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TargetTransient receptor potential cation channel subfamily V member 4
LigandBDBM50521995
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1885905 (CHEMBL4387487)
IC50 1.2±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:
BDBM50521995
n/a
NameBDBM50521995
Synonyms:CHEMBL4578182
TypeSmall organic molecule
Emp. Form.C24H31Cl2FN6OS
Mol. Mass.541.512
SMILESCl.Cl.Cc1c(cnn1-c1ccc(F)cn1)C(=O)Nc1nc(C2CCC2)c(CCN2CCCCC2)s1
Structure
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