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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50502640
Substrate
n/a
Meas. Tech.
ChEMBL_1823196 (CHEMBL4322960)
IC50
1.8±n/a nM
Citation
 Brooks, CA; Barton, LS; Behm, DJ; Brnardic, EJ; Costell, MH; Holt, DA; Jolivette, LJ; Matthews, JM; McAtee, JJ; McCleland, BW; Patterson, JR; Pero, JE; Rivero, RA; Roethke, TJ; Sanchez, RM; Shenje, R; Terrell, LR; Lawhorn, BG Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4). J Med Chem 62:9270-9280 (2019) [PubMed]  Article 
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:
BDBM50502640
Synonyms:
CHEMBL4470585
Type:
Small organic molecule
Emp. Form.:
C25H28N6O3
Mol. Mass.:
460.5282
SMILES:
CC(C)(O)c1cnc(cn1)N1C[C@@]2(CCC[C@](C)(Cn3cnc4ccc(cc34)C#N)C2)OC1=O |r|
Structure:
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