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Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50439217
Substrate
n/a
Meas. Tech.
ChEMBL_978615 (CHEMBL2422132)
IC50
12500±n/a nM
Citation
 Washburn, DG; Holt, DA; Dodson, J; McAtee, JJ; Terrell, LR; Barton, L; Manns, S; Waszkiewicz, A; Pritchard, C; Gillie, DJ; Morrow, DM; Davenport, EA; Lozinskaya, IM; Guss, J; Basilla, JB; Negron, LK; Klein, M; Willette, RN; Fries, RE; Jensen, TC; Xu, X; Schnackenberg, CG; Marino, JP The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg Med Chem Lett 23:4979-84 (2013) [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:
BDBM50439217
Synonyms:
CHEMBL2418811
Type:
Small organic molecule
Emp. Form.:
C18H21ClFN3OS
Mol. Mass.:
381.895
SMILES:
C[C@H]1CCCN([C@H]1C)C(=O)c1nc(Nc2ccc(Cl)cc2F)sc1C |r|
Structure:
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