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TargetTransient receptor potential cation channel subfamily V member 4
LigandBDBM50522021
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1885908 (CHEMBL4387490)
IC50 0.730000±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:
BDBM50522021
n/a
NameBDBM50522021
Synonyms:CHEMBL4465116
TypeSmall organic molecule
Emp. Form.C24H31Cl2FN6OS
Mol. Mass.541.512
SMILESCl.Cl.Cc1nn(cc1C(=O)Nc1nc(C2CCC2)c(CCN2CCCCC2)s1)-c1ccc(F)cn1
Structure
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