RS 39604 [Ligand Id: 254] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL83954 (RS-23597-190) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| 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 | 5.7 | pKi | 1995.26 | 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 | Binding affinity at 5HT4 receptor | B | 7.5 | pKi | 31.62 | nM | Ki | Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Br J Pharmacol (2000) 129: 771-81 [PMID:10683202]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]; Br J Pharmacol (2004) 143: 361-70 [PMID:15351779] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand | B | 7.55 | pKi | 28.1 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting | B | 7.72 | pKi | 19 | nM | Ki | Medchemcomm (2017) 8: 647-651 [PMID:30108781] |
| ChEMBL | Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method | B | 7.72 | pKi | 19 | nM | Ki | Medchemcomm (2018) 9: 1466-1471 [PMID:30288221] |
| ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
ChEMBL data shown on this page come from version 35:
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]
