lofexidine [Ligand Id: 9868] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL17860 (Lofexidine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | Calculated from [3H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α2A-AR. | - | 8.36 | pKi | 4.36 | nM | Ki | Bioorg Med Chem (2012) 20: 2082-90 [PMID:22341244] |
| ChEMBL | Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A expressed in CHO cells | B | 8.36 | pKi | 4.37 | nM | Ki | Bioorg Med Chem (2012) 20: 2082-2090 [PMID:22341244] |
| ChEMBL | Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis | F | 8.2 | pEC50 | 6.31 | nM | EC50 | Bioorg Med Chem (2012) 20: 2082-2090 [PMID:22341244] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2B expressed in CHO cells | B | 7.17 | pKi | 67.61 | nM | Ki | Bioorg Med Chem (2012) 20: 2082-2090 [PMID:22341244] |
| GtoPdb | Calculated from [3H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α2B-AR. | - | 7.17 | pKi | 67.7 | nM | Ki | Bioorg Med Chem (2012) 20: 2082-90 [PMID:22341244] |
| ChEMBL | Agonist activity at human adrenoceptor aplha 2B expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis | F | 6.9 | pEC50 | 125.89 | nM | EC50 | Bioorg Med Chem (2012) 20: 2082-2090 [PMID:22341244] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | Calculated from [3H]RS-79948-197 radioligand competition binding to membrane preparations from CHO cells expressing human α2C-AR. | - | 7.16 | pKi | 69.2 | nM | Ki | Bioorg Med Chem (2012) 20: 2082-90 [PMID:22341244] |
| ChEMBL | Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C expressed in CHO cells | B | 7.16 | pKi | 69.18 | nM | Ki | Bioorg Med Chem (2012) 20: 2082-2090 [PMID:22341244] |
| ChEMBL | Agonist activity at human adrenoceptor aplha 2C expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis | F | 8.86 | pEC50 | 1.38 | nM | EC50 | Bioorg Med Chem (2012) 20: 2082-2090 [PMID:22341244] |
| Nischarin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017] | ||||||||
| ChEMBL | Displacement of [125I]PIC from Imidazoline-1 receptor in rat PC12 cell membrane incubated for 30 mins by gamma counting method | B | 8.25 | pKi | 5.62 | nM | Ki | Bioorg Med Chem (2016) 24: 3174-3183 [PMID:27265687] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in HeLa cells after 30 mins | B | 6.9 | pKi | 125.89 | nM | Ki | ACS Med Chem Lett (2012) 3: 535-539 [PMID:24900506] |
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]
