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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50502650
Substrate
n/a
Meas. Tech.
ChEMBL_1808133 (CHEMBL4307492)
IC50
5.5±n/a nM
Citation
 Brooks, CA; Barton, LS; Behm, DJ; Eidam, HS; Fox, RM; Hammond, M; Hoang, TH; Holt, DA; Hilfiker, MA; Lawhorn, BG; Patterson, JR; Stoy, P; Roethke, TJ; Ye, G; Zhao, S; Thorneloe, KS; Goodman, KB; Cheung, M Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4). ACS Med Chem Lett 10:1228-1233 (2019) [PubMed]  Article
Target
Name:
Transient receptor potential cation channel subfamily V member 4
Synonyms:
TRPV4_RAT | Trpv4 | Vanilloid receptor | Vroac
Type:
PROTEIN
Mol. Mass.:
98016.72
Organism:
Rattus norvegicus
Description:
ChEMBL_1514408
Residue:
871
Sequence:
MADPGDGPRAAPGDVAEPPGDESGTSGGEAFPLSSLANLFEGEEGSSSLSPVDASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHPSDNKRWRRKVVEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLSYLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCSRLFPDSNLETVLNNDGLSPLMMAAKTGKIGVFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEVSVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLLTGVLFFFTSIKDLFMKKCPGVNSLFVDGSFQLLYFIYSVLVVVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVTLLNPCTNMKVCNEDQSNCTVPSYPACRDSETFSAFLLDLFKLTIGMGDLEMLSSAKYPVVFILLLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKSEIYQYYGFSHTMGRLRRDRWSSVVPRVVELNKNSGTDEVVVPLDNLGNPNCDGHQQGYAPKWRAEDAPL
  
Inhibitor
Name:
BDBM50502650
Synonyms:
CHEMBL4549613
Type:
Small organic molecule
Emp. Form.:
C22H28N4O2
Mol. Mass.:
380.4833
SMILES:
CC(C)(C)CN1C[C@@]2(CCC[C@H](Cn3cnc4ccc(cc34)C#N)C2)OC1=O |r|
Structure:
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