Reaction Details |
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Target | 5-hydroxytryptamine receptor 6 |
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Ligand | BDBM21357 |
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Substrate/Competitor | BDBM21342 |
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Meas. Tech. | Radioligand Labeled Binding Assay and cAMP Production |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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Ki | 10±1 nM |
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EC50 | 9.6±1 nM |
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Comments | Antagonism of 5-HT stimulated cAMP production. |
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Citation | Cole, DC; Stock, JR; Lennox, WJ; Bernotas, RC; Ellingboe, JW; Boikess, S; Coupet, J; Smith, DL; Leung, L; Zhang, GM; Feng, X; Kelly, MF; Galante, R; Huang, P; Dawson, LA; Marquis, K; Rosenzweig-Lipson, S; Beyer, CE; Schechter, LE Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist. J Med Chem50:5535-8 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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5-hydroxytryptamine receptor 6 |
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Name: | 5-hydroxytryptamine receptor 6 |
Synonyms: | 5-HT-6 | 5-HT6 | 5-hydroxytryptamine receptor 6 (5-HT-6) | 5-hydroxytryptamine receptor 6 (5-HT6R) | 5-hydroxytryptamine receptor 6 (5HT6) | 5HT6R_HUMAN | HTR6 | Serotonin (5-HT3) receptor | Serotonin 6 (5-HT6) receptor | Serotonin Receptor 6 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 46968.43 |
Organism: | Homo sapiens (Human) |
Description: | P50406 |
Residue: | 440 |
Sequence: | MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNT
SNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLI
SLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQC
RLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVP
RTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPG
LFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGP
RPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNF
FNIDPAEPELRPHPLGIPTN
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BDBM21357 |
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BDBM21342 |
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Name | BDBM21357 |
Synonyms: | 5-thiazolylsulfonyl tryptamine, 11p | 5-{[3-(2-aminoethyl)-1H-indole-1-]sulfonyl}-4-methyl-1,3-thiazol-2-amine |
Type | Small organic molecule |
Emp. Form. | C14H16N4O2S2 |
Mol. Mass. | 336.432 |
SMILES | Cc1nc(N)sc1S(=O)(=O)n1cc(CCN)c2ccccc12 |
Structure |
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