TD-8954 [Ligand Id: 8426] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2402904 (Felcisetrag, Tak-954, TAK-954, Td-8954, TD-8954, THRX-149699) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Binding affinity to human recombinant 5HT3 receptor | B | 4 | pKi | 100000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| GtoPdb | - | - | 9.4 | pKi | - | - | - | Bioorg Med Chem Lett (2013) 23: 4210-5 [PMID:23756062] |
| ChEMBL | Binding affinity to human recombinant 5HT4 receptor | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062] |
| ChEMBL | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay | F | 8.82 | pEC50 | 1.5 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
| ChEMBL | Agonist activity at human recombinant 5HT4 receptor assessed as cAMP accumulation | F | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Agonist activity at 5-HT4 receptor in guinea pig colon | B | 8.07 | pEC50 | 8.6 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
| ChEMBL | Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus | B | 8.6 | pEC50 | 2.51 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 4210-4215 [PMID:23756062] |
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]
