capsaicin [Ligand Id: 2486] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL294199 (FEMA NO. 3404, NSC-56353, Zacin, ALGRX 4975, NGX-1998, NGX-4010, Qutenza, Zostrix, Ngx-1998, ALGRX-4975, Capsaicin, Zostrix HP)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
There should be some charts here, you may need to enable JavaScript!
  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • NADH-ubiquinone oxidoreductase chain 1 in Bovine [ChEMBL: CHEMBL4497] [UniProtKB: P03887]
There should be some charts here, you may need to enable JavaScript!
  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Mouse [ChEMBL: CHEMBL3108632] [GtoPdb: 500] [UniProtKB: Q8R4D5]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
  • Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
There should be some charts here, you may need to enable JavaScript!
  • Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
There should be some charts here, you may need to enable JavaScript!
  • Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
There should be some charts here, you may need to enable JavaScript!
  • Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cell membrane B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cell membrane B 5 pKi >10000 nM Ki J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL Inhibition of COX1 B 5.42 pIC50 3800 nM IC50 J. Nat. Prod. (2005) 68: 985-991 [PMID:16038536]
ChEMBL DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) B 5.81 pIC50 1551 nM IC50 DrugMatrix in vitro pharmacology data
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.52 pIC50 3000 nM IC50 DrugMatrix in vitro pharmacology data
NADH-ubiquinone oxidoreductase chain 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4497] [UniProtKB: P03887]
ChEMBL Inhibition of Bos taurus (bovine) heart submitochondrial particle NDH1 assessed as NADH-DB reductase activity B 4.28 pIC50 52480.75 nM IC50 Biochim. Biophys. Acta (1996) 1273: 21-30 [PMID:8573592]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108632] [GtoPdb: 500] [UniProtKB: Q8R4D5]
ChEMBL 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 B 4 pIC50 >100000 nM IC50 J. Nat. Prod. (2014) 77: 285-297 [PMID:24484240]
ChEMBL 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 B 4.55 pIC50 28000 nM IC50 J. Nat. Prod. (2014) 77: 285-297 [PMID:24484240]
Tyrosyl-tRNA synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577]
ChEMBL Compound was tested for the inhibition of aminoacyl tRNA Synthetase B 4.38 pKi 42000 nM Ki Bioorg. Med. Chem. Lett. (1997) 7: 2363-2366
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Displacement of [3H]MPOU from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method B 5.6 pKi 2530 nM Ki J Med Chem (2017) 60: 8246-8252 [PMID:28892388]
ChEMBL Displacement of [3H]RTX from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method B 5.94 pKi 1140 nM Ki J Med Chem (2017) 60: 8246-8252 [PMID:28892388]
ChEMBL Binding affinity to human recombinant TRPV1 B 8.22 pKi 6 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7137-7141 [PMID:20947352]
ChEMBL 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 B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 1009-1011 [PMID:25666822]
ChEMBL Agonist activity at TRPV1 (unknown origin) expressed in human SH-SY5Y cells assessed as increase in calcium influx after 25 mins by Fluo-4 NW dye-based fluorescence assay B 6 pEC50 1000 nM EC50 J Med Chem (2018) 61: 4436-4455 [PMID:29722529]
ChEMBL Agonist activity at recombinant TRPV1 (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux administered for 1 min followed by compound washout via perfusion for 1 min by FURA-2AM-dye based fluorescence assay B 6.06 pEC50 870.96 nM EC50 J Med Chem (2018) 61: 3126-3137 [PMID:29543451]
ChEMBL Agonist activity at recombinant TRPV1 (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux administered for 1 min followed by compound washout via perfusion for 1 min by FURA-2AM-dye based fluorescence assay B 6.06 pEC50 870 nM EC50 J Med Chem (2018) 61: 3126-3137 [PMID:29543451]
ChEMBL Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells F 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 132-135 [PMID:17046253]
ChEMBL Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level F 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 97-99 [PMID:19951840]
GtoPdb - - 7.5 pEC50 31.6 nM EC50 Nature (2004) 430: 748-54 [PMID:15306801]
ChEMBL Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level F 7.7 pEC50 20 nM EC50 J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
ChEMBL 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 F 7.7 pEC50 19.95 nM EC50 J. Med. Chem. (2002) 45: 3739-3745 [PMID:12166946]
ChEMBL Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as Ca2+ influx by Fluo-4 dye based assay B 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1009-1011 [PMID:25666822]
ChEMBL Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed as calcium influx by fluo-4-Am-based fluorimetry F 8.41 pEC50 3.9 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 1674-1677 [PMID:22257892]
ChEMBL Agonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as increase in intracellular calcium levels by fluorimetric assay F 8.6 pEC50 2.51 nM EC50 Bioorg. Med. Chem. (2010) 18: 3299-3306 [PMID:20381363]
TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3]
GtoPdb - - 8 pEC50 - - - Neurosci. Lett. (2004) 370: 55-60 [PMID:15489017]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL Binding affinity against Vanilloid receptor in dorsal Root Ganglion (DRG) membranes using [3H]RTX binding assay. B 5.7 pKi 2000 nM Ki J. Med. Chem. (1996) 39: 2939-2952 [PMID:8709128]
ChEMBL Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranes B 5.7 pKi 2000 nM Ki J. Med. Chem. (1996) 39: 3123-3131 [PMID:8759633]
ChEMBL Displacement of [3H]RTX form rat TRPV1 receptor expressed in CHO/VR1 cell system B 5.74 pKi 1808 nM Ki Bioorg. Med. Chem. (2009) 17: 690-698 [PMID:19135377]
ChEMBL In vitro binding affinity towards Rat Vanilloid receptor 1 (VR1) by [3H]RTX displacement. B 5.74 pKi 1800 nM Ki J. Med. Chem. (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL In vitro binding to Rat Vanilloid receptor 1 (VR1) expressing CHO cells compared to capsaicin B 5.77 pKi 1700 nM Ki J. Med. Chem. (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL Binding affinity to rat TRPV1 B 7.72 pIC50 19 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7137-7141 [PMID:20947352]
GtoPdb - - 6.1 pEC50 - - - Nature (1997) 389: 816-24 [PMID:9349813]
ChEMBL In vitro [Ca2+] influx relative to capsaicin by Rat Vanilloid receptor (VR1) expressing CHO cells F 7.35 pEC50 44.8 nM EC50 J. Med. Chem. (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptake F 7.35 pEC50 44.8 nM EC50 Bioorg. Med. Chem. (2009) 17: 690-698 [PMID:19135377]
Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
ChEMBL Inhibition of Kv1.1 (unknown origin) B 4.54 pIC50 29000 nM IC50 J Med Chem (2017) 60: 2245-2256 [PMID:28225274]
Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
GtoPdb - - 4.5 pIC50 - - - Mol. Pharmacol. (1994) 45: 1227-34 [PMID:7517498]
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
GtoPdb - - 4.4 pKd 45000 nM Kd Mol. Pharmacol. (1994) 45: 1227-34 [PMID:7517498]
Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
GtoPdb - - 4.6 pIC50 - - - J. Biol. Chem. (1998) 273: 5851-7 [PMID:9488722]
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
GtoPdb - - 3.8 pIC50 - - - Mol. Pharmacol. (1994) 45: 1227-34 [PMID:7517498]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]