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TargetGamma-aminobutyric acid receptor subunit alpha-1 [F99C]/beta-2 [26-512]/gamma-2 [40-467]
LigandBDBM26265
Substrate/CompetitorBDBM26263
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature295.15±n/a K
Ki 407±123 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 Chem51:7243-52 (2008) [PubMed]  Article
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Gamma-aminobutyric acid receptor subunit alpha-1 [F99C]/beta-2 [26-512]/gamma-2 [40-467]
Name:Gamma-aminobutyric acid receptor subunit alpha-1 [F99C]/beta-2 [26-512]/gamma-2 [40-467]
Synonyms:GABAA Receptor Mutant, alpha-1 (F99C), 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:
QKSDDDYEDYASNKTWVLTPKVPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVN
SIGPVNAINMEYTIDIFFAQTWYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKAD
AHWITTPNRMLRIWNDGRVLYTLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIV
YQWKRSSVEVGDTRSWRLYQFSFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQT
YIPCTLIVVLSWVSFWINKDAVPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFV
SVCFIFVFSALVEYGTLHYFVSNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQE
RDEEYGYECLDGKDCASFFCCFEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLV
YWVSYLYL
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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:
SVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPVAVGMNIDIASIDMVSEVNMDYTLTM
YFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHPD
GTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGDDNAVTGVTKI
ELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKRNIGYFILQTYMPSILITILSWVSFW
INYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFMALLEYAL
VNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKIFYKDIKQNGTQYRSLWDPTGNLSPT
RRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAG
LPRHSFGRNALERHVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIV
YWLYYVN
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Component 3
Name:Gamma-aminobutyric acid receptor subunit alpha-1 [F99C]
Synonyms:GABA(A) receptor subunit alpha-1 benzodiazepine binding site loop A mutant | GABAA Receptor Subunit alpha-1 Mutant (F99C) | GABRA1 | GBRA1_HUMAN
Type:Ionic channel
Mol. Mass.:48763.78
Organism:Homo sapiens (Human)
Description:P14867[F99C]
Residue:429
Sequence:
QPSLQDELKDNTTVFTRILDRLLDGYDNRLRPGLGERVTEVKTDIFVTSFGPVSDHDMEY
TIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKIWTPDTCFHNGKKSVAHNMTMPNKLLR
ITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACPLKFGSYAYTRAEVVYEWTREPARSVV
VAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVIL
SQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSA
LIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPLIKKNNTYAPTATSYTPNLARGDPGLA
TIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDRLSRIAFPLLFGIFNLVYWATYLNREP
QLKAPTPHQ
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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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