olvanil [Ligand Id: 2488] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL76903 (NE-19550, Olvanil, TCMDC-124289) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2] | ||||||||
| ChEMBL | Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of CBD-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2018) 61: 8255-8281 [PMID:30176215] |
| ChEMBL | Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of LPC-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2018) 61: 8255-8281 [PMID:30176215] |
| TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
| GtoPdb | - | - | 7.7 | pEC50 | 19.9 | nM | EC50 | Eur J Pharmacol (2001) 417: 51-8 [PMID:11301059] |
| ChEMBL | Concentration necessary to induce a relative half-maximal response measured by the entry of [Ca2+] into human embryonic kidney HEK293 cells overexpressing the human VR1 | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2002) 45: 3739-3745 [PMID:12166946] |
| TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3] | ||||||||
| GtoPdb | - | - | 8.4 | 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 | Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells | B | 6.85 | pKi | 142 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 5227-5231 [PMID:22796184] |
| ChEMBL | Agonist activity at rat TRPV1 expressed in CHO cells assessed as calcium uptake | F | 6.69 | pEC50 | 202 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 5227-5231 [PMID:22796184] |
| GtoPdb | - | - | 8.1 | pEC50 | - | - | - | Br J Pharmacol (2000) 130: 916-22 [PMID:10864900] |
| GPR119 in Human [GtoPdb: 126] [UniProtKB: Q8TDV5] | ||||||||
| GtoPdb | - | - | 5.1 | pEC50 | - | - | - | Mol Endocrinol (2010) 24: 161-70 [PMID:19901198] |
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]
