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 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]
