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TargetGamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-200],P14867[176-456]
LigandBDBM26265
Substrate/CompetitorBDBM26263
Meas. Tech.Radioligand Binding Assay
Temperature298.15±n/a K
Ki 22.4±n/a nM
Commentsextracted
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 Chem51:7243-52 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-200],P14867[176-456]
Name:Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-200],P14867[176-456]
Synonyms:GABAA Receptor Mutant, alpha-1, beta-2, gamma-2 (Chimera)
Type:Protein Complex
Mol. Mass.:n/a
Description:It is expressed with WT alpha-1, beta-2, and a chimeric subunit containing residues up to gamma-2 amino acid 161, and alpha-1 residues C-terminal to 161.
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:
SVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTM
YFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPD
GTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKI
ELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFW
INYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYAL
VNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKIFYKDIKQNGTQYRSLWDPTGNLSPT
RRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAG
LPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIV
YWLYYVN
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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:
QPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEY
TIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTFFHNGKKSVAHNMTMPNKLLR
ITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVV
VAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVIL
SQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSA
LIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLA
TIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREP
QLKAPTPHQ
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Component 3
Name:Gamma-aminobutyric acid receptor subunit gamma-2 [40-200],P14867[176-456]
Synonyms:Complex of Gamma-aminobutyric acid receptor subunit gamma-2 [40-200] and Gamma-aminobutyric acid receptor subunit alpha-1 [176-456] | GABA(A) receptor chimeric subunit gamma-2/alpha-1 | GABA(A) receptor subunit gamma-2 mutant (gamma-2 D161/alpha-1 A149) | GABAA Receptor Subunit gamma-2 Mutant (Chimera)
Type:Ionic channel
Mol. Mass.:50363.91
Organism:Homo sapiens (Human)
Description:P18507[40-200],P14867[176-456]
Residue:442
Sequence:
QKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVN
SIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKAD
AHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDDAHACPLKFGSYAYTRAEV
VYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFV
IQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMD
WFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATS
YTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIF
NLVYWATYLNREPQLKAPTPHQ
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BDBM26265
BDBM26263
NameBDBM26265
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
TypeSmall organic molecule
Emp. Form.C17H17ClN6O3
Mol. Mass.388.808
SMILESCN1CCN(CC1)C(=O)Oc1n(-c2ccc(Cl)cn2)c(=O)c2ncc[nH]c12
Structure
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