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TargetTransient receptor potential cation channel subfamily V member 4
LigandBDBM50192804
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1613834 (CHEMBL3855634)
IC50 15±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_RAT | Trpv4 | Vanilloid receptor | Vroac
Type:PROTEIN
Mol. Mass.:98016.72
Organism:Rattus norvegicus
Description:ChEMBL_1514408
Residue:871
Sequence:
MADPGDGPRAAPGDVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDN
KRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSYLLTHKKRL
TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT
ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI
VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDS
NLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD
LSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC
AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLLTGVLFFFTSIKDLFMKKCPGV
NSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG
TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCNEDQSNCTVPSYPAC
RDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGE
TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV
DEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTMGRLRRDRWSSVVPRVVELNKNSGTDE
VVVPLDNLGNPNCDGHQQGYAPKWRAEDAPL
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  Blast E-value cutoff:
BDBM50192804
n/a
NameBDBM50192804
Synonyms:CHEMBL3933401
TypeSmall organic molecule
Emp. Form.C21H21F3N6O3S2
Mol. Mass.526.555
SMILESCOC(=O)N1CCN(C(C1)C(F)(F)F)C(=O)c1ccc(Nc2nc(cs2)-c2sc(C)nc2C)nc1
Structure
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