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 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]
