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Target
Gamma-aminobutyric acid receptor subunit alpha-6/beta-3/gamma-2
Ligand
BDBM50083910
Substrate
n/a
Meas. Tech.
ChEMBL_68433 (CHEMBL683045)
Ki
>10000±n/a nM
Citation
 Huang, Q; He, X; Ma, C; Liu, R; Yu, S; Dayer, CA; Wenger, GR; McKernan, R; Cook, JM Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach. J Med Chem 43:71-95 (2000) [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:
BDBM50083910
Synonyms:
7,12-Dihydro-4,5,7,12-tetraaza-indeno[1,2-a]fluorene | CHEMBL172866
Type:
Small organic molecule
Emp. Form.:
C16H10N4
Mol. Mass.:
258.2774
SMILES:
c1ccc2c(c1)[nH]c1c[nH]c3c(nc4cccnc34)c21
Structure:
Search PDB for entries with ligand similarity: