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TargetGamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2
LigandBDBM50185340
Substrate/Competitorn/a
Meas. Tech.ChEMBL_341839 (CHEMBL865018)
Ki 0.5±n/a nM
Citation Lewis, RTBlackaby, WPBlackburn, TJennings, ASPike, AWilson, RAHallett, DJCook, SMFerris, PMarshall, GRReynolds, DSSheppard, WFSmith, AJSohal, BStanley, JTye, SJWafford, KAAtack, JR A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety. J Med Chem49:2600-10 (2006) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2
Name:Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2
Synonyms:GABA receptor alpha-1/beta-3/gamma-2 subunit | GABA-A receptor; alpha-1/beta-3/gamma-2
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 312
Components:This complex has 3 components.
Component 1
Name:Gamma-aminobutyric acid receptor subunit alpha-1
Synonyms:Benzodiazepine central | GABA A Benzodiazepine brain | GABA A Benzodiazepine liver | GABA receptor alpha-1 subunit | GABA(A) receptor subunit alpha-1 | GABA-A | GABA-A receptor | GABRA1 | GBRA1_HUMAN | Gamma-aminobutyric acid receptor subunit alpha (GABAA) | TBPS | agonist GABA site
Type:Protein
Mol. Mass.:51817.35
Organism:Homo sapiens (Human)
Description:P14867
Residue:456
Sequence:
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
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Component 2
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 3
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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BDBM50185340
n/a
NameBDBM50185340
Synonyms:5-[4-fluoro-3-(3-fluoropyridin-2-yl)-phenyl]-3-(3-fluoropyridin-2-yl)pyridazine | CHEMBL206620
TypeSmall organic molecule
Emp. Form.C20H11F3N4
Mol. Mass.364.3233
SMILESFc1ccc(cc1-c1ncccc1F)-c1cnnc(c1)-c1ncccc1F
Structure
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