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TargetTransient receptor potential cation channel subfamily V member 4
LigandBDBM50522014
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1885905 (CHEMBL4387487)
IC50 1.9±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 | 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
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  Blast E-value cutoff:
BDBM50522014
n/a
NameBDBM50522014
Synonyms:CHEMBL4460657
TypeSmall organic molecule
Emp. Form.C23H27FN6OS
Mol. Mass.454.563
SMILESCN1CCN(CC1)c1sc(NC(=O)c2cnn(c2C)-c2ccc(F)cc2)nc1C1CCC1
Structure
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