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Target
5-hydroxytryptamine receptor 2B
Ligand
BDBM21358
Substrate
BDBM10755
Meas. Tech.
Radioligand Labeled Binding Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
458±n/a nM
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 2B
Synonyms:
5-HT-2B | 5-HT2B | 5-hydroxytryptamine (serotonin) receptor 2B [Homo sapiens] | 5-hydroxytryptamine receptor 2B (5-HT2B) | 5-hydroxytryptamine receptor 2C (5HT2C) | 5HT2B_HUMAN | HTR2B | Serotonin (5-HT3) receptor | Serotonin 2b (5-HT2b) receptor | Serotonin Receptor 2B
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
54312.47
Organism:
Homo sapiens (Human)
Description:
Receptor binding assays were performed using human clone stably expressed in CHO cells.
Residue:
481
Sequence:
MALSYRVSELQSTIPEHILQSTFVHVISSNWSGLQTESIPEEMKQIVEEQGNKLHWAALLILMVIIPTIGGNTLVILAVSLEKKLQYATNYFLMSLAVADLLVGLFVMPIALLTIMFEAMWPLPLVLCPAWLFLDVLFSTASIMHLCAISVDRYIAIKKPIQANQYNSRATAFIKITVVWLISIGIAIPVPIKGIETDVDNPNNITCVLTKERFGDFMLFGSLAAFFTPLAIMIVTYFLTIHALQKKAYLVKNKPPQRLTWLTVSTVFQRDETPCSSPEKVAMLDGSRKDKALPNSGDETLMRRTSTIGKKSVQTISNEQRASKVLGIVFFLFLLMWCPFFITNITLVLCDSCNQTTLQMLLEIFVWIGYVSSGVNPLVYTLFNKTFRDAFGRYITCNYRATKSVKTLRKRSSKIYFRNPMAENSKFFKKHGIRNGINPAMYQSPMRLRSSTIQSSSIILLDTLLLTENEGDKTEEQVSYV
  
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:
BDBM10755
Synonyms:
14C-5-hydroxy tryptamine creatinine disulfate | 2-imino-1-methylimidazolidin-4-one; 3-(2-aminoethyl)-1H-indol-5-ol; bis(sulfuric acid) | 5-HT | 5-Hydroxy Tryptamine | 5-hydroxy tryptamine creatinine disulfate | CHEMBL535832 | Serotonin | [3H]-5-HT
Type:
Small organic molecule
Emp. Form.:
C10H12N2O
Mol. Mass.:
176.2151
SMILES:
NCCc1c[nH]c2ccc(O)cc12
Structure:
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