RS 67333 [Ligand Id: 237] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL85251 (RS-67333) |
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| 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 human erythrocyte AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate by Ellman' method | B | 6.39 | pIC50 | 403 | nM | IC50 | J Med Chem (2015) 58: 3172-3187 [PMID:25793650] |
| ChEMBL | 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 | 6.39 | pIC50 | 403 | nM | IC50 | Eur J Med Chem (2018) 158: 463-477 [PMID:30243151] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins | B | 8.03 | pKi | 9.33 | nM | Ki | Eur J Med Chem (2019) 162: 234-248 [PMID:30447434] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Br J Pharmacol (2000) 129: 771-81 [PMID:10683202]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734] |
| ChEMBL | Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae | F | 8.4 | pEC50 | 3.98 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 2477-2480 |
| ChEMBL | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Agonist activity at 5-HT4 receptor in Sprague-Dawley rat oesophagus assessed as relaxation of carbachol precontracted oesophagus | B | 8.06 | pEC50 | 8.7 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
| 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 | 8.03 | pKi | 9.3 | nM | Ki | J Med Chem (2015) 58: 3172-3187 [PMID:25793650] |
| ChEMBL | Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method | B | 8.41 | pKi | 3.9 | nM | Ki | Medchemcomm (2018) 9: 1466-1471 [PMID:30288221] |
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]
