Reaction Details
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Transient receptor potential cation channel subfamily V member 1
Ligand
BDBM50263384
Substrate
n/a
Meas. Tech.
ChEMBL_536370 (CHEMBL994288)
pH
5.3±n/a
IC50
63±n/a nM
Comments
extracted
Citation
Westaway, SM; Thompson, M; Rami, HK; Stemp, G; Trouw, LS; Mitchell, DJ; Seal, JT; Medhurst, SJ; Lappin, SC; Biggs, J; Wright, J; Arpino, S; Jerman, JC; Cryan, JE; Holland, V; Winborn, KY; Coleman, T; Stevens, AJ; Davis, JB; Gunthorpe, MJ Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1. Bioorg Med Chem Lett 18:5609-13 (2008) [PubMed] Article More Info.:
Target
Name:
Transient receptor potential cation channel subfamily V member 1
Synonyms:
TRPV1_CAVPO | Trpv1 | Vanilloid receptor 1
Type:
PROTEIN
Mol. Mass.:
95254.87
Organism:
Cavia porcellus
Description:
ChEMBL_536370
Residue:
839
Sequence:
MKKRASVDSKESEDPPQEDYSLDPLDVDANSKTPPAKPHTFSVSKSRNRLFGKSDLEESSPIDCSFREGEAASCPTITVSSVVTSPRPADGPTSTRQLTQDSIPTSAEKPLKLYDRRSIFDAVAQNNCQDLDSLLPFLQKSKKRLTDTEFKDPETGKTCLLKAMLNLHNGQNDTISLLLDIARQTNSLKEFVNASYTDSYYRGQTALHIAIERRNMVLVTLLVENGADVQAAANGDFFKKTKGRPGFYFGELPLSLAACTNQLAIVKFLLQNSWQPADISARDSVGNTVLHALVEVADNTADNTKFVTSMYNEILILGAKLYPTLKLEELTNKKGFTPLALAASSGKIGVLAYILQREIPEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFFIYCLYMIIFTMAAYYRPVDGLPPYKMKNTVGDYFRVTGEILSVIGGFHFFFRGIQYFLQRRPSVKTLFVDSYSEILFFVQSLFLLASVVLYFSHRKEYVACMVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYLVFLFGFSTAVVTLIEDGKNESLSAEPHRWRGPGCRSAKNSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSGRVSGRNWKNFALVPLLRDASTRDRHSAQPEEVHLKHFSGSLKPEDAEVFKDSAVPGEK
Inhibitor
Name:
BDBM50263384
Synonyms:
6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide | CHEMBL514691 | SB-782443
Type:
Small organic molecule
Emp. Form.:
C21H16FN3OS
Mol. Mass.:
377.435
SMILES:
Cc1nc2cc(NC(=O)c3ccc(nc3C)-c3ccc(F)cc3)ccc2s1
Structure:
