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ChEMBL ligand: CHEMBL1473 (Aerivio spiromax, Airflusal forspiro, Armonair digihaler, Armonair respiclick, CCI 18781, CCI-18781, CCI18781, Cutivate, Flixonase, Flixotide, Flonase, Flonase allergy relief, Flovent, FLOVENT, Flovent diskus 100, Flovent diskus 250, Flovent diskus 50, Flovent hfa, Fluticaps, Fluticasone, Fluticasone-17-propionate, Fluticasone propionate, Fluticasone propionate, Flutiform, Nasofan, NSC-759889, Opn-375, Optinose, PF-00241939, Pirinase, R01AD08, Sereflo, Seretide 100, Seretide 125, Seretide 250, Seretide 50, Seretide 500, Sirdupla, Xhance) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]