[3H]Ro 63-0563 [Ligand Id: 3246] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL46071 (Ro-63-0563) |
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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] | ||||||||
| 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 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]
