RS-127445 [Ligand Id: 188] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL473186 (RS-127445) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity to 5HT1B receptor (unknown origin) | B | 9.5 | pKi | 0.32 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3451-3454 [PMID:26227772] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 9.49 | pKi | 0.32 | nM | Ki |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Br J Pharmacol (1999) 127: 1075-82 [PMID:10455251] |
| ChEMBL | Binding affinity to 5-HT2B (unknown origin) assessed as inhibition constant | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| ChEMBL | Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin | F | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2206-2210 [PMID:19307114] |
| ChEMBL | Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay | F | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2206-2210 [PMID:19307114] |
| 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 6 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
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]
