Target
5-hydroxytryptamine receptor 2B
Ligand
BDBM50342545
Substrate
n/a
Meas. Tech.
ChEMBL_744733 (CHEMBL1772754)
EC50
178±n/a nM
Citation
 Andrews, MDFish, PVBlagg, JBrabham, TKBrennan, PEBridgeland, ABrown, ADBungay, PJConlon, KMEdmunds, NJaf Forselles, KGibbons, CPGreen, MPHanton, GHolbrook, MJessiman, ASMcIntosh, KMcMurray, GNichols, CLRoot, JAStorer, RISutton, MRWard, RVWestbrook, DWhitlock, GA Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Bioorg Med Chem Lett 21:2715-20 (2011) [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:
BDBM50342545
Synonyms:
2-(2-chlorobenzyl)-6,7,8,9-tetrahydro-5H-pyrimido[5,4-d]azepine | CHEMBL1770381
Type:
Small organic molecule
Emp. Form.:
C15H16ClN3
Mol. Mass.:
273.761
SMILES:
Clc1ccccc1Cc1ncc2CCNCCc2n1
Structure:
Search PDB for entries with ligand similarity: