E6801 [Ligand Id: 3217] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL362628 (E-6801)
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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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 32:

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]