Target
Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-467,T165C]
Ligand
BDBM26266
Substrate
BDBM26263
Meas. Tech.
Radioligand Binding Assay
Temperature
298.15±n/a K
Ki
72.7±n/a nM
Comments
extracted
Citation
 Hanson, SMMorlock, EVSatyshur, KACzajkowski, 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-1 [28-456]/beta-2 [26-512]/gamma-2 [40-467,T165C]
Synonyms:
GABAA Receptor Mutant, alpha-1, beta-2, gamma-2 (T126C)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
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 2
Name:
Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]
Synonyms:
GABA(A) receptor subunit alpha-1 | GABAA Receptor Subunit alpha-1 | GABRA1 | GBRA1_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-1
Type:
Ionic channel
Mol. Mass.:
48807.81
Organism:
Homo sapiens (Human)
Description:
P14867[28-456]
Residue:
429
Sequence:
QPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
  
Component 3
Name:
Gamma-aminobutyric acid receptor subunit gamma-2 [40-467,T165C]
Synonyms:
GABA(A) receptor subunit gamma-2 benzodiazepine binding site loop E mutant | GABAA Receptor Subunit gamma-2 Mutant (T126C) | GABRG2 | GBRG2_HUMAN
Type:
Ionic channel
Mol. Mass.:
49864.80
Organism:
Homo sapiens (Human)
Description:
P18507[40-467,T165C]
Residue:
428
Sequence:
QKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITCPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
Inhibitor
Name:
BDBM26266
Synonyms:
Ambien | CHEMBL911 | Dalparan | N,N-dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide | ZPM | Zolpidem | Zolpidem tartrate
Type:
Small organic molecule
Emp. Form.:
C19H21N3O
Mol. Mass.:
307.3895
SMILES:
CN(C)C(=O)Cc1c(nc2ccc(C)cn12)-c1ccc(C)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM26263
Synonyms:
Anexate | CHEMBL407 | FLUMAZENIL | Ro15-1788 | Romazicon | [3H]Ro15-1788 | ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,10,12-pentaene-5-carboxylate
Type:
Small organic molecule
Emp. Form.:
C15H14FN3O3
Mol. Mass.:
303.2884
SMILES:
CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(F)ccc-21
Structure:
Search PDB for entries with ligand similarity: