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Target
5-hydroxytryptamine receptor 2B
Ligand
BDBM50086055
Substrate
n/a
Meas. Tech.
ChEMBL_2877 (CHEMBL617780)
Ki
10±n/a nM
Citation
 Bromidge, SM; Dabbs, S; Davies, DT; Davies, S; Duckworth, DM; Forbes, IT; Gaster, LM; Ham, P; Jones, GE; King, FD; Mulholland, KR; Saunders, DV; Wyman, PA; Blaney, FE; Clarke, SE; Blackburn, TP; Holland, V; Kennett, GA; Lightowler, S; Middlemiss, DN; Trail, B; Riley, GJ; Wood, MD Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem 43:1123-34 (2000) [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:
BDBM50086055
Synonyms:
5-Methoxy-6-trifluoromethyl-2,3-dihydro-indole-1-carboxylic acid (3-ethyl-5-pyridin-3-yl-phenyl)-amide | CHEMBL416896
Type:
Small organic molecule
Emp. Form.:
C24H22F3N3O2
Mol. Mass.:
441.4456
SMILES:
CCc1cc(NC(=O)N2CCc3cc(OC)c(cc23)C(F)(F)F)cc(c1)-c1cccnc1
Structure:
Search PDB for entries with ligand similarity: