Reaction Details |
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Target | Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-200],P14867[176-456] |
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Ligand | BDBM26265 |
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Substrate/Competitor | BDBM26263 |
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Meas. Tech. | Radioligand Binding Assay |
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Temperature | 298.15±n/a K |
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Ki | 22.4±n/a nM |
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Comments | extracted |
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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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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Gamma-aminobutyric acid receptor subunit alpha-1 [28-456]/beta-2 [26-512]/gamma-2 [40-200],P14867[176-456] |
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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 |
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BDBM26263 |
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Name | BDBM26265 |
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 |
Type | Small organic molecule |
Emp. Form. | C17H17ClN6O3 |
Mol. Mass. | 388.808 |
SMILES | CN1CCN(CC1)C(=O)Oc1n(-c2ccc(Cl)cn2)c(=O)c2ncc[nH]c12 |
Structure |
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