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Target
Gamma-aminobutyric acid receptor subunit alpha-6 [20-453]/beta-2 [26-512]/gamma-2 [40-467]
Ligand
BDBM26265
Substrate
BDBM26267
Meas. Tech.
Radioligand Binding Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
>15000±n/a nM
Citation
 Hanson, SM; Morlock, EV; Satyshur, KA; Czajkowski, C Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different. J Med Chem 51:7243-52 (2008) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-6 [20-453]/beta-2 [26-512]/gamma-2 [40-467]
Synonyms:
GABAA Receptor, alpha-6, beta-2, gamma-2
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
Name:
Gamma-aminobutyric acid receptor subunit gamma-2 [40-467]
Synonyms:
GABA(A) receptor subunit gamma-2 | GABAA Receptor Subunit gamma-2 | GABRG2 | GBRG2_HUMAN | Gamma-aminobutyric acid receptor subunit gamma-2
Type:
Ionic channel
Mol. Mass.:
49862.76
Organism:
Homo sapiens (Human)
Description:
P18507[40-467]
Residue:
428
Sequence:
QKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
Component 2
Name:
Gamma-aminobutyric acid receptor subunit beta-2 [26-512]
Synonyms:
GABA(A) receptor subunit beta-2 | GABAA Receptor Subunit beta-2 | GABRB2 | GBRB2_HUMAN | Gamma-aminobutyric acid receptor subunit beta-2
Type:
Ionic channel
Mol. Mass.:
56212.32
Organism:
Homo sapiens (Human)
Description:
P47870[26-512]
Residue:
487
Sequence:
SVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKIFYKDIKQNGTQYRSLWDPTGNLSPTRRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
  
Component 3
Name:
Gamma-aminobutyric acid receptor subunit alpha-6 [20-453]
Synonyms:
GABA(A) receptor subunit alpha-6 | GABAA Receptor Subunit alpha-6 | GABRA6 | GBRA6_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-6
Type:
Ionic channel
Mol. Mass.:
48918.05
Organism:
Homo sapiens (Human)
Description:
Q16445[20-453]
Residue:
434
Sequence:
KLEVEGNFYSENVSRILDNLLEGYDNRLRPGFGGAVTEVKTDIYVTSFGPVSDVEMEYTMDVFFRQTWTDERLKFGGPTEILSLNNLMVSKIWTPDTFFRNGKKSIAHNMTTPNKLFRIMQNGTILYTMRLTINADCPMRLVNFPMDGHACPLKFGSYAYPKSEIIYTWKKGPLYSVEVPEESSSLLQYDLIGQTVSSETIKSNTGEYVIMTVYFHLQRKMGYFMIQIYTPCIMTVILSQVSFWINKESVPARTVFGITTVLTMTTLSISARHSLPKVSYATAMDWFIAVCFAFVFSALIEFAAVNYFTNLQTQKAKRKAQFAAPPTVTISKATEPLEAEIVLHPDSKYHLKKRITSLSLPIVSSSEANKVLTRAPILQSTPVTPPPLSPAFGGTSKIDQYSRILFPVAFAGFNLVYWVVYLSKDTMEVSSSVE
  
Inhibitor
Name:
BDBM26265
Synonyms:
(5S)-6-(5-chloropyridin-2-yl)-7-oxo-5H,6H,7H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate | ESZ | Estorra | Eszopiclone | Lunesta | cid_5735
Type:
Small organic molecule
Emp. Form.:
C17H17ClN6O3
Mol. Mass.:
388.808
SMILES:
CN1CCN(CC1)C(=O)Oc1n(-c2ccc(Cl)cn2)c(=O)c2ncc[nH]c12
Structure:
Search PDB for entries with ligand similarity:
Substrate
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: