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 | 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 | 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 | 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 | Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant | B | 9.24 | pKi | 0.58 | nM | Ki | Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086] |
| ChEMBL | Binding affinity to 5-HT6 receptor (unknown origin) | B | 9.24 | pKi | 0.58 | nM | Ki | J Med Chem (2024) 67: 1580-1610 [PMID:38190615] |
| 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 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]
