velusetrag [Ligand Id: 8425] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2087337 (TD-5108, Velusetrag)
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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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 32:

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]