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Target
Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM20383
Substrate
BDBM10852
Meas. Tech.
Ca2+ Influx Functional Assay for the Determination of in Vitro Activity.
pH
7.4±n/a
Temperature
295.15±n/a K
EC50
22±9 nM
Citation
 Gomtsyan, A; Bayburt, EK; Keddy, R; Turner, SC; Jinkerson, TK; Didomenico, S; Perner, RJ; Koenig, JR; Drizin, I; McDonald, HA; Surowy, CS; Honore, P; Mikusa, J; Marsh, KC; Wetter, JM; Faltynek, CR; Lee, CH Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model. Bioorg Med Chem Lett 17:3894-9 (2007) [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:
BDBM20383
Synonyms:
1-isoquinolin-5-yl-3-{1-[4-(trifluoromethyl)phenyl]ethyl}urea | CHEMBL389715 | isoquinoline antagonist, 5a
Type:
Small organic molecule
Emp. Form.:
C19H16F3N3O
Mol. Mass.:
359.345
SMILES:
CC(NC(=O)Nc1cccc2cnccc12)c1ccc(cc1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate