5'-iodoresiniferatoxin [Ligand Id: 4109] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL595069 (5-Iodoresiniferatoxin, 5-Iodo-Resiniferatoxin, Iodoresiniferatoxin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| ChEMBL | Displacement of [3H]RTX from human TRPV1 expressed in CHO cells | B | 7.93 | pKi | 11.8 | 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 | 7.93 | pKi | 11.8 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 382-385 [PMID:24321344] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of RTX-induced 45Ca2+ uptake after 20 mins by liquid scintillation counting analysis | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 382-385 [PMID:24321344] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-stimulated Ca2+ uptake | B | 8.23 | pKi | 5.87 | nM | Ki | Eur J Med Chem (2013) 68: 233-243 [PMID:23981530] |
| ChEMBL | Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of intracellular calcium level | F | 5.4 | pIC50 | 4000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 97-99 [PMID:19951840] |
| GtoPdb | - | - | 8.4 | pIC50 | 3.9 | nM | IC50 | |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium 45 uptake | F | 7.91 | pKi | 12.2 | nM | Ki | J Med Chem (2008) 51: 57-67 [PMID:18072720] |
| ChEMBL | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells | B | 9.21 | pKi | 0.61 | nM | Ki | J Med Chem (2008) 51: 57-67 [PMID:18072720] |
ChEMBL data shown on this page come from version 33:
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]
