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Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM50391055
Substrate
n/a
Meas. Tech.
ChEMBL_840432 (CHEMBL2089708)
IC50
3.7±n/a nM
Citation
 Besidski, Y; Brown, W; Bylund, J; Dabrowski, M; Dautrey, S; Harter, M; Horoszok, L; Hu, Y; Johnson, D; Johnstone, S; Jones, P; Leclerc, S; Kolmodin, K; Kers, I; Labarre, M; Labrecque, D; Laird, J; Lundström, T; Martino, J; Maudet, M; Munro, A; Nylöf, M; Penwell, A; Rotticci, D; Slaitas, A; Sundgren-Andersson, A; Svensson, M; Terp, G; Villanueva, H; Walpole, C; Zemribo, R; Griffin, AM Potent and orally efficacious benzothiazole amides as TRPV1 antagonists. Bioorg Med Chem Lett 22:6205-11 (2012) [PubMed]  Article 
Target
Name:
Transient receptor potential cation channel subfamily V member 1
Synonyms:
Capsaicin receptor | OTRPC1 | Osm-9-like TRP channel 1 | TRPV1 | TRPV1_HUMAN | Transient receptor potential cation channel subfamily V member 1 | Transient receptor potential cation channel subfamily V member 1 (TRPV1) | Transient receptor potential cation channel subfamily V member 1 (VR1/TRPV1) | Transient receptor potential cation channel subfamily V member 1(TRPV1) | VR1 | Vanilloid VR1 | Vanilloid receptor | Vanilloid receptor 1 | Vanilloid receptor 1 (TrpV1/Vr1) | Vanilloid receptor 1 (VRI/TRPV1)
Type:
Protein
Mol. Mass.:
94960.75
Organism:
Homo sapiens (Human)
Description:
Q8NER1
Residue:
839
Sequence:
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFPVDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFEAVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEIARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKTKGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTADNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEILSVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVASMVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIEDGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSSRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
  
Inhibitor
Name:
BDBM50391055
Synonyms:
CHEMBL2088399
Type:
Small organic molecule
Emp. Form.:
C19H20N2O2S
Mol. Mass.:
340.439
SMILES:
CC(C)(C)c1ccc(cc1)C(=O)Nc1ccc2sc(CO)nc2c1
Structure:
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