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Target
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
Ligand
BDBM26267
Substrate
n/a
Meas. Tech.
ChEMBL_69811 (CHEMBL677846)
Ki
3.8±n/a nM
Citation
 Li, X; Cao, H; Zhang, C; Furtmueller, R; Fuchs, K; Huck, S; Sieghart, W; Deschamps, J; Cook, JM Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist. J Med Chem 46:5567-70 (2003) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
Synonyms:
GABA receptor alpha-6/beta-3/gamma-2 subunit | GABA-A receptor; alpha-6/beta-3/gamma-2
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 68432
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:
MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
Component 2
Name:
Gamma-aminobutyric acid receptor subunit alpha-6
Synonyms:
GABA A alpha6 | GABA receptor alpha-6 subunit | GABRA6 | GBRA6_HUMAN
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51029.60
Organism:
Homo sapiens (Human)
Description:
GABA A alpha6 0 HUMAN::Q16445
Residue:
453
Sequence:
MASSLPWLCIILWLENALGKLEVEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFGGPTEILSLNNLMVSKIWTPDTFFRNGKKSIAHNMTTPNKLFRIMQNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYPKSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKMGYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNLQTQKAKRKAQFAAPPTVTISKATEPLEAEIVLHPDSKYHLKKRITSLSLPIVSSSEANKVLTRAPILQSTPVTPPPLSPAFGGTSKIDQYSRILFPVAFAGFNLVYWVVYLSKDTMEVSSSVE
  
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:
MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPPVCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNRVDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRSLPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
  
Inhibitor
Name:
BDBM26267
Synonyms:
RO-154513 | Ro15-4513 | [3H]Ro15-4513 | ethyl 12-azido-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,11,13-pentaene-5-carboxylate
Type:
radiolabeled ligand
Emp. Form.:
C15H14N6O3
Mol. Mass.:
326.3101
SMILES:
CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(ccc-21)N=[N+]=[N-]
Structure:
Search PDB for entries with ligand similarity: