Reaction Details
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Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM230244
Substrate
n/a
Meas. Tech.
Inhibition Assay
Temperature
310.15±n/a K
Ki
2800±n/a nM
IC50
5800±n/a nM
Comments
extracted
Citation
Yukimasa, A Aromatic heterocyclic derivative having TRPV4-inhibiting activity US Patent US9340500 Publication Date 5/17/2016 More Info.:
Target
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:
MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDNKRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDSNLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGVNSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSCRDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDEVVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL
Inhibitor
Name:
BDBM230244
Synonyms:
US9340500, I-088
Type:
Small organic molecule
Emp. Form.:
C26H26F3N3O2
Mol. Mass.:
469.4987
SMILES:
FC(F)(F)c1cccc(NC(=O)c2cnc(c(CCCN3CCOCC3)c2)-c2ccccc2)c1
Structure:
