert-butyl-6-(2-methyl-2H-1,2,4-trizol-3-ylmethoxy)-3-phenyl-1,2,4-triazolo[4,3-b]pyridazine | CHEMBL225631
TypeSmall organic molecule
Emp. Form.C19H21N7O
Mol. Mass.363.4163
SMILESCn1ncnc1COc1nn2c(nnc2cc1C(C)(C)C)-c1ccccc1
Structure
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