E6801 [Ligand Id: 3217] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL362628 (E-6801) |
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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 | Antagonist activity at 5-HT6 receptor (unknown origin) | B | 6.51 | pKi | 312 | nM | Ki | Eur J Med Chem (2019) 162: 679-734 [PMID:30496988] |
| ChEMBL | Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2005) 48: 1781-1795 [PMID:15771424] |
| ChEMBL | Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2009) 52: 675-687 [PMID:19159187] |
| ChEMBL | Binding affinity to 5HT6 receptor | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2009) 52: 6153-6157 [PMID:19739674] |
| ChEMBL | Binding affinity to 5HT6 receptor | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem (2009) 17: 7387-7397 [PMID:19758807] |
| GtoPdb | - | - | 8.7 | pKi | 1.9 | nM | Ki | J Med Chem (2005) 48: 1781-95 [PMID:15771424] |
| ChEMBL | Agonist activity at human 5HT6 receptor expressed in HEK293F cells assessed as stimulation of cAMP level after 30 mins by HTRF assay Inhibition of rat adrenergic alpha1 receptor | F | 10.19 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2009) 52: 675-687 [PMID:19159187] |
| ChEMBL | Agonist activity at 5HT6 receptor | F | 10.19 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2009) 52: 6153-6157 [PMID:19739674] |
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]
