lofexidine [Ligand Id: 9868] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL17860 (Lofexidine)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
1 CHEMBL17860_lig_chart_1 Alpha-2a adrenergic receptor Human
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
2 CHEMBL17860_lig_chart_2 Alpha-2b adrenergic receptor Human
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
3 CHEMBL17860_lig_chart_3 Alpha-2c adrenergic receptor Human
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  • Nischarin in Rat [ChEMBL: CHEMBL5221] [UniProtKB: Q4G017]
  • This target only has 1 pki data point
4 CHEMBL17860_lig_chart_4 Nischarin Rat
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • This target only has 1 pki data point
5 CHEMBL17860_lig_chart_5 Serotonin 1a (5-HT1a) receptor Human
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]