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] |
| ChEMBL | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay | B | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2021) 64: 10641-10665 [PMID:34251799] |
| 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 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]
