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TargetTransient receptor potential cation channel subfamily V member 4
LigandBDBM50521996
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1885908 (CHEMBL4387490)
IC50 1.1±n/a nM
Citation Sami, YMorita, MKubota, HHirabayashi, RSeo, RNakagawa, N Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit. Bioorg Med Chem27:3775-3787 (2019) [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:
BDBM50521996
n/a
NameBDBM50521996
Synonyms:CHEMBL4459940
TypeSmall organic molecule
Emp. Form.C25H32Cl2FN5OS
Mol. Mass.540.524
SMILESCl.Cl.Cc1c(cnn1-c1ccc(F)cc1)C(=O)Nc1nc(C2CCC2)c(CCN2CCCCC2)s1
Structure
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