Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM436101
Substrate
n/a
Meas. Tech.
FLIPR Assay
IC50
55±n/a nM
Citation
 Brnardic, EJBrooks, CABudzik, BWLawhorn, BGMatthews, JMMcAtee, JJPero, JEBehm, DJ TRPV4 antagonists US Patent  US10590077 Publication Date 3/17/2020 
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:
BDBM436101
Synonyms:
4-(((3S,4R)-1- ((5-chloropyridin- 2-yl)sulfonyl)-4- hydroxy-4- (hydroxymethyl) pyrrolidin-3-yl) methyl)-3-(2,2,2- trifluoroethoxy) benzonitrile | US10590077, Example 3
Type:
Small organic molecule
Emp. Form.:
C20H19ClF3N3O5S
Mol. Mass.:
505.895
SMILES:
OC[C@]1(O)CN(C[C@@H]1Cc1ccc(cc1OCC(F)(F)F)C#N)S(=O)(=O)c1ccc(Cl)cn1 |r|
Structure:
Search PDB for entries with ligand similarity: