Reaction Details Report a problem with these data
Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM20495
Substrate
BDBM10852
Meas. Tech.
FLIPR (Fluorescence Imaging Plate Reader)-Based Ca2+ Assay
pH
7.2±n/a
Temperature
298.15±n/a K
EC50
40±n/a nM
Citation
 Rami, HK; Thompson, M; Stemp, G; Fell, S; Jerman, JC; Stevens, AJ; Smart, D; Sargent, B; Sanderson, D; Randall, AD; Gunthorpe, MJ; Davis, JB Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett 16:3287-91 (2006) [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:
BDBM20495
Synonyms:
3-(2-bromophenyl)-1-[2-(6-methyl-1,2,3,4-tetrahydroquinolin-1-yl)ethyl]urea | tetrahydroquinoline derivative, 6
Type:
Small organic molecule
Emp. Form.:
C19H22BrN3O
Mol. Mass.:
388.301
SMILES:
Cc1ccc2N(CCNC(=O)Nc3ccccc3Br)CCCc2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate