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Target
Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-467,D95C]
Ligand
BDBM26265
Substrate
BDBM26263
Meas. Tech.
Radioligand Binding Assay
Temperature
298.1500±n/a K
Ki
82.4±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 [28-456]/beta-2 [26-512]/gamma-2 [40-467,D95C]
Synonyms:
GABAA Receptor Mutant, alpha-1, beta-2, gamma-2 (D56C)
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:
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 2
Name:
Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]
Synonyms:
GABA(A) receptor subunit alpha-1 | Gamma-aminobutyric acid receptor subunit alpha-1 | GBRA1_HUMAN | GABRA1 | GABAA Receptor Subunit alpha-1
Type:
Ionic channel
Mol. Mass.:
48807.81
Organism:
Human
Description:
P14867[28-456]
Residue:
429
Sequence:
QPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
  
Component 3
Name:
Gamma-aminobutyric acid receptor subunit gamma-2 [40-467,D95C]
Synonyms:
GBRG2_HUMAN | GABRG2 | GABAA Receptor Subunit gamma-2 Mutant (D56C)
Type:
Ionic channel
Mol. Mass.:
49851.83
Organism:
Human
Description:
P18507[40-467,D95C]
Residue:
428
Sequence:
QKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTCMYVNSIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
  
Inhibitor
Name:
BDBM26265
Synonyms:
ESZ | Estorra | cid_5735 | (5S)-6-(5-chloropyridin-2-yl)-7-oxo-5H,6H,7H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate | Lunesta | Eszopiclone
Type:
Small organic molecule
Emp. Form.:
C17H17ClN6O3
Mol. Mass.:
388.11
SMILES:
CN1CCN(CC1)C(=O)Oc1n(-c2ccc(Cl)cn2)c(=O)c2ncc[nH]c12
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: