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Target5-hydroxytryptamine receptor 6
LigandBDBM34159
Substrate/CompetitorBDBM21342
Meas. Tech.5-HT6 Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki 43±n/a nM
IC50 3000±n/a nM
Comments78% inhibition @ 100 nM.
Citation Alcalde, EMesquida, NLópez-Pérez, SFrigola, JMercè, RHolenz, JPujol, MHernández, E Indene-based frameworks targeting the 5-HT6 serotonin receptor: ring constraint in indenylsulfonamides using cyclic amines and structurally abbreviated counterparts. Bioorg Med Chem17:7387-97 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
5-hydroxytryptamine receptor 6
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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  Blast E-value cutoff:
BDBM34159
BDBM21342
NameBDBM34159
Synonyms:indenylsulfonamide, 47+48 | isomeric mixture (70% 5-indenyl, 30% 6-indenyl)
TypeSmall organic molecule
Emp. Form.C15H12ClN3O2S2
Mol. Mass.365.858
SMILESCC1=Cc2cc(NS(=O)(=O)c3c(Cl)nc4sccn34)ccc2C1 |t:1|
Structure
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