fluticasone propionate [Ligand Id: 7080] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1473 (Pirinase, Flovent diskus 50, CCI-18781, Sirdupla, Flutiform, Flixonase, Seretide 250, Flonase allergy relief, Xhance, Armonair digihaler, Flovent diskus 100, Sereflo, Seretide 125, Seretide 50, CCI 18781, Armonair respiclick, Seretide 500, Seretide 100, Opn-375, Fluticasone, Fluticasone propionate, Nasofan, Aerivio spiromax, FLOVENT, Flovent hfa, Flonase, Flovent diskus 250, Fluticasone propionate, Airflusal forspiro, Cutivate, Flovent, PF-00241939, Flixotide)
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
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  • Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
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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 pIC50 >10000 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 pIC50 >10000 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 pIC50 >10000 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 fluormone labelled GS Red from human recombinant glucocorticoid receptor after 2 hrs by fluorescence polarization assay B 9.05 pIC50 0.9 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb Inhibition of [3H]dexamethasone binding to recombinant human glucocorticoid receptor ecpressed in Tni cells. - 9.3 pIC50 0.5 nM IC50 J Med Chem (2000) 43: 19-21 [PMID:10633034]
ChEMBL Inhibition of [3H]dexamethasone binding to human Glucocorticoid Receptor B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2000) 43: 19-21 [PMID:10633034]
ChEMBL Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-stimulated IL-6 cytokine synthesis B 10.12 pIC50 0.07 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6343-6347 [PMID:21944381]
ChEMBL Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by LPS addition measured after 18 hrs by ELISA B 10.36 pIC50 0.04 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells expressing TRE-LacZ construct assessed as inhibition of AP-1 mediated TRE-LacZ activity after 24 hrs by beta-galactosidase reporter gene assay B 10.4 pIC50 0.04 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb - - 8.05 pEC50 9 nM EC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Agonist activity at GR in human SW1353 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity F 8.96 pEC50 1.09 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 5826-5830 [PMID:21880489]
ChEMBL Transactivation activity at glucocorticoid receptor in human HepG2 cells assessed as induction of tyrosine amino transferase B 9.15 pEC50 0.7 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 6343-6347 [PMID:21944381]
Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536]
ChEMBL Steroid binding against the rat thymus glucocorticoid receptor B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1996) 39: 4888-4896 [PMID:8960547]
ChEMBL Transrepression of glucocorticoid receptor in Wistar rat PBMC assessed as inhibition of LPS induced TNF alpha release preincubated for 45 mins followed by LPS addition measured after 18 hrs by ELISA B 9.85 pIC50 0.14 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
ChEMBL Transactivation activity at glucocorticoid receptor in rat H4II-E cells assessed as induction of tyrosine amino transferase B 9.12 pEC50 0.76 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 6343-6347 [PMID:21944381]
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 6.83 pIC50 149 nM IC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
GtoPdb - - 6.83 pEC50 149 nM EC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]
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]
GtoPdb - - 7.68 pEC50 21 nM EC50 J Med Chem (2017) 60: 8591-8605 [PMID:28937774]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]