velusetrag [Ligand Id: 8425] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2087337 (TD-5108, Velusetrag) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity to 5HT1D receptor | B | 7 | pKi | <100 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity to 5HT2A receptor | B | 7 | pKi | <100 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Binding affinity to 5HT2B receptor | B | 8.7 | pKi | <2 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity to 5HT2C receptor | B | 7 | pKi | <100 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - |
Bioorg Med Chem Lett (2012) 22: 6048-52 [PMID:22959244]; Naunyn Schmiedebergs Arch Pharmacol (2008) 378: 125-37 [PMID:18415081] |
| ChEMBL | Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| ChEMBL | Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP | F | 8.3 | pEC50 | 5.01 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| ChEMBL | Agonist activity at 5HT4c receptor expressed in cells at 100-fold physiological level assessed as cAMP accumulation | F | 9.2 | pEC50 | 0.63 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Agonist activity at 5HT4 receptor in guinea pig colonic longitudinal muscle/myenteric plexus assessed as contraction | F | 7.9 | pEC50 | 12.59 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinity to 5HT7 receptor | B | 7 | pKi | <100 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 6048-6052 [PMID:22959244] |
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]
