Ro 04-6790 [Ligand Id: 274] 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: CHEMBL433461 (Ro-046790)
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
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]
ChEMBL Binding affinity to 5-HT6 receptor (unknown origin) B 7.24 pKi 58 nM Ki Med Chem Res (2005) 14: 1-18
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells B 7.26 pKi 55 nM Ki Bioorg Med Chem Lett (2009) 19: 3214-3216 [PMID:19433358]
ChEMBL Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells B 7.26 pKi 55 nM Ki J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 6 receptor B 7.26 pKi 55 nM Ki J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells B 7.26 pKi 55 nM Ki Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
ChEMBL Binding affinity to human 5HT6R B 7.26 pKi 54.95 nM Ki Eur J Med Chem (2017) 135: 117-124 [PMID:28441580]
ChEMBL Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD B 7.3 pKi 50.12 nM Ki J Med Chem (1999) 42: 202-205 [PMID:9925723]
ChEMBL Binding affinity for human 5-hydroxytryptamine 6 receptor B 7.3 pKi 50.12 nM Ki J Med Chem (2005) 48: 4216-4219 [PMID:15974573]
ChEMBL Binding affinity to 5HT6 receptor B 7.3 pKi 50.12 nM Ki Bioorg Med Chem Lett (2011) 21: 698-703 [PMID:21190848]
ChEMBL Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells B 7.3 pKi 50 nM Ki Bioorg Med Chem Lett (2000) 10: 1719-1721 [PMID:10937732]
ChEMBL Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting B 7.33 pKi 47 nM Ki J Med Chem (2009) 52: 675-687 [PMID:19159187]
ChEMBL Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells B 7.35 pKi 44.7 nM Ki J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
GtoPdb - - 7.9 pKi - - - Mol Pharmacol (1998) 54: 577-583 [PMID:9730917];
Br J Pharmacol (1998) 124: 556-62 [PMID:9647481]
ChEMBL Binding affinity towards 5-hydroxytryptamine 6 receptor using [3H]- LSD as radioligand B 7.58 pIC50 26.3 nM IC50 J Med Chem (2003) 46: 4834-4837 [PMID:14584934]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.6 pKi - - - Mol Pharmacol (1998) 54: 577-583 [PMID:9730917];
Br J Pharmacol (1998) 124: 556-62 [PMID:9647481]

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]