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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 |
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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]