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ChEMBL ligand: CHEMBL1210710 (SB-399885) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]