Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetTransient receptor potential cation channel subfamily V member 4
LigandBDBM50192826
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1613832 (CHEMBL3855632)
IC50 2.1±n/a nM
Citation Tsuno, NYukimasa, AYoshida, OSuzuki, SNakai, HOgawa, TFujiu, MTakaya, KNozu, AYamaguchi, HMatsuda, HFunaki, SNishimura, YIto, TNagamatsu, DAsaki, THorita, NYamamoto, MHinata, MSoga, MImai, MMorioka, YKanemasa, TSakaguchi, GIso, Y Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2. Bioorg Med Chem Lett26:4936-4941 (2016) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Transient receptor potential cation channel subfamily V member 4
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:
MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDN
KRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRL
TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT
ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI
VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDS
NLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD
LSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC
AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGV
NSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG
TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSC
RDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGE
TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV
DEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDE
VVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50192826
n/a
NameBDBM50192826
Synonyms:CHEMBL3979114
TypeSmall organic molecule
Emp. Form.C22H23F3N6OS2
Mol. Mass.508.583
SMILESCc1nc(C)c(s1)-c1csc(Nc2ccc(cn2)C(=O)N2C3CCC2CN(CC(F)(F)F)C3)n1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: