Ro 63-0563 [Ligand Id: 275] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL46071 (Ro-63-0563)
  • 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]
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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 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]
GtoPdb - - 8.4 pKi 3.98 nM Ki Mol Pharmacol (1998) 54: 577-583 [PMID:9730917];
Br J Pharmacol (1998) 124: 556-62 [PMID:9647481]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 8 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 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]