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TargetGamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
LigandBDBM50457440
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1759652 (CHEMBL4194660)
IC50 5510±n/a nM
Citation Yakoub, KJung, SSattler, CDamerow, HWeber, JKretzschmann, ACankaya, ASPiel, MRösch, FHaugaard, ASFrølund, BSchirmeister, TLüddens, H Structure-Function Evaluation of Imidazopyridine Derivatives Selective for ?-Subunit-Containing ?-Aminobutyric Acid Type A (GABA J Med Chem61:1951-1968 (2018) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
Name:Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
Synonyms:n/a
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 1759707
Components:This complex has 3 components.
Component 1
Name:Gamma-aminobutyric acid receptor subunit gamma-2
Synonyms:GBRG2_RAT | Gabrg2 | Gamma-aminobutyric acid receptor subunit gamma-2 (GABA(A) gamma-2)
Type:Enzyme
Mol. Mass.:54087.63
Organism:Rattus norvegicus (Rat)
Description:P18508
Residue:466
Sequence:
MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKV
PEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTW
YDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYT
LRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFS
FVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAV
PARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVS
NRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCF
EDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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Component 2
Name:Gamma-aminobutyric acid receptor subunit alpha-6
Synonyms:GABA A Alpha6Beta3Gamma2 | GABA A receptor alpha-6/beta-2/gamma-2 | GABA receptor alpha-6 subunit | GBRA6_RAT | Gabra-6 | Gabra6 | Gamma-aminobutyric acid receptor subunit alpha-6
Type:Enzyme Catalytic Domain
Mol. Mass.:51188.24
Organism:RAT
Description:GABA A Alpha6Beta2Gamma2 0 RAT::P30191
Residue:453
Sequence:
MLLLLPWLFSLLWIENAQAQLEDEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKT
DIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFKGPAEILSLNNLMVSKIWTPDTFFRN
GKKSIAHNMTTPNKLFRLMHNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYP
KSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKM
GYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYA
TAMDWFIAVCFAFVFSALIEFAAVNYFTNLQSQKAERQAQTAAKPPVAKSKTTESLEAEI
VVHSDSKYHLKKRISSLTLPIVPSSEASKVLSRTPILPSTPVTPPLLLPAIGGTSKIDQY
SRILFPVAFAGFNLVYWIVYLSKDTMEVSSTVE
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Component 3
Name:Gamma-aminobutyric acid receptor subunit beta-3
Synonyms:GABA receptor beta-3 subunit | GBRB3_RAT | Gabrb-3 | Gabrb3
Type:PROTEIN
Mol. Mass.:54180.66
Organism:Rattus norvegicus
Description:EBI_12481
Residue:473
Sequence:
MWGFAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSEINR
VDAHGNILLAPMDVHNEMNEVAGSVGDTRNSAISFDNSGIQYRKQSMPKEGHGRYMGDRS
IPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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BDBM50457440
n/a
NameBDBM50457440
Synonyms:CHEMBL4204097
TypeSmall organic molecule
Emp. Form.C22H19Br2N3O2S
Mol. Mass.549.278
SMILESCCCCOc1ccc(cc1)C(=O)Nc1c(nc2c(Br)cc(Br)cn12)-c1cccs1
Structure
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