Reaction Details |
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Target | Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2 |
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Ligand | BDBM50065229 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_217130 (CHEMBL822162) |
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Ki | 5.7±n/a nM |
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Citation | Cox, ED; Diaz-Arauzo, H; Huang, Q; Reddy, MS; Ma, C; Harris, B; McKernan, R; Skolnick, P; Cook, JM Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors J Med Chem41:2537-52 (1998) [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-3/gamma-2 |
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Name: | Gamma-aminobutyric acid receptor subunit alpha-1/beta-3/gamma-2 |
Synonyms: | GABA receptor alpha-1/beta-3/gamma-2 subunit | GABA-A receptor; alpha-1/beta-3/gamma-2 | GABAA alpha1beta3gamma2 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 3 components. |
Component 1 |
Name: | Gamma-aminobutyric acid receptor subunit alpha-1 |
Synonyms: | Benzodiazepine central | GABA A Benzodiazepine brain | GABA A Benzodiazepine liver | GABA receptor alpha-1 subunit | GABA(A) receptor subunit alpha-1 | GABA-A | GABA-A receptor | GABRA1 | GBRA1_HUMAN | Gamma-aminobutyric acid receptor subunit alpha (GABAA) | TBPS | agonist GABA site |
Type: | Protein |
Mol. Mass.: | 51817.35 |
Organism: | Homo sapiens (Human) |
Description: | P14867 |
Residue: | 456 |
Sequence: | MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
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Component 2 |
Name: | Gamma-aminobutyric acid receptor subunit beta-3 |
Synonyms: | GABA A receptor alpha-4/beta-3/gamma-2 | GABA receptor beta-3 subunit | GABA-A receptor | GABRB3 | GBRB3_HUMAN | agonist GABA site |
Type: | PROTEIN |
Mol. Mass.: | 54130.51 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_448071 |
Residue: | 473 |
Sequence: | MWGLAGGRLFGIFSAPVLVAVVCCAQSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPP
VCVGMNIDIASIDMVSEVNMDYTLTMYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPD
TYFLNDKKSFVHGVTVKNRMIRLHPDGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIE
SYGYTTDDIEFYWRGGDKAVTGVERIELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLK
RNIGYFILQTYMPSILITILSWVSFWINYDASAARVALGITTVLTMTTINTHLRETLPKI
PYVKAIDMYLMGCFVFVFLALLEYAFVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNR
VDAHGNILLTSLEVHNEMNEVSGGIGDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRS
LPHKKTHLRRRSSQLKIKIPDLTDVNAIDRWSRIVFPFTFSLFNLVYWLYYVN
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Component 3 |
Name: | Gamma-aminobutyric acid receptor subunit gamma-2 |
Synonyms: | GABA(A) receptor subunit gamma-2 | GABRG2 | GBRG2_HUMAN |
Type: | PROTEIN |
Mol. Mass.: | 54172.74 |
Organism: | Homo sapiens (Human) |
Description: | EBI_217 |
Residue: | 467 |
Sequence: | MSSPNIWSTGSSVYSTPVFSQKMTVWILLLLSLYPGFTSQKSDDDYEDYASNKTWVLTPK
VPEGDVTVILNNLLEGYDNKLRPDIGVKPTLIHTDMYVNSIGPVNAINMEYTIDIFFAQT
WYDRRLKFNSTIKVLRLNSNMVGKIWIPDTFFRNSKKADAHWITTPNRMLRIWNDGRVLY
TLRLTIDAECQLQLHNFPMDEHSCPLEFSSYGYPREEIVYQWKRSSVEVGDTRSWRLYQF
SFVGLRNTTEVVKTTSGDYVVMSVYFDLSRRMGYFTIQTYIPCTLIVVLSWVSFWINKDA
VPARTSLGITTVLTMTTLSTIARKSLPKVSYVTAMDLFVSVCFIFVFSALVEYGTLHYFV
SNRKPSKDKDKKKKNPAPTIDIRPRSATIQMNNATHLQERDEEYGYECLDGKDCASFFCC
FEDCRTGAWRHGRIHIRIAKMDSYARIFFPTAFCLFNLVYWVSYLYL
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BDBM50065229 |
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n/a |
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Name | BDBM50065229 |
Synonyms: | 4-Ethyl-6,7-dimethoxy-9H-beta-carboline-3-carboxylic acid methyl ester | 4-Ethyl-6,7-dimethoxy-9H-beta-carboline-3-carboxylic acid methyl ester(DMCM) | 4-Ethyl-6,7-dimethoxy-9H-carbazole-3-carboxylic acid methyl ester | CHEMBL17468 |
Type | Small organic molecule |
Emp. Form. | C17H18N2O4 |
Mol. Mass. | 314.3358 |
SMILES | CCc1c([nH]cc2nc3cc(OC)c(OC)cc3c12)C(=O)OC |
Structure |
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