Target
5-hydroxytryptamine receptor 6
Ligand
BDBM78940
Substrate
n/a
Meas. Tech.
ChEMBL_1468777 (CHEMBL3414316)
IC50
4.7±n/a nM
Citation
 Kolaczkowski, MMarcinkowska, MBucki, ASniecikowska, JPawlowski, MKazek, GSiwek, AJastrzebska-Wiesek, MPartyka, AWasik, AWesolowska, AMierzejewski, PBienkowski, P Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia. Eur J Med Chem 92:221-35 (2015) [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:
BDBM78940
Synonyms:
METHIOTHEPIN | MLS000859918 | Methiothepin mesylate salt | SMR000326779 | cid_3039995 | mesylic acid;1-methyl-4-[3-(methylthio)-5,6-dihydrobenzo[b][1]benzothiepin-5-yl]piperazine | methanesulfonic acid;1-methyl-4-(3-methylsulfanyl-5,6-dihydrobenzo[b][1]benzothiepin-5-yl)piperazine | methanesulfonic acid;1-methyl-4-[3-(methylthio)-5,6-dihydrobenzo[b][1]benzothiepin-5-yl]piperazine
Type:
Small organic molecule
Emp. Form.:
C20H24N2S2
Mol. Mass.:
356.548
SMILES:
CSc1ccc2Sc3ccccc3CC(N3CCN(C)CC3)c2c1
Structure:
Search PDB for entries with ligand similarity: