resiniferatoxin [Ligand Id: 2491] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL17976 (Lopain, Mtx-071, MTX-71, Neuroclastin, Resiniferatoxin, RTX) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | pIC50 | >100000 | nM | IC50 | J Nat Prod (2014) 77: 285-297 [PMID:24484240] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Displacement of [3H]RTX binding from vanilloid receptor | B | 7.64 | pKi | 23.1 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 1331-1334 |
| ChEMBL | Binding affinity to human recombinant TRPV1 | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 7137-7141 [PMID:20947352] |
| ChEMBL | Displacement of [3H]RTX from human TRPV1 expressed in CHO cells | B | 8.91 | pKi | 1.23 | nM | Ki | Eur J Med Chem (2013) 68: 233-243 [PMID:23981530] |
| ChEMBL | Displacement of [3H]RTX from human TRPV1 expressed in CHO cells after 60 mins by liquid scintillation counting analysis | B | 8.91 | pKi | 1.23 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 382-385 [PMID:24321344] |
| ChEMBL | Inhibition of [3H]RTX binding to human Vanilloid receptor subtype 1 expressed in HEK293 cells | B | 9.32 | pKi | 0.48 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1189-1192 [PMID:11934585] |
| GtoPdb | - | - | 8.4 | pEC50 | 3.98 | nM | EC50 | Eur J Pharmacol (2001) 417: 51-8 [PMID:11301059] |
| ChEMBL | Induced [Ca2+] influx in Vanilloid receptor subtype 1 expressing HEK 293 cells | F | 8.72 | pEC50 | 1.9 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 1189-1192 [PMID:11934585] |
| ChEMBL | Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of Ca2+ uptake | B | 9.04 | pEC50 | 0.92 | nM | EC50 | Eur J Med Chem (2013) 68: 233-243 [PMID:23981530] |
| ChEMBL | Agonist activity at human TRPV1 expressed in CHO cells assessed as 45Ca2+ uptake after 20 mins by liquid scintillation counting analysis | B | 9.04 | pEC50 | 0.92 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 382-385 [PMID:24321344] |
| ChEMBL | Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells | F | 10.72 | pEC50 | 0.02 | 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 | 10.72 | pEC50 | 0.02 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 97-99 [PMID:19951840] |
| TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3] | ||||||||
| GtoPdb | - | - | 9.8 | 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 | 8.36 | pKi | 4.4 | nM | Ki | J Med Chem (1996) 39: 2939-2952 [PMID:8709128] |
| ChEMBL | In vitro binding to Rat Vanilloid receptor 1 (VR1) expressing CHO cells compared to capsaicin | B | 9.89 | pKi | 0.13 | nM | Ki | J Med Chem (2003) 46: 3116-3126 [PMID:12825950] |
| ChEMBL | Binding affinity against Vanilloid receptor in dorsal Root Ganglion (DRG) membranes using [3H]RTX binding assay. | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (1996) 39: 2939-2952 [PMID:8709128] |
| ChEMBL | Displacement of [3H]RTX from rat TRV1 expressed in CHO cells by competitive binding assay | B | 10.37 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 299-302 [PMID:21111618] |
| ChEMBL | Displacement of [3H]RTX form rat TRPV1 receptor expressed in CHO/VR1 cell system | B | 10.37 | pKi | 0.04 | nM | Ki | Bioorg Med Chem (2009) 17: 690-698 [PMID:19135377] |
| ChEMBL | In vitro binding affinity towards vanilloid receptor by [3H]RTX displacement. | B | 10.64 | pKi | 0.02 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2909-2914 [PMID:10571146] |
| ChEMBL | Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranes | B | 10.7 | pKi | 0.02 | nM | Ki | J Med Chem (1996) 39: 3123-3131 [PMID:8759633] |
| ChEMBL | Binding affinity to rat TRPV1 | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7137-7141 [PMID:20947352] |
| GtoPdb | - | - | 7.5 | pEC50 | - | - | - | Nature (1997) 389: 816-24 [PMID:9349813] |
| ChEMBL | Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptake | F | 9.57 | pEC50 | 0.27 | nM | EC50 | Bioorg Med Chem (2009) 17: 690-698 [PMID:19135377] |
| ChEMBL | Agonist activity at rat TRPV1 expressed in CHO cells assessed as 45Ca2+ uptake | F | 9.57 | pEC50 | 0.27 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 299-302 [PMID:21111618] |
| Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388] | ||||||||
| GtoPdb | - | - | 5.1 | pIC50 | - | - | - | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
| Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142] | ||||||||
| GtoPdb | - | - | 4.5 | pKd | 31000 | nM | Kd | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
| Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460] | ||||||||
| GtoPdb | - | - | 4.6 | pKd | - | - | - | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
| Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2] | ||||||||
| GtoPdb | - | - | 4.7 | pIC50 | - | - | - | J Biol Chem (1998) 273: 5851-7 [PMID:9488722] |
| Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388] | ||||||||
| GtoPdb | - | - | 4.3 | 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]
