[3H]Ro 63-0563 [Ligand Id: 3246] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL46071 (Ro-63-0563)
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 8.3 pKd 5 nM Kd Mol Pharmacol (1998) 54: 577-583 [PMID:9730917]
ChEMBL Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells B 6.29 pKi 512 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 738-743 [PMID:18053713]
ChEMBL Binding affinity to 5HT6 receptor B 7.8 pKi 15.85 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 698-703 [PMID:21190848]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor B 7.8 pKi 15.85 nM Ki J. Med. Chem. (2005) 48: 4216-4219 [PMID:15974573]
ChEMBL Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells B 7.83 pKi 14.8 nM Ki J. Med. Chem. (2005) 48: 1781-1795 [PMID:15771424]
ChEMBL Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells B 7.9 pKi 12.6 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1719-1721 [PMID:10937732]
ChEMBL Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD B 7.9 pKi 12.59 nM Ki J. Med. Chem. (1999) 42: 202-205 [PMID:9925723]
ChEMBL Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis B 7.91 pKi 12.3 nM Ki J. Med. Chem. (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 7.92 pKi 12 nM Ki J. Med. Chem. (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 3214-3216 [PMID:19433358]
ChEMBL Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis B 7.92 pKi 12 nM Ki J. Med. Chem. (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells B 7.92 pKi 12 nM Ki J. Med. Chem. (2014) 57: 7160-7181 [PMID:24850589]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]