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Target
5-hydroxytryptamine receptor 2C
Ligand
BDBM50161646
Substrate
n/a
Meas. Tech.
ChEMBL_744893 (CHEMBL1772914)
EC50
16.2±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 
Target
Name:
5-hydroxytryptamine receptor 2C
Synonyms:
5-HT2C | 5-hydroxytryptamine receptor 2C | 5HT2C_CANLF | HTR2C
Type:
Enzyme Catalytic Domain
Mol. Mass.:
51858.52
Organism:
CANINE
Description:
5-HT2C HTR2C CANINE::Q60F97
Residue:
458
Sequence:
MVNLRKAVHSFLVHLIGLLVWQCDISVSPVAALVTDIFNTSDGGRFKFPDGVQNWPALSIVIIIILTIGGNILVIMAVSLEKKLHNATNYFLMSLAIADMLVGLLVMPLSLLAILYDYVWPLPRYLCPVWISLDVLFSTASIMHLCAISLDRYVAIRNPVEHSRFNSRTKAIMKIAIVWAISIGVSVPIPVIGLRDEEKVFVNNTTCVLNDPNFVLIGSFVAFFIPLTIMVITYCLTIHVLRRQALMLLHGHVEEPPRINLDFLKCCRRNGTEEENSANPNQDSNPRRRKKKERRPRGTMQAINNERKASKVLGIVFFVFLVMWCPFFITNILSVLCGKACNQKLMEKLLNVFVWIGYVCSGINPLVYTLFNKIYRRAFSNYLRCNYKPEKKPPVRQMPRVAATALSGRELNVNIYRHTNEPVLKKANDKEPGIEMQVENLELPVNPSSVVSERISSV
  
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|
Structure:
Search PDB for entries with ligand similarity: