Reaction Details Report a problem with these data
Target
Gamma-aminobutyric acid receptor subunit alpha-1 [T162C]/beta-2 [26-512]/gamma-2 [40-467]
Ligand
BDBM26266
Substrate
BDBM26263
Meas. Tech.
Radioligand Binding Assay
Temperature
298.1500±n/a K
Ki
109±n/a nM
Comments
extracted
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-1 [T162C]/beta-2 [26-512]/gamma-2 [40-467]
Synonyms:
GABAA Receptor Mutant, alpha-1 (T162C), 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 | Gamma-aminobutyric acid receptor subunit gamma-2 | GBRG2_HUMAN | GABRG2 | GABAA Receptor Subunit gamma-2
Type:
Ionic channel
Mol. Mass.:
49862.76
Organism:
Human
Description:
P18507[40-467]
Residue:
428
Sequence:
QKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
Component 2
Name:
Gamma-aminobutyric acid receptor subunit beta-2 [26-512]
Synonyms:
GBRB2_HUMAN | GABRB2 | GABA(A) receptor subunit beta-2 | Gamma-aminobutyric acid receptor subunit beta-2 | GABAA Receptor Subunit beta-2
Type:
Ionic channel
Mol. Mass.:
56212.32
Organism:
Human
Description:
P47870[26-512]
Residue:
487
Sequence:
SVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKIFYKDIKQNGTQYRSLWDPTGNLSPTRRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
  
Component 3
Name:
Gamma-aminobutyric acid receptor subunit alpha-1 [T162C]
Synonyms:
GBRA1_HUMAN | GABRA1 | GABAA Receptor Subunit alpha-1 Mutant (T162C) | GABA(A) receptor subunit alpha-1 benzodiazepine binding site loop B mutant
Type:
Ionic channel
Mol. Mass.:
48809.85
Organism:
Human
Description:
P14867[T162C]
Residue:
429
Sequence:
QPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYCRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
  
Inhibitor
Name:
BDBM26266
Synonyms:
Ambien | CHEMBL911 | ZPM | N,N-dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide | Dalparan | Zolpidem | Zolpidem tartrate
Type:
Small organic molecule
Emp. Form.:
C19H21N3O
Mol. Mass.:
307.17
SMILES:
CN(C)C(=O)Cc1c(nc2ccc(C)cn12)-c1ccc(C)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM26263
Synonyms:
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 | FLUMAZENIL | Anexate | Romazicon | CHEMBL407 | [3H]Ro15-1788 | Ro15-1788
Type:
Small organic molecule
Emp. Form.:
C15H14FN3O3
Mol. Mass.:
303.10
SMILES:
CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(F)ccc-21
Structure:
Search PDB for entries with ligand similarity: