Assay of Pungent Compounds

PID Structure Name IC50 EC50 Assay Organism Target Name Assay_References Note
PID00003 Capsaicin 3000 nM - Homo sapiens Cytochrome P450 1A2 CHEMBL1909046 DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)
PID00003 Capsaicin 3800 nM - Homo sapiens Cyclooxygenase-1 J. Nat. Prod., (2005) 68:7:985 Inhibition of COX1
PID00003 Capsaicin 52480.75 nM - Bos taurus NADH-ubiquinone oxidoreductase chain 1 Biochim. Biophys. Acta, (1996) 1273:1:21 Inhibition of Bos taurus (bovine) heart submitochondrial particle NDH1 assessed as NADH-DB reductase activity
PID00003 Capsaicin 28000 nM - Mus musculus Transient receptor potential cation channel subfamily M member 8 J. Nat. Prod., (2014) 77:2:285 Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of menthol-induced intracellular Ca2+ influx by fluorescence-based assay
PID00003 Capsaicin 19 nM - Rattus norvegicus Vanilloid receptor Bioorg. Med. Chem. Lett., (2010) 20:23:7137 Binding affinity to rat TRPV1
PID00003 Capsaicin 8 nM - Homo sapiens Vanilloid receptor Bioorg. Med. Chem. Lett., (2015) 25:5:1009 Antagonist activity against human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx pre-treated 5 mins before capsaicin addition by Fluo-4 dye based assay
PID00003 Capsaicin - - Homo sapiens Vascular endothelial growth factor receptor 1 CHEMBL1909046 DRUGMATRIX: Vascular Endothelial Growth Factor (VEGF) radioligand binding (ligand: [125I] VEGF)
PID00003 Capsaicin - - Homo sapiens Vasoactive intestinal polypeptide receptor 1 CHEMBL1909046 DRUGMATRIX: Vasoactive Intestinal Peptide VIP1 radioligand binding (ligand: [125I] VIP)
PID00003 Capsaicin - - Homo sapiens Vasopressin V1a receptor CHEMBL1909046 DRUGMATRIX: Vasopressin V1A radioligand binding (ligand: [125I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr)
PID00003 Capsaicin > 100000 nM - Mus musculus Transient receptor potential cation channel subfamily M member 8 J. Nat. Prod., (2014) 77:2:285 Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx by fluorescence-based assay