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