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Target
Gamma-aminobutyric acid receptor subunit alpha-2/beta-2/gamma-2
Ligand
BDBM50206938
Substrate
n/a
Meas. Tech.
ChEMBL_428868 (CHEMBL917144)
Ki
553±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-2/beta-2/gamma-2
Synonyms:
GABA receptor alpha-2/beta-2/gamma-2 subunit
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 37810
Components:
This complex has 3 components.
Component 1
Name:
Gamma-aminobutyric acid receptor subunit beta-2
Synonyms:
GBRB2_RAT | Gabrb-2 | Gabrb2 | Gamma-aminobutyric acid receptor subunit beta-2 (GABA(A) beta-2)
Type:
Enzyme
Mol. Mass.:
54648.97
Organism:
Rattus norvegicus (Rat)
Description:
P63138
Residue:
474
Sequence:
MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAANANNEKMRLDVNKMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
  
Component 2
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 3
Name:
Gamma-aminobutyric acid receptor subunit alpha-2
Synonyms:
GABA A Alpha2Beta2Gamma2 | GABA A alpha2 | GABA A receptor alpha-2/beta-2/gamma-2 | GABA receptor alpha-2 subunit | GABA(A) receptor subunit alpha-2 | GBRA2_RAT | Gabra-2 | Gabra2 | Gamma-aminobutyric acid receptor subunit alpha-2
Type:
Enzyme
Mol. Mass.:
51195.57
Organism:
Rattus norvegicus (Rat)
Description:
P23576
Residue:
451
Sequence:
MRTKLSTCNVWFPLLVLLVWNPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPGLGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNSMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSCPLKFGSYAYTTSEVTYIWTYNPSDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKGSVMIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRMSRIVFPVLFGTFNLVYWATYLNREPVLGVSP
  
Inhibitor
Name:
BDBM50206938
Synonyms:
CHEMBL222316 | N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide
Type:
Small organic molecule
Emp. Form.:
C14H15N3O4
Mol. Mass.:
289.2866
SMILES:
CCCCNC(=O)C(=O)c1c[nH]c2ccc(cc12)[N+]([O-])=O
Structure:
Search PDB for entries with ligand similarity: