JYL1421 [Ligand Id: 4230] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL388824 (SC-0030, SC0030) |
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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 | Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of capsaicin-induced activity by FLIPR assay | F | 7.59 | pKi | 26 | nM | Ki | J Med Chem (2012) 55: 8392-8408 [PMID:22957803] |
| ChEMBL | Concentration required to inhibit [3H]RTX radioligand binding towards transient receptor potential cation channel (subfamily V, member 1) expressed in chinese hamster ovary cells | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2005) 48: 5823-5836 [PMID:16134949] |
| ChEMBL | Antagonist activity at TRPV1 (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2023) 245: 114893-114893 [PMID:36395649] |
| ChEMBL | Concentration required to antagonized capsaicin-induced calcium uptake at the transient receptor potential cation channel (subfamily V member 1) expressed in chinese hamster ovary cells | B | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2005) 48: 5823-5836 [PMID:16134949] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX | B | 7.27 | pKi | 53.5 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4136-4142 [PMID:16005215] |
| ChEMBL | In vitro inhibition of [3H]RTX binding to rat TRPV1 expressed in CHO cells | B | 7.27 | pKi | 53.5 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4143-4150 [PMID:15993063] |
| ChEMBL | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells | B | 7.27 | pKi | 53.5 | nM | Ki | Bioorg Med Chem (2007) 15: 6043-6053 [PMID:17629487] |
| ChEMBL | Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells after 60 mins by scintillation counting | B | 7.27 | pKi | 53.5 | nM | Ki | Bioorg Med Chem (2012) 20: 215-224 [PMID:22169633] |
| ChEMBL | Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as decrease in capsaicin-induced intracellular 45Ca2+ uptake after 1 hr by fluorometric analysis | F | 8.04 | pKi | 9.2 | nM | Ki | Bioorg Med Chem (2012) 20: 215-224 [PMID:22169633] |
| ChEMBL | Antagonist activity at rat TRPV1 receptor expressed in CHO cells by Ca2+ uptake assay | F | 8.04 | pKi | 9.2 | nM | Ki | Bioorg Med Chem (2007) 15: 6043-6053 [PMID:17629487] |
| ChEMBL | Antagonist activity for rat TRPV1 expressed in CHO cells | F | 8.04 | pKi | 9.16 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4136-4142 [PMID:16005215] |
| ChEMBL | Antagonist activity towards rat TRPV1 expressed in CHO cells | F | 8.04 | pKi | 9.16 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4143-4150 [PMID:15993063] |
| ChEMBL | Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as reduction of capsaicin-stimulated intracellular 45Ca2+ influx by scintillation counting | F | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2010) 18: 111-116 [PMID:19931463] |
| ChEMBL | Inhibitory effect on capsaicin (0.5 uM)-induced calcium uptake in rat DRG neurons upon incubation at RT for 10 minutes | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2005) 48: 5823-5836 [PMID:16134949] |
| ChEMBL | Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as reduction of capsaicin-stimulated 45Ca2+ uptake | F | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2009) 17: 3557-3567 [PMID:19398205] |
| ChEMBL | Antagonist activity at TRPV1 in Sprague-Dawley rat DRG neurons assessed as inhibition of capsaicin-induced [45]Ca2+ uptake | F | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2009) 17: 8149-8160 [PMID:19897373] |
| GtoPdb | - | - | 8 | pIC50 | 9.2 | nM | IC50 | Mol Pharmacol (2002) 62: 947-56 [PMID:12237342] |
| ChEMBL | Agonist activity at TRPV1 in Sprague-Dawley rat DRG neuron assessed as intracellular 45Ca2+ influx by scintillation counting | F | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem (2010) 18: 111-116 [PMID:19931463] |
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]
