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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50117650
Substrate
n/a
Meas. Tech.
ChEMBL_1514407 (CHEMBL3615486)
IC50
800±n/a nM
Citation
 Wei, ZL; Nguyen, MT; O'Mahony, DJ; Acevedo, A; Zipfel, S; Zhang, Q; Liu, L; Dourado, M; Chi, C; Yip, V; DeFalco, J; Gustafson, A; Emerling, DE; Kelly, MG; Kincaid, J; Vincent, F; Duncton, MA Identification of orally-bioavailable antagonists of the TRPV4 ion-channel. Bioorg Med Chem Lett 25:4011-5 (2015) [PubMed]  Article 
Target
Name:
Transient receptor potential cation channel subfamily V member 4
Synonyms:
TRPV4 | TRPV4_HUMAN | Transient receptor potential cation channel subfamily V member 4 (TRPV4) | VRL2 | VROAC
Type:
Enzyme
Mol. Mass.:
98290.10
Organism:
Homo sapiens (Human)
Description:
Q9HBA0
Residue:
871
Sequence:
MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDNKRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDSNLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGVNSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSCRDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDEVVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL
  
Inhibitor
Name:
BDBM50117650
Synonyms:
CHEMBL3613638
Type:
Small organic molecule
Emp. Form.:
C23H26F3N3O3S
Mol. Mass.:
481.531
SMILES:
FC(F)(F)c1ccc(cc1)C(=O)Nc1ccc(cc1)S(=O)(=O)N1CCN(CC1)C1CCCC1
Structure:
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