| Reaction Details |
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 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2 |
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| Ligand | BDBM50459889 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1767455 (CHEMBL4219567) |
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| EC50 | 17700±n/a nM |
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| Citation |  Sparling, BA; DiMauro, EF Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors. Bioorg Med Chem Lett27:3207-3218 (2017) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Gamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2 |
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| Name: | Gamma-aminobutyric acid receptor subunit alpha-3/beta-2/gamma-2 |
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| Synonyms: | GABA A receptor alpha-3/beta-2/gamma-2 | GABA receptor alpha-3/beta-2/gamma-2 subunit |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of EBI is 69791 |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Gamma-aminobutyric acid receptor subunit gamma-2 |
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| Synonyms: | GABA(A) receptor subunit gamma-2 | GABRG2 | GBRG2_HUMAN |
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| Type: | PROTEIN |
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| Mol. Mass.: | 54172.74 |
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| Organism: | Homo sapiens (Human) |
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| Description: | EBI_217 |
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| Residue: | 467 |
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| Sequence: | MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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| Component 2 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-2 |
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| Synonyms: | GABA(A) receptor subunit beta-2 | GABRB2 | GBRB2_HUMAN |
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| Type: | PROTEIN |
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| Mol. Mass.: | 59167.91 |
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| Organism: | Homo sapiens (Human) |
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| Description: | EBI_221 |
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| Residue: | 512 |
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| Sequence: | MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKI
FYKDIKQNGTQYRSLWDPTGNLSPTRRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEA
VMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPD
LTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
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| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-3 |
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| Synonyms: | GABA A Alpha3Beta3Gamma2 | GABA A receptor alpha-3/beta-2/gamma-2 | GABA C | GABA receptor alpha-3 subunit | GABA-A receptor | GABRA3 | GBRA3_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-3 | agonist GABA site |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 55175.47 |
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| Organism: | Homo sapiens (Human) |
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| Description: | GABA A Alpha3Beta1Gamma2 0 HUMAN::P34903 |
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| Residue: | 492 |
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| Sequence: | MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
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| Component 4 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-2 |
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| Synonyms: | GABA(A) receptor subunit beta-2 | GABRB2 | GBRB2_HUMAN |
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| Type: | PROTEIN |
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| Mol. Mass.: | 59167.91 |
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| Organism: | Homo sapiens (Human) |
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| Description: | EBI_221 |
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| Residue: | 512 |
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| Sequence: | MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAASANNEKMRLDVNKI
FYKDIKQNGTQYRSLWDPTGNLSPTRRTTNYDFSLYTMDPHENILLSTLEIKNEMATSEA
VMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALERHVAQKKSRLRRRASQLKITIPD
LTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
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| BDBM50459889 |
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| n/a |
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| Name | BDBM50459889 |
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| Synonyms: | CHEMBL4224740 |
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| Type | Small organic molecule |
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| Emp. Form. | C17H16O4 |
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| Mol. Mass. | 284.3065 |
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| SMILES | COc1ccc(cc1)C(=O)\C=C\c1cc(OC)ccc1O |
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| Structure | 
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