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 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]
