donecopride [Ligand Id: 10584] 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: CHEMBL3417009 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | Inhibition of AChE (unknown origin) | B | 7.8 | pKi | 16 | nM | Ki | Eur J Med Chem (2019) 162: 234-248 [PMID:30447434] |
| ChEMBL | Inhibition of human erythrocyte AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate by Ellman' method | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2015) 58: 3172-3187 [PMID:25793650] |
| ChEMBL | Mixed type competitive inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured every 1 min for 10 mins by Ellman's method | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2018) 158: 463-477 [PMID:30243151] |
| ChEMBL | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition by Ellman's method | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2019) 169: 200-223 [PMID:30884327] |
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | Proc Natl Acad Sci USA (2014) 111: E3825-30 [PMID:25157130] |
| Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
| ChEMBL | Inhibition of equine serum BuChE pre-incubated for 5 mins before butyrylthiocholine iodide substrate by Ellman' method | B | 5.45 | pIC50 | 3530 | nM | IC50 | J Med Chem (2015) 58: 3172-3187 [PMID:25793650] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Agonist activity at 5-HT4R (unknown origin) | B | 7.98 | pKi | 10.4 | nM | Ki | Eur J Med Chem (2019) 162: 234-248 [PMID:30447434] |
| ChEMBL | Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins | B | 8.02 | pKi | 9.5 | nM | Ki | Eur J Med Chem (2019) 162: 234-248 [PMID:30447434] |
| ChEMBL | Displacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding method | B | 8.18 | pKi | 6.6 | nM | Ki | Eur J Med Chem (2019) 169: 200-223 [PMID:30884327] |
| ChEMBL | Activity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha release | B | 7.95 | pEC50 | 11.3 | nM | EC50 | J Med Chem (2015) 58: 3172-3187 [PMID:25793650] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay | B | 8.18 | pKi | 6.6 | nM | Ki | J Med Chem (2015) 58: 3172-3187 [PMID:25793650] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method | B | 7.29 | pKi | 51 | nM | Ki | Eur J Med Chem (2019) 162: 234-248 [PMID:30447434] |
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]
