[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: 577-83 [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 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]
