| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-5 [32-462]/beta-3 [26-473]/gamma-2 [40-467] |
|---|
| Ligand | BDBM25877 |
|---|
| Substrate/Competitor | BDBM25878 |
|---|
| Meas. Tech. | Radioligand Binding Assay |
|---|
| Ki | 0.49±n/a nM |
|---|
| Citation |  Han, D; Holger Försterling, F; Li, X; Deschamps, JR; Parrish, D; Cao, H; Rallapalli, S; Clayton, T; Teng, Y; Majumder, S; Sankar, S; Roth, BL; Sieghart, W; Furtmuller, R; Rowlett, JK; Weed, MR; Cook, JM A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis. Bioorg Med Chem16:8853-62 (2008) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Solution Info, Assay Method |
|---|
| |
| Gamma-aminobutyric acid receptor subunit alpha-5 [32-462]/beta-3 [26-473]/gamma-2 [40-467] |
|---|
| Name: | Gamma-aminobutyric acid receptor subunit alpha-5 [32-462]/beta-3 [26-473]/gamma-2 [40-467] |
|---|
| Synonyms: | GABAA Receptor, alpha-5, beta-3, gamma-2 |
|---|
| Type: | Protein Complex |
|---|
| Mol. Mass.: | n/a |
|---|
| Description: | Cell membranes from HEK cells transfected with GABAA beta-3, gamma-2, and alpha-5 were used in binding assays. |
|---|
| 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
|
|
|
|---|
| Component 2 |
| Name: | Gamma-aminobutyric acid receptor subunit beta-3 [26-473] |
|---|
| Synonyms: | GABA(A) receptor subunit beta-3 | GABAA Receptor Subunit beta-3 | GABRB3 | GBRB3_HUMAN | Gamma-aminobutyric acid receptor subunit beta-3 |
|---|
| Type: | Ionic channel |
|---|
| Mol. Mass.: | 51609.41 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P28472[26-473] |
|---|
| Residue: | 448 |
|---|
| Sequence: | QSVNDPGNMSFVKETVDKLLKGYDIRLRPDFGGPPVCVGMNIDIASIDMVSEVNMDYTLT
MYFQQYWRDKRLAYSGIPLNLTLDNRVADQLWVPDTYFLNDKKSFVHGVTVKNRMIRLHP
DGTVLYGLRITTTAACMMDLRRYPLDEQNCTLEIESYGYTTDDIEFYWRGGDKAVTGVER
IELPQFSIVEHRLVSRNVVFATGAYPRLSLSFRLKRNIGYFILQTYMPSILITILSWVSF
WINYDASAARVALGITTVLTMTTINTHLRETLPKIPYVKAIDMYLMGCFVFVFLALLEYA
FVNYIFFGRGPQRQKKLAEKTAKAKNDRSKSESNRVDAHGNILLTSLEVHNEMNEVSGGI
GDTRNSAISFDNSGIQYRKQSMPREGHGRFLGDRSLPHKKTHLRRRSSQLKIKIPDLTDV
NAIDRWSRIVFPFTFSLFNLVYWLYYVN
|
|
|
|---|
| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-5 [32-462] |
|---|
| Synonyms: | GABA(A) receptor subunit alpha-5 | GABAA Receptor Subunit alpha-5 | GABRA5 | GBRA5_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-5 |
|---|
| Type: | Ionic channel |
|---|
| Mol. Mass.: | 48674.94 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P31644[32-462] |
|---|
| Residue: | 431 |
|---|
| Sequence: | QMPTSSVKDETNDNITIFTRILDGLLDGYDNRLRPGLGERITQVRTDIYVTSFGPVSDTE
MEYTIDVFFRQSWKDERLRFKGPMQRLPLNNLLASKIWTPDTFFHNGKKSIAHNMTTPNK
LLRLEDDGTLLYTMRLTISAECPMQLEDFPMDAHACPLKFGSYAYPNSEVVYVWTNGSTK
SVVVAEDGSRLNQYHLMGQTVGTENISTSTGEYTIMTAHFHLKRKIGYFVIQTYLPCIMT
VILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFV
FSALIEFATVNYFTKRGWAWDGKKALEAAKIKKKREVILNKSTNAFTTGKMSHPPNIPKE
QTPAGTSNTTSVSVKPSEEKTSESKKTYNSISKIDKMSRIVFPVLFGTFNLVYWATYLNR
EPVIKGAASPK
|
|
|
|---|
| BDBM25877 |
|---|
| BDBM25878 |
|---|
| Name | BDBM25877 |
|---|
| Synonyms: | CHEMBL286594 | RY-80, 1 | ethyl 12-ethynyl-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(14),3,5,10,12-pentaene-5-carboxylate |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C17H15N3O3 |
|---|
| Mol. Mass. | 309.3193 |
|---|
| SMILES | CCOC(=O)c1ncn-2c1CN(C)C(=O)c1cc(ccc-21)C#C |
|---|
| Structure | 
|
|---|
Search and Browse
