5-fluorotryptamine [Ligand Id: 146] 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: CHEMBL275628 (5-Fluorotryptamine)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
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
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 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]