Assay of Pungent Compounds

PID Structure Name IC50 EC50 Assay Organism Target Name Assay_References Note
PID00003 Capsaicin - 5.3 nM Homo sapiens Vanilloid receptor Bioorg. Med. Chem. Lett., (2015) 25:5:1009 Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as Ca2+ influx by Fluo-4 dye based assay
PID00003 Capsaicin - 2.512 nM Homo sapiens Vanilloid receptor Bioorg. Med. Chem., (2010) 18:9:3299 Agonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as increase in intracellular calcium levels by fluorimetric assay
PID00003 Capsaicin - 44.8 nM Rattus norvegicus Vanilloid receptor Bioorg. Med. Chem., (2009) 17:2:690 Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptake
PID00003 Capsaicin - 300 nM Rattus norvegicus Vanilloid receptor J. Med. Chem., (1993) 36:16:2373 Effective concentration for [Ca2+] uptake into dorsal root ganglia neurones in rat cultured spinal sensory neurones
PID00003 Capsaicin - 30 nM Rattus norvegicus Vanilloid receptor Bioorg. Med. Chem. Lett., (2004) 14:3:787 In vitro agonist activity, increased [Ca2+] influx, at vanilloid receptor of rat dorsal root ganglia
PID00003 Capsaicin - 3.9 nM Homo sapiens Vanilloid receptor Bioorg. Med. Chem. Lett., (2012) 22:4:1674 Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed as calcium influx by fluo-4-Am-based fluorimetry
PID00003 Capsaicin - 40 nM Homo sapiens Vanilloid receptor Bioorg. Med. Chem. Lett., (2007) 17:1:132 Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells
PID00003 Capsaicin - 44.8 nM Rattus norvegicus Vanilloid receptor J. Med. Chem., (2003) 46:14:3116 In vitro [Ca2+] influx relative to capsaicin by Rat Vanilloid receptor (VR1) expressing CHO cells
PID00003 Capsaicin - 19.95 nM Homo sapiens Vanilloid receptor J. Med. Chem., (2002) 45:17:3739 Concentration necessary to induce a relative half-maximal response measured by the entry of [Ca2+] into human embryonic kidney HEK293 cells overexpressing the human VR1
PID00003 Capsaicin 1551 nM - Homo sapiens Cyclooxygenase-1 CHEMBL1909046 DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)