Target
5-hydroxytryptamine receptor 2B
Ligand
BDBM50249130
Substrate
n/a
Meas. Tech.
ChEMBL_499777 (CHEMBL968750)
IC50
6±n/a nM
Citation
 Moss, NChoi, YCogan, DFlegg, AKahrs, ALoke, PMeyn, ONagaraja, RNapier, SParker, AThomas Peterson, JRamsden, PSarko, CSkow, DTomlinson, JTye, HWhitaker, M A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties. Bioorg Med Chem Lett 19:2206-10 (2009) [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:
BDBM50249130
Synonyms:
(4-(1H-benzo[d]imidazol-2-yl)piperidin-1-yl)(4-ethoxy-2-phenylpyrimidin-5-yl)methanone | CHEMBL514453
Type:
Small organic molecule
Emp. Form.:
C25H25N5O2
Mol. Mass.:
427.4983
SMILES:
CCOc1nc(ncc1C(=O)N1CCC(CC1)c1nc2ccccc2[nH]1)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: