SB399885 [Ligand Id: 3241] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1210710 (SB-399885)
  • 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]
GtoPdb - - 9 pKi 1 nM Ki Eur J Pharmacol (2006) 553: 109-19 [PMID:17069795]
ChEMBL Antagonist activity at 5-HT6 receptor (unknown origin) B 9.1 pKi 0.8 nM Ki Bioorg Med Chem (2013) 21: 4614-4627 [PMID:23787290]
ChEMBL Displacement of [125I]SB-258585 from human recombinant 5HT6 receptor using methiothepin after 45 mins by liquid scintillation spectrometry B 9.11 pKi 0.78 nM Ki Bioorg Med Chem (2011) 19: 5255-5259 [PMID:21821420]
ChEMBL Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells B 9.14 pKi 0.72 nM Ki Eur J Med Chem (2017) 135: 117-124 [PMID:28441580]
ChEMBL Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells B 9.15 pKi 0.7 nM Ki J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
ChEMBL Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method B 9.15 pKi 0.7 nM Ki J Med Chem (2021) 64: 13279-13298 [PMID:34467765]
ChEMBL Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay F 7.01 pIC50 97 nM IC50 J Med Chem (2021) 64: 13279-13298 [PMID:34467765]

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]