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Target
Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2
Ligand
BDBM50206937
Substrate
n/a
Meas. Tech.
ChEMBL_428870 (CHEMBL917146)
Ki
1154±n/a nM
Citation
 Primofiore, G; Taliani, S; Da Settimo, F; Marini, AM; La Motta, C; Simorini, F; Patrizi, MP; Sergianni, V; Novellino, E; Greco, G; Cosimelli, B; Calderone, V; Montali, M; Besnard, F; Martini, C Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands. J Med Chem 50:1627-34 (2007) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-2
Synonyms:
GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5/beta-3/gamma-2 subunit
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 70706
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:
MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
Component 2
Name:
Gamma-aminobutyric acid receptor subunit alpha-5
Synonyms:
GABA A Alpha5Beta2Gamma2 | GABA A Alpha5Beta3Gamma2 | GABA A Alpha5m10Beta2Gamma2 | GABA A Alpha5m8Beta2Gamma2 | GABA A Alpha5m9Beta2Gamma2 | GABA A alpha5 | GABA A receptor alpha-5/beta-3/gamma-2 | GABA receptor alpha-5 subunit | GBRA5_RAT | Gabra-5 | Gabra5 | Gamma-aminobutyric acid receptor subunit alpha-5
Type:
Enzyme Catalytic Domain
Mol. Mass.:
52350.79
Organism:
RAT
Description:
GABA A alpha5 0 RAT::P19969
Residue:
464
Sequence:
MDNGMLSRFIMTKTLLVFCISMTLSSHFGFSQMPTSSVQDETNDNITIFTRILDGLLDGYDNRLRPGLGERITQVRTDIYVTSFGPVSDTEMEYTIDVFFRQSWKDERLRFKGPMQRLPLNNLLASKIWTPDTFFHNGKKSIAHNMTTPNKLLRLEDDGTLLYTMRLTISAECPMQLEDFPMDAHACPLKFGSYAYPNSEVVYVWTNGSTKSVVVAEDGSRLNQYHLMGQTVGTENISTSTGEYTIMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKKALEAAKIKKKERELILNKSTNAFTTGKLTHPPNIPKEQLPGGTGNAVGTASIRASEEKTSESKKTYNSISKIDKMSRIVFPILFGTFNLVYWATYLNREPVIKGATSPK
  
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:
MWGFAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPPVCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSEINRVDAHGNILLAPMDVHNEMNEVAGSVGDTRNSAISFDNSGIQYRKQSMPKEGHGRYMGDRSIPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
  
Inhibitor
Name:
BDBM50206937
Synonyms:
CHEMBL373871 | N-(4-ethynylbenzyl)-2-(1H-indol-3-yl)-2-oxoacetamide
Type:
Small organic molecule
Emp. Form.:
C19H14N2O2
Mol. Mass.:
302.3267
SMILES:
O=C(NCc1ccc(cc1)C#C)C(=O)c1c[nH]c2ccccc12
Structure:
Search PDB for entries with ligand similarity: