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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM539984
Substrate
n/a
Meas. Tech.
FLIPR Assay for hTRPV4 Expressed in BHK Cells
IC50
5±n/a nM
Citation
Brnardic, EJ; Brooks, CA; Lawhorn, BG; Li, P; Matthews, JM; McAtee, JJ; Pero, JE; Sender, MR; Terrell, LR; Behm, DJ TRPV4 antagonists US Patent US11260049 Publication Date 3/1/2022
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:
BDBM539984
Synonyms:
4-(((3R,4S)-3- (aminomethyl)-4- ((4-chlorophenyl) sulfonyl)-3- hydroxypyrrolidin- 1-yl)sulfonyl)-3- chlorobenzonitrile | US11260049, Ex. 122
Type:
Small organic molecule
Emp. Form.:
C18H17Cl2N3O5S2
Mol. Mass.:
490.381
SMILES:
NC[C@@]1(O)CN(C[C@@H]1S(=O)(=O)c1ccc(Cl)cc1)S(=O)(=O)c1ccc(cc1Cl)C#N |r|