Reaction Details  Report a problem with these data
Target
Transient receptor potential cation channel subfamily V member 4
Ligand
BDBM50256210
Substrate
n/a
Meas. Tech.
ChEMBL_1699599 (CHEMBL4050581)
IC50
1.3±n/a nM
Citation
 Tsuno, N; Yukimasa, A; Yoshida, O; Suzuki, S; Nakai, H; Ogawa, T; Fujiu, M; Takaya, K; Nozu, A; Yamaguchi, H; Matsuda, H; Funaki, S; Yamanada, N; Tanimura, M; Nagamatsu, D; Asaki, T; Horita, N; Yamamoto, M; Hinata, M; Soga, M; Imai, M; Morioka, Y; Kanemasa, T; Sakaguchi, G; Iso, Y Pharmacological evaluation of novel (6-aminopyridin-3-yl)(4-(pyridin-2-yl)piperazin-1-yl) methanone derivatives as TRPV4 antagonists for the treatment of pain. Bioorg Med Chem 25:2177-2190 (2017) [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:
Human
Description:
Q9HBA0
Residue:
871
Sequence:
MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGPGDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDNKRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRLTDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQTALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHIVNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDSNLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYDLSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLCAMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGVNSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTGTYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSCRDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGETVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRVDEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDEVVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL
  
Inhibitor
Name:
BDBM50256210
Synonyms:
CHEMBL4080527
Type:
Small organic molecule
Emp. Form.:
C25H24F3N9OS
Mol. Mass.:
555.578
SMILES:
Cc1cc(-c2csc(Nc3ccc(cn3)C(=O)N3C4CCC3CN(C4)c3ncc(cn3)C(F)(F)F)n2)n(C)n1
Structure:
Search PDB for entries with ligand similarity: