| Reaction Details |
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 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2 |
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| Ligand | BDBM50205615 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_435782 (CHEMBL904137) |
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| Ki | 2.6±n/a nM |
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| Citation |  Guerrini, G; Ciciani, G; Cambi, G; Bruni, F; Selleri, S; Besnard, F; Montali, M; Martini, C; Ghelardini, C; Galeotti, N; Costanzo, A Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage. Bioorg Med Chem15:2573-86 (2007) [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-1/beta-2/gamma-2 |
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| Name: | Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/gamma-2 |
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| Synonyms: | GABA receptor alpha-1/beta-2/gamma-2 subunit | GABA-A receptor; alpha-1/beta-2/gamma-2 | GABAA Subunit α1β2γ2 | GABAA Subunit alpha-1, beta-2, gamma-2 |
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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 69455 |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-2 |
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| Synonyms: | GBRB2_RAT | Gabrb-2 | Gabrb2 | Gamma-aminobutyric acid receptor subunit beta-2 (GABA(A) beta-2) |
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| Type: | Enzyme |
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| Mol. Mass.: | 54648.97 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P63138 |
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| Residue: | 474 |
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| Sequence: | MWRVRKRGYFGIWSFPLIIAAVCAQSVNDPSNMSLVKETVDRLLKGYDIRLRPDFGGPPV
AVGMNIDIASIDMVSEVNMDYTLTMYFQQAWRDKRLSYNVIPLNLTLDNRVADQLWVPDT
YFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIES
YGYTTDDIEFYWRGDDNAVTGVTKIELPQFSIVDYKLITKKVVFSTGSYPRLSLSFKLKR
NIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKIP
YVKAIDMYLMGCFVFVFMALLEYALVNYIFFGRGPQRQKKAAEKAANANNEKMRLDVNKM
DPHENILLSTLEIKNEMATSEAVMGLGDPRSTMLAYDASSIQYRKAGLPRHSFGRNALER
HVAQKKSRLRRRASQLKITIPDLTDVNAIDRWSRIFFPVVFSFFNIVYWLYYVN
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| Component 2 |
| Name: | Gamma-aminobutyric acid receptor subunit gamma-2 |
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| Synonyms: | GBRG2_RAT | Gabrg2 | Gamma-aminobutyric acid receptor subunit gamma-2 (GABA(A) gamma-2) |
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| Type: | Enzyme |
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| Mol. Mass.: | 54087.63 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P18508 |
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| Residue: | 466 |
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| Sequence: | MSSPNTWSTGSTVYSPVFSQKMTLWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPKV
PEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQTW
YDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLYT
LRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQFS
FVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDAV
PARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFVS
NRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCCF
EDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-1 |
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| Synonyms: | Benzodiazepine central | Benzodiazepine receptors | GABA A Benzodiazepine | GABA A Benzodiazepine Type I | GABA A Benzodiazepine Type II | GABA A Benzodiazepine Type IIL | GABA A Benzodiazepine Type IIM | GABA A Benzodiazepine omega1 | GABA A Benzodiazepine omega2 | GABA A Benzodiazepine omega5 | GABA A alpha1 | GABA A anti-Alpha1 | GABA receptor alpha-1 subunit | GABA, Chloride, TBOB | GABA-PICROTOXIN | GBRA1_RAT | Gabra-1 | Gabra1 | TBPS |
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| Type: | Enzyme |
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| Mol. Mass.: | 51770.21 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | P62813 |
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| Residue: | 455 |
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| Sequence: | MKKSRGLSDYLWAWTLILSTLSGRSYGQPSQDELKDNTTVFTRILDRLLDGYDNRLRPGL
GERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASKI
WTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHACP
LKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVMT
THFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISAR
NSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDPL
IKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKIDR
LSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
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| BDBM50205615 |
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| n/a |
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| Name | BDBM50205615 |
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| Synonyms: | 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine4-oxide | CHEMBL229145 |
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| Type | Small organic molecule |
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| Emp. Form. | C11H9IN4O2 |
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| Mol. Mass. | 356.1192 |
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| SMILES | CCOc1ccc2n[n+]([O-])c3c(I)cnn3c2c1 |
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| Structure | 
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