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

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ChEMBL ligand: CHEMBL294199 (ALGRX 4975, ALGRX-4975, Ausanil, Axsain, Capsaicin, Capzasin-hp, Cntx-4975, Dolenon, FEMA NO. 3404, Mioton, Ngx-1998, NGX-1998, NGX-4010, NSC-56353, Ovocap, Qutenza, Ratden pe 40, Togarashi orenji, Trans-capsaicin, Zacin, Zostrix, Zostrix hp)
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • NADH-ubiquinone oxidoreductase chain 1 in Bovine [ChEMBL: CHEMBL4497] [UniProtKB: P03887]
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  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Mouse [ChEMBL: CHEMBL3108632] [GtoPdb: 500] [UniProtKB: Q8R4D5]
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  • 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]
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  • Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
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  • Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
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  • Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of human PMNL 5-LOX using arachidonic acid as substrate after 5 mins by HPLC method B 4.25 pIC50 56000 nM IC50 Bioorg Med Chem (2019) 27: 3745-3759 [PMID:31331653]
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]
ChEMBL Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in HEK cells by Cheng-Prusoff analysis B 5.25 pKi >5600 nM Ki J Med Chem (2020) 63: 12290-12358 [PMID:32686940]
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 Displacement of [3H]-RTX from human TRPV1 expressed in CHO cells incubated for 60 mins by radioligand competition assay based scintillation counting method B 5.97 pKi 1070 nM Ki J Med Chem (2020) 63: 418-424 [PMID:31702924]
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 Antagonist activity at human TRPV1 stably transfected in HEK293 cells assessed as decrease in calcium influx preincubated for 5 mins followed by capsaicin addition by Fluo-4-AM dye based spectrofluorimetric method B 8.1 pIC50 8 nM IC50 J Nat Prod (2020) 83: 3476-3481 [PMID:33136399]
ChEMBL Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as effect on intracellular calcium level by FLOU-4 dye based fluorescence spectrometry B 4.52 pEC50 30200 nM EC50 J Med Chem (2020) 63: 12290-12358 [PMID:32686940]
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 TRPV1 expressed in CHO cells assessed as stimulation of calcium uptake by 45Ca2+ uptake assay B 7.35 pEC50 44.8 nM EC50 J Med Chem (2021) 64: 370-384 [PMID:33385210]
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 TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method B 7.59 pEC50 25.9 nM EC50 J Med Chem (2020) 63: 418-424 [PMID:31702924]
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 TRPV1 expressed in HEK293T cells assessed as increase in Ca2+ transport incubated for 5 mins by calcium-5 fluorescence dye-based FLIPR assay B 8.14 pEC50 7.2 nM EC50 Bioorg Med Chem (2019) 27: 2893-2904 [PMID:31104785]
ChEMBL Agonist activity at human TRPV1 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method B 8.28 pEC50 5.3 nM EC50 J Nat Prod (2020) 83: 3476-3481 [PMID:33136399]
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 from rat TRPV1 expressed in CHO cells incubated for 60 mins by radioligand competition assay based scintillation counting method B 5.74 pKi 1810 nM Ki J Med Chem (2020) 63: 418-424 [PMID:31702924]
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]
ChEMBL Agonist activity at rat TRPV1 expressed in human SH-SY5Y cells assessed as intracellular calcium accumulation by Fluo-4 NW dye based fluorescence assay B 5.63 pEC50 2320 nM EC50 ACS Med Chem Lett (2019) 10: 143-144 [PMID:30783490]
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]
ChEMBL Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method B 7.35 pEC50 44.8 nM EC50 J Med Chem (2020) 63: 418-424 [PMID:31702924]
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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]