capsaicin [Ligand Id: 2486] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL294199 (ALGRX 4975, ALGRX-4975, Ausanil, Axsain, Capsaicin, Capsaicina, Capsaicine, 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) |
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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 |
| lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341] | ||||||||
| ChEMBL | Inhibition of recombinant LSD1 (unknown origin) using 10-acetyl-3,7-dihydroxyphenoxazine fluorometric substrate measured after 30 mins by multiplate reader | B | 6.22 | pIC50 | 600 | nM | IC50 | Eur J Med Chem (2021) 214: 113254-113254 [PMID:33581557] |
| ChEMBL | Inhibition of LSD1 (unknown origin) by KDM1A assay kit | B | 6.22 | pIC50 | 600 | nM | IC50 | Eur J Med Chem (2022) 240: 114564-114564 [PMID:35820351] |
| ChEMBL | Inhibition of KDM1A (unknown origin) | B | 6.22 | pIC50 | 600 | nM | IC50 | Eur J Med Chem (2022) 231: 114143-114143 [PMID:35101649] |
| ChEMBL | Inhibition of LSD1 (unknown origin) | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2021) 64: 2466-2488 [PMID:33619958] |
| 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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Antagonist activity at TRPM8 (unknown origin) | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2016) 59: 10006-10029 [PMID:27437828] |
| 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 | Inhibition of TRPV1 (unknown origin) | B | 6.38 | pIC50 | 420 | nM | IC50 | Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649] |
| ChEMBL | Activation of human TRPV1 expressed in HEK293F cells | B | 6.5 | pIC50 | 313 | nM | IC50 | Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649] |
| 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 | Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as desensitization by measuring inhibition of capsaicin-induced intracellular calcium accumulation preincubated for 5 mins followed by capsaicin stimulation by Fluo4-AM based assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2023) 66: 6994-7015 [PMID:37192374] |
| 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 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] |
| 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] |
| GtoPdb | - | - | 7.5 | pEC50 | 31.6 | nM | EC50 | Nature (2004) 430: 748-54 [PMID:15306801] |
| ChEMBL | Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium accumulation measured at 180 sec by fluorescence based microplate reader analysis | B | 7.54 | pEC50 | 29 | nM | EC50 | J Med Chem (2022) 65: 11658-11678 [PMID:36008373] |
| 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 recombinant TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo4-AM based assay | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2023) 66: 6994-7015 [PMID:37192374] |
| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
