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Target
5-hydroxytryptamine receptor 2C
Ligand
BDBM50161646
Substrate
n/a
Meas. Tech.
ChEMBL_744732 (CHEMBL1772753)
Ki
167±n/a nM
Citation
Andrews, MD; Fish, PV; Blagg, J; Brabham, TK; Brennan, PE; Bridgeland, A; Brown, AD; Bungay, PJ; Conlon, KM; Edmunds, NJ; af Forselles, K; Gibbons, CP; Green, MP; Hanton, G; Holbrook, M; Jessiman, AS; McIntosh, K; McMurray, G; Nichols, CL; Root, JA; Storer, RI; Sutton, MR; Ward, RV; Westbrook, D; Whitlock, 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
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:
BDBM50161646
Synonyms:
(1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine | (R)-8-Chloro-1-methyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine | CHEMBL360328 | LORCASERIN
Type:
Small organic molecule
Emp. Form.:
C11H14ClN
Mol. Mass.:
195.689
SMILES:
C[C@H]1CNCCc2ccc(Cl)cc12 |r|