5-fluorotryptamine [Ligand Id: 146] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL275628 (5-Fluorotryptamine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Induction of DAT-mediated dopamine release in rat brain synaptosomes by [3H]DA release assay | B | 7.08 | pEC50 | 82.3 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| myeloperoxidase/Myeloperoxidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2439] [GtoPdb: 2789] [UniProtKB: P05164] | ||||||||
| ChEMBL | Inhibition of recombinant MPO mediated LDL oxidation using MPO/Cl-/H2O2 system | B | 6.03 | pIC50 | 940 | nM | IC50 | J Med Chem (2010) 53: 8747-8759 [PMID:21090682] |
| ChEMBL | Inhibition of recombinant human myeloperoxidase | B | 6.1 | pIC50 | 790 | nM | IC50 | J Med Chem (2012) 55: 7208-7218 [PMID:22793255] |
| ChEMBL | Inhibition of recombinant MPO mediated taurine chlorination by microplate reader method | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2010) 53: 8747-8759 [PMID:21090682] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | Induction of NET-mediated norepinephrine release in rat brain synaptosomes by [3H]NE release assay | B | 6.33 | pEC50 | 464 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Agonist activity at 5HT2A receptor (unknown origin) by cell based calcium mobilization assay | F | 8.58 | pEC50 | 2.64 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Induction of 5-HTT-mediated 5-HT release in rat brain synaptosomes by [3H]5-HT release assay | B | 8 | pEC50 | 10.1 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4754-4758 [PMID:25193229] |
| TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
| ChEMBL | Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of icilin-induced 45calcium influx treated 5 mins before icilin challenge measured after 5 mins | F | 4.88 | pIC50 | 13100 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7076-7079 [PMID:20965726] |
| ChEMBL | Antagonist activity at human TRPM8 receptor expressed in human T-REx-293 cells assessed as inhibition of menthol-induced 45calcium influx treated 5 mins before menthol challenge measured after 5 mins | F | 4.91 | pIC50 | 12300 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 7076-7079 [PMID:20965726] |
| 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596] |
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]
