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Target
5-hydroxytryptamine receptor 6
Ligand
BDBM21358
Substrate
BDBM21342
Meas. Tech.
Radioligand Labeled Binding Assay and cAMP Production
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
2±0 nM
EC50
6.5±0.5 nM
Comments
Agonism of cAMP production.
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 Chem 50:5535-8 (2007) [PubMed]  Article 
Target
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:
MVPEPGPTANSTPAWGAGPPSAPGGSGWVAAALCVVIALTAAANSLLIALICTQPALRNTSNFFLVSLFTSDLMVGLVVMPPAMLNALYGRWVLARGLCLLWTAFDVMCCSASILNLCLISLDRYLLILSPLRYKLRMTPLRALALVLGAWSLAALASFLPLLLGWHELGHARPPVPGQCRLLASLPFVLVASGLTFFLPSGAICFTYCRILLAARKQAVQVASLTTGMASQASETLQVPRTPRPGVESADSRRLATKHSRKALKASLTLGILLGMFFVTWLPFFVANIVQAVCDCISPGLFDVLTWLGYCNSTMNPIIYPLFMRDFKRALGRFLPCPRCPRERQASLASPSLRTSHSGPRPGLSLQQVLPLPLPPDSDSDSDAGSGGSSGLRLTAQLLLPGEATQDPPLPTRAAAAVNFFNIDPAEPELRPHPLGIPTN
  
Inhibitor
Name:
BDBM21358
Synonyms:
2-[1-({6-chloroimidazo[2,1-b][1,3]thiazole-5-}sulfonyl)-1H-indol-3-yl]ethan-1-amine | N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine | SAX-187 | WAY-181187
Type:
Small organic molecule
Emp. Form.:
C15H13ClN4O2S2
Mol. Mass.:
380.872
SMILES:
NCCc1cn(c2ccccc12)S(=O)(=O)c1c(Cl)nc2sccn12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM21342
Synonyms:
(4R,7R)-N,N-diethyl-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide | CHEMBL263881 | LSD | LSD 25 | LSD,(+) | LSD,l- | Lysergic Acid Diethylamide | Lysergic Acid Diethylamide Tartrate | [3H]-LSD | d-Isolysergic acid amide
Type:
radiolabeled ligand
Emp. Form.:
C20H25N3O
Mol. Mass.:
323.432
SMILES:
[H][C@@]12Cc3c[nH]c4cccc(C1=C[C@H](CN2C)C(=O)N(CC)CC)c34 |c:12|
Structure:
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