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TargetGamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2
LigandBDBM50176770
Substrate/Competitorn/a
Meas. Tech.ChEMBL_430693 (CHEMBL919089)
Ki 1.8±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 Chem48:7089-92 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2
Name:Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2
Synonyms:GABA receptor alpha-3/beta-3/gamma-2 subunit | 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:Gamma-aminobutyric acid receptor subunit gamma-2
Synonyms:GABA(A) receptor subunit gamma-2 | GABRG2 | GBRG2_HUMAN
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 beta-3
Synonyms:GABA A receptor alpha-4/beta-3/gamma-2 | GABA receptor beta-3 subunit | GABA-A receptor | GABRB3 | GBRB3_HUMAN | 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-3
Synonyms:GABA A Alpha3Beta3Gamma2 | GABA A receptor alpha-3/beta-2/gamma-2 | GABA C | GABA receptor alpha-3 subunit | GABA-A receptor | GABRA3 | GBRA3_HUMAN | 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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BDBM50176770
n/a
NameBDBM50176770
Synonyms:3,7-diphenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[4,3-b]pyridazine | CHEMBL224134
TypeSmall organic molecule
Emp. Form.C23H17N5O
Mol. Mass.379.414
SMILESC(Oc1nn2c(nnc2cc1-c1ccccc1)-c1ccccc1)c1ccccn1
Structure
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