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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50232798
Substrate
n/a
Meas. Tech.
ChEMBL_1648651 (CHEMBL3997707)
IC50
4.0±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_RAT | Trpv4 | Vanilloid receptor | Vroac
Type:
PROTEIN
Mol. Mass.:
98016.72
Organism:
Rattus norvegicus
Description:
ChEMBL_1514408
Residue:
871
Sequence:
MADPGDGPRAAPGDVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDNKRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSYLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDSNLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLLTGVLFFFTSIKDLFMKKCPGVNSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCNEDQSNCTVPSYPACRDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTMGRLRRDRWSSVVPRVVELNKNSGTDEVVVPLDNLGNPNCDGHQQGYAPKWRAEDAPL
  
Inhibitor
Name:
BDBM50232798
Synonyms:
CHEMBL4095413
Type:
Small organic molecule
Emp. Form.:
C37H38F6N4O2
Mol. Mass.:
684.7136
SMILES:
COc1ccc2c(C(=O)N[C@H](c3ccccc3)C(F)(F)F)c(CN3CCC(CC3)N3CCCCC3)c(nc2c1)-c1cccc(c1)C(F)(F)F |r|
Structure:
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