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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50192821
Substrate
n/a
Meas. Tech.
ChEMBL_1648700 (CHEMBL3997756)
IC50
17±n/a nM
Citation
 Cheung, M; Bao, W; Behm, DJ; Brooks, CA; Bury, MJ; Dowdell, SE; Eidam, HS; Fox, RM; Goodman, KB; Holt, DA; Lee, D; Roethke, TJ; Willette, RN; Xu, X; Ye, G; Thorneloe, KS Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. ACS Med Chem Lett 8:549-554 (2017) [PubMed]  Article 
Target
Name:
Transient receptor potential cation channel subfamily V member 4
Synonyms:
TRPV4_MOUSE | Trp12 | Trpv4 | Vrl2 | Vroac
Type:
PROTEIN
Mol. Mass.:
98032.61
Organism:
Mus musculus
Description:
ChEMBL_1514430
Residue:
871
Sequence:
MADPGDGPRAAPGEVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDNKRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSFLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTSLHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDSNLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTSIKDLFTKKCPGVNSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCDEDQSNCTVPTYPACRDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSSADEVVVPLDNLGNPNCDGHQQGYAPKWRTDDAPL
  
Inhibitor
Name:
BDBM50192821
Synonyms:
CHEMBL2133556
Type:
Small organic molecule
Emp. Form.:
C26H28F3N3O2
Mol. Mass.:
471.5146
SMILES:
Cc1c(cc(-c2ccccc2)n1CCCN1CCOCC1)C(=O)Nc1cccc(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: