lofexidine [Ligand Id: 9868] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL17860 (Lofexidina, 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 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]
