tizanidine [Ligand Id: 7308] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1079 (Tizanidine, Zanaflex) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay | F | 6.58 | pEC50 | 264 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| Alpha-1B adrenergic receptor in Cricetulus griseus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988626] [UniProtKB: G3HDX1] | ||||||||
| ChEMBL | Agonist activity at hamster recombinant alpha-1B receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay | F | 6.49 | pEC50 | 322 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.6 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | increased cAMP generation | - | 5.8 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| ChEMBL | Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay | F | 7.07 | pEC50 | 86 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| GtoPdb | increased ERK1/2 phosphorylation | - | 8.4 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Agonist activity at human recombinant alpha-2C receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay | F | 5.91 | pEC50 | 1231 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| Nischarin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3923] [UniProtKB: Q9Y2I1] | ||||||||
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 7.55 | pKi | 28.31 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| ChEMBL | Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR | B | 7.55 | pKi | 28.3 | nM | Ki | Bioorg Med Chem (2008) 16: 7134-7140 [PMID:18621536] |
| α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | inhibition of forskolin stimulated cAMP generation | - | 7.8 | pIC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | cAMP generation | - | 6.3 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
| GtoPdb | ERK1/2 phosphorylation | - | 7 | pEC50 | - | - | - | Pharmacol Res Perspect (2022) 10: e01003 [PMID:36101495] |
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]
