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Target
5-hydroxytryptamine receptor 2C
Ligand
BDBM50161638
Substrate
n/a
Meas. Tech.
ChEMBL_460519 (CHEMBL926599)
EC50
7.9±n/a nM
Citation
Smith, BM; Smith, JM; Tsai, JH; Schultz, JA; Gilson, CA; Estrada, SA; Chen, RR; Park, DM; Prieto, EB; Gallardo, CS; Sengupta, D; Dosa, PI; Covel, JA; Ren, A; Webb, RR; Beeley, NR; Martin, M; Morgan, M; Espitia, S; Saldana, HR; Bjenning, C; Whelan, KT; Grottick, AJ; Menzaghi, F; Thomsen, WJ Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. J Med Chem 51:305-13 (2008) [PubMed] Article
More Info.:
Target
Name:
5-hydroxytryptamine receptor 2C
Synonyms:
5-HT-1C | 5-HT-2C | 5-HT1C | 5-HT2C | 5-HT2C-INI | 5-HT2c VGI | 5-HTR2C | 5-hydroxytryptamine receptor 1C | 5-hydroxytryptamine receptor 2C (5-HT-2C) | 5-hydroxytryptamine receptor 2C (5HT-2C) | 5HT-1C | 5HT2C_HUMAN | HTR1C | HTR2C | Serotonin (5-HT3) receptor | Serotonin 2c (5-HT2c) receptor | Serotonin Receptor 2C
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
51836.79
Organism:
Homo sapiens (Human)
Description:
P28335
Residue:
458
Sequence:
MVNLRNAVHSFLVHLIGLLVWQSDISVSPVAAIVTDIFNTSDGGRFKFPDGVQNWPALSIVIIIIMTIGGNILVIMAVSMEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVWPLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPIEHSRFNSRTKAIMKIAIVWAISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIYVLRRQALMLLHGHTEEPPGLSLDFLKCCKRNTAEEENSANPNQDQNARRRKKKERRPRGTMQAINNERKASKVLGIVFFVFLIMWCPFFITNILSVLCEKSCNQKLMEKLLNVFVWIGYVCSGINPLVYTLFNKIYRRAFSNYLRCNYKVEKKPPVRQIPRVAATALSGRELNVNIYRHTNEPVIEKASDNEPGIEMQVENLELPVNPSSVVSERISSV
Inhibitor
Name:
BDBM50161638
Synonyms:
(1R,S)-8-chloro-7-methoxy-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine | 8-Chloro-7-methoxy-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine | CHEMBL181787
Type:
Small organic molecule
Emp. Form.:
C12H16ClNO
Mol. Mass.:
225.715
SMILES:
COc1cc2CCNCC(C)c2cc1Cl