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 | 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 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]
