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Target
5-hydroxytryptamine receptor 2B
Ligand
BDBM473021
Substrate
n/a
Meas. Tech.
ChEMBL_2059288 (CHEMBL4714289)
Ki
251±n/a nM
Citation
 Schrader, TO; Zhu, X; Kasem, M; Ren, A; Liu, C; Wu, C; Dang, H; Le, M; Gatlin, J; Chase, K; Frazer, J; Whelan, KT; Grottick, AJ; Hutton, C; Barden, J; Chen, C; Ortiz, A; Feichtinger, K; Semple, G Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT Bioorg Med Chem Lett 38:0 (2021) [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:
BDBM473021
Synonyms:
(R)-4-benzyl-6,6a,7,8,9,10-hexahydro-5H- pyrazino[1,2-a][1,7]naphthyridine | US10836764, Compound 175
Type:
Small organic molecule
Emp. Form.:
C18H21N3
Mol. Mass.:
279.3794
SMILES:
C(c1ccccc1)c1cncc2N3CCNC[C@H]3CCc12 |r|
Structure:
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