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Target
GABA-A receptor; alpha-2/beta-3/gamma-2
Ligand
BDBM86521
Substrate
n/a
Meas. Tech.
ChEMBL_938814 (CHEMBL2327958)
EC50
1630±n/a nM
Citation
 Bagal, SK; Brown, AD; Cox, PJ; Omoto, K; Owen, RM; Pryde, DC; Sidders, B; Skerratt, SE; Stevens, EB; Storer, RI; Swain, NA Ion channels as therapeutic targets: a drug discovery perspective. J Med Chem 56:593-624 (2013) [PubMed]  Article 
Target
Name:
GABA-A receptor; alpha-2/beta-3/gamma-2
Synonyms:
GABA receptor alpha-2/beta-3/gamma-2 subunit | Gamma-aminobutyric acid receptor subunit alpha-2/beta-3/gamma-2
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 2148174
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 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
  
Component 3
Name:
Gamma-aminobutyric acid receptor subunit alpha-2
Synonyms:
GABA receptor alpha-2 subunit | GABRA2 | GBRA2_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2)
Type:
Protein
Mol. Mass.:
51338.78
Organism:
Homo sapiens (Human)
Description:
P47869
Residue:
451
Sequence:
MKTKLNIYNMQFLLFVFLVWDPARLVLANIQEDEAKNNITIFTRILDRLLDGYDNRLRPGLGDSITEVFTNIYVTSFGPVSDTDMEYTIDVFFRQKWKDERLKFKGPMNILRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRIQDDGTLLYTMRLTVQAECPMHLEDFPMDAHSCPLKFGSYAYTTSEVTYIWTYNASDSVQVAPDGSRLNQYDLLGQSIGKETIKSSTGEYTVMTAHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGWAWDGKSVVNDKKKEKASVMIQNNAYAVAVANYAPNLSKDPVLSTISKSATTPEPNKKPENKPAEAKKTFNSVSKIDRMSRIVFPVLFGTFNLVYWATYLNREPVLGVSP
  
Inhibitor
Name:
BDBM86521
Synonyms:
CAS_5719 | NSC_5719 | Zaleplon
Type:
Small organic molecule
Emp. Form.:
C17H15N5O
Mol. Mass.:
305.3339
SMILES:
CCN(C(C)=O)c1cccc(c1)-c1ccnc2c(cnn12)C#N
Structure:
Search PDB for entries with ligand similarity: