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 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]
