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, 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 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]
