SB258585 [Ligand Id: 3232] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL60264 (SB-258585) |
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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 | - | - | 8.53 | pKi | - | - | - | Br J Pharmacol (2000) 130: 1597-605 [PMID:10928963] |
| ChEMBL | Binding affinity against human cloned 5-hydroxytryptamine 6 receptor in HeLa cells using [3H]LSD | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (1999) 42: 202-205 [PMID:9925723] |
| ChEMBL | Binding affinity for human 5-hydroxytryptamine 6 receptor | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2005) 48: 4216-4219 [PMID:15974573] |
| ChEMBL | Antagonist activity at human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation pretreated for 10 mins before 5-HT addition measured after 30 mins | F | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4696-4700 [PMID:23820387] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075268] [GtoPdb: 11] [UniProtKB: Q9R1C8] | ||||||||
| ChEMBL | Antagonist activity at mouse 5HT6 receptor F6.52A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay | F | 6.94 | pKi | 114 | nM | Ki | J Med Chem (2010) 53: 1357-1369 [PMID:20078106] |
| ChEMBL | Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay | F | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2010) 53: 1357-1369 [PMID:20078106] |
| ChEMBL | Antagonist activity at mouse wild type 5HT6 receptor expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay | F | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (2010) 53: 1357-1369 [PMID:20078106] |
| ChEMBL | Antagonist activity at mouse 5HT6 receptor W6.48A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay | F | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2010) 53: 1357-1369 [PMID:20078106] |
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]
