fluticasone furoate [Ligand Id: 10892] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1676 (Allermist, Arnuity ellipta, Avamys, Ennhale, Flonase sensimist allergy relief, Fluticasone furoate, Furamist, Furoate de fluticasone, Furoato de fluticasona, GSK 685 698, GSK-685968, GSK685968, GW-685698X, GW685698X, Relvar ellipta, Trelegy ellipta, Veramyst) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
| ChEMBL | Displacement of fluormone labelled AL green from rat recombinant His/GST-tagged androgen receptor LBD after 4 to 6 hrs by fluorescence polarization assay | B | 5.73 | pIC50 | 1880 | nM | IC50 | J Med Chem (2017) 60: 8591-8605 [PMID:28937774] |
| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| ChEMBL | Displacement of fluormone labelled EL Red from human recombinant estrogen receptor alpha after 1 to 5 hrs by fluorescence polarization assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8591-8605 [PMID:28937774] |
| Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] | ||||||||
| ChEMBL | Displacement of fluormone labelled EL Red from human recombinant estrogen receptor beta after 1 to 5 hrs by fluorescence polarization assay | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8591-8605 [PMID:28937774] |
| Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
| ChEMBL | Displacement of [3H]dexamethasone from human recombinant glucocorticoid receptor expressed in insect cells after 24 hrs by scintillation proximity assay | B | 9.29 | pKi | 0.51 | nM | Ki | J Med Chem (2018) 61: 4757-4773 [PMID:29741897] |
| ChEMBL | Displacement of fluormone labelled GS Red from human recombinant glucocorticoid receptor after 2 hrs by fluorescence polarization assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2017) 60: 8591-8605 [PMID:28937774] |
| ChEMBL | Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay | F | 10.4 | pIC50 | 0.04 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4846-4850 [PMID:19592247] |
| ChEMBL | Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity | F | 9.31 | pEC50 | 0.49 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 5826-5830 [PMID:21880489] |
| ChEMBL | Induction of nuclear translocation of human recombinant ProLabel-tagged glucocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method | B | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2018) 61: 4757-4773 [PMID:29741897] |
| Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] | ||||||||
| ChEMBL | Displacement of [3H]-aldosterone from N terminal maltose binding protein tagged human mineralocorticoid receptor LBD (726 to 984 residues) expressed in baculovirus infected high five cells after 8 hrs by scintillation proximity assay | B | 6.78 | pIC50 | 166 | nM | IC50 | J Med Chem (2017) 60: 8591-8605 [PMID:28937774] |
| ChEMBL | Induction of nuclear translocation of human recombinant ProLabel-tagged mineralocorticoid receptor expressed in CHO-K1 cells after 3 hrs by luminescence method | B | 5.52 | pEC50 | >3000 | nM | EC50 | J Med Chem (2018) 61: 4757-4773 [PMID:29741897] |
| Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
| ChEMBL | Displacement of fluormone labelled PL Red from human recombinant progesterone receptor after 1 to 6 hrs ligand by fluorescence polarization assay | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2017) 60: 8591-8605 [PMID:28937774] |
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]
