| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2 |
|---|
| Ligand | BDBM50185505 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_373310 (CHEMBL853517) |
|---|
| Ki | 2.7±n/a nM |
|---|
| Citation |  Carling, RW; Russell, MG; Moore, KW; Mitchinson, A; Guiblin, A; Smith, A; Wafford, KA; Marshall, G; Atack, JR; Street, LJ 2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists. Bioorg Med Chem Lett16:3550-4 (2006) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2 |
|---|
| Name: | Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/gamma-2 |
|---|
| Synonyms: | GABA receptor alpha-3/beta-3/gamma-2 subunit | GABA-A receptor; alpha-3/beta-3/gamma-2 |
|---|
| Type: | n/a |
|---|
| Mol. Mass.: | n/a |
|---|
| Description: | ASSAY_ID of EBI is 68410 |
|---|
| Components: | This complex has 3 components. |
|---|
| Component 1 |
| 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
|
|
|
|---|
| 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
|
|
|
|---|
| Component 3 |
| Name: | Gamma-aminobutyric acid receptor subunit alpha-3 |
|---|
| 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 |
|---|
| Type: | Enzyme Catalytic Domain |
|---|
| Mol. Mass.: | 55175.47 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | GABA A Alpha3Beta1Gamma2 0 HUMAN::P34903 |
|---|
| Residue: | 492 |
|---|
| Sequence: | MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDS
TDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQ
TWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLL
YTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRL
NQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLN
RESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVN
YFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGA
APSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVN
RESAIKGMIRKQ
|
|
|
|---|
| BDBM50185505 |
|---|
| n/a |
|---|
| Name | BDBM50185505 |
|---|
| Synonyms: | 3-(2-fluoro-phenyl)-2-(2-methyl-2H-[1,2,4]triazol-3-ylmethoxy)-7-pyrazin-1-yl-pyrazolo[1,5-d][1,2,4]triazine | CHEMBL212637 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C19H15FN9O |
|---|
| Mol. Mass. | 404.38 |
|---|
| SMILES | Cn1ncnc1COc1nn2c(nncc2c1-c1ccccc1F)-[n+]1ccncc1 |(19.11,-18.43,;17.59,-18.21,;16.52,-19.32,;15.14,-18.64,;15.35,-17.11,;16.88,-16.84,;17.65,-15.51,;16.89,-14.18,;17.66,-12.84,;19.2,-12.69,;19.53,-11.18,;20.87,-10.41,;20.86,-8.86,;19.52,-8.09,;18.2,-8.86,;18.19,-10.4,;17.04,-11.43,;15.7,-10.67,;15.71,-9.13,;14.38,-8.37,;13.04,-9.14,;13.05,-10.69,;14.39,-11.45,;14.4,-12.99,;22.2,-11.18,;22.2,-12.72,;23.53,-13.49,;24.87,-12.72,;24.86,-11.17,;23.53,-10.4,)| |
|---|
| Structure | 
|
|---|
Search and Browse
