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 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]
