prucalopride [Ligand Id: 243] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL117287 (Prucalopride, R-093877, R093877, Resolor) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 at 5HT3 receptor | B | 5.4 | pKi | 3981.07 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Tested for selectivity for 5-hydroxytryptamine 4 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| ChEMBL | Tested for selectivity for 5-hydroxytryptamine 4 receptor | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| ChEMBL | Tested for selectivity for 5-hydroxytryptamine 4 receptor | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| ChEMBL | Tested for agonist activity against 5-hydroxytryptamine 4 receptor | F | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| ChEMBL | Binding affinity at 5HT4 receptor | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - |
J Neurochem (2000) 74: 478-89 [PMID:10646498]; Eur J Pharmacol (2001) 423: 71-83 [PMID:11438309] |
| ChEMBL | Agonist activity at 5-HT4E receptor (unknown origin) | B | 7.59 | pEC50 | 26 | nM | EC50 | J Med Chem (2018) 61: 4993-5008 [PMID:29763304] |
| ChEMBL | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay | F | 8.28 | pEC50 | 5.2 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
| ChEMBL | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay | B | 8.28 | pEC50 | 5.2 | nM | EC50 | J Med Chem (2018) 61: 4993-5008 [PMID:29763304] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay | F | 7.59 | pEC50 | 26 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
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]
