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Target
5-hydroxytryptamine receptor 2B
Ligand
BDBM35247
Substrate
BDBM10755
Meas. Tech.
Norepinephrine Uptake Assay (IC50)
Citation
Heffernan, GD; Coghlan, RD; Manas, ES; McDevitt, RE; Li, Y; Mahaney, PE; Robichaud, AJ; Huselton, C; Alfinito, P; Bray, JA; Cosmi, SA; Johnston, GH; Kenney, T; Koury, E; Winneker, RC; Deecher, DC; Trybulski, EJ Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles. Bioorg Med Chem 17:7802-15 (2009) [PubMed] Article
More Info.:
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:
BDBM35247
Synonyms:
3-(phenylsulfonyl)-1H-indole, 18i
Type:
Small organic molecule
Emp. Form.:
C21H24N2O2S
Mol. Mass.:
368.492
SMILES:
O=S(=O)(c1c[nH]c2cccc(CCN3CCCCC3)c12)c1ccccc1
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