prednisolone [Ligand Id: 2866] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL131 (Verdeso, Deltalone, Hydeltra-Tba, Poly-Pred, Desowen, Prednisolone, Tridesilon, NSC-9120, Neo-Delta-Cortef, Fernisolone-p, Pred-G, Cortalone, Deltacortril, Precortisyl, Pevanti, Prelone, Dekotil, Dilacort, NSC-9900, Delta-cortef, Hydeltra, Precortisyl fte, Scheriproct, Meticortelone, Meti-derm, Sterane, Servisone)
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
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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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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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  • GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ADAM17 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536]
ChEMBL Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR. B 7.83 pIC50 14.9 nM IC50 US-8901310-B2. Tricyclic compounds, compositions, and methods (2014)
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Binding affinity for androgen receptor B 5.56 pKi 2762 nM Ki J. Med. Chem. (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL Binding affinity towards testosterone receptor B 5.56 pKi 2760 nM Ki J. Med. Chem. (2003) 46: 1016-1030 [PMID:12620078]
ChEMBL Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells B 5.6 pKi 2520 nM Ki J. Med. Chem. (2014) 57: 849-860 [PMID:24446728]
ChEMBL Displacement of [3H]methyltrienolone from androgen receptor in human LNCaP cells after 1440 mins by scintillation counting method B 4.47 pIC50 34000 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Binding affinity to AR (unknown origin) by FP assay B 5.7 pIC50 >2000 nM IC50 Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) B 4.37 pIC50 >42657.95 nM IC50 J. Med. Chem. (2005) 48: 5666-5674 [PMID:16134935]
Corticosteroid binding globulin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2421] [UniProtKB: P08185]
ChEMBL In silico binding affinity to human corticosteriod binding globulin B 6.51 pKd 6.51 - -Log Kdiss J. Med. Chem. (1997) 40: 3161-3172 [PMID:9379435]
ChEMBL Binding affinity to human CBG receptor (corticosteroid-binding globulins) B 7.51 pKi 30.9 nM Ki J. Med. Chem. (2004) 47: 2732-2742 [PMID:15139751]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL Binding affinity to ERalpha by fluorescence polarization assay B 5.3 pKi >5000 nM Ki J. Med. Chem. (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL Displacement of fluorescently labeled ligand from ERalpha receptor by fluorescence polarization assay B 5.3 pKi >5000 nM Ki J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Binding affinity to human ERalpha expressed in Sf9 cells by fluoligand binding-based fluorescence polarization method B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Binding affinity to ERalpha (unknown origin) by FP assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
ChEMBL Binding affinity to human ERbeta expressed in Sf9 cells by fluoligand binding-based fluorescence polarization method B 4 pIC50 >100000 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Binding affinity to ERbeta (unknown origin) by FP assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 5.58 pKi 2660 nM Ki J. Med. Chem. (2008) 51: 3755-3764 [PMID:18533710]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 8.13 pKi 7.4 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Displacement of radiolabeled Dexamethasone from GR B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1658-1662 [PMID:21349714]
ChEMBL Displacement of radiolabeled Dexamethasone from GR B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1697-1700 [PMID:21316964]
ChEMBL Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 168-171 [PMID:21115247]
ChEMBL Displacement of radiolabeled Dexamethasone from glucocorticoid receptor B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 3504-3508 [PMID:18513967]
ChEMBL Displacement of radiolabeled Dexamethasone from glucocorticoid receptor B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 4158-4162 [PMID:17553679]
ChEMBL Displacement of radiolabeled Dexamethasone from glucocorticoid receptor expressed in baculovirus B 8.28 pKi 5.3 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1654-1657 [PMID:21324689]
ChEMBL Binding affinity towards human glucocorticoid receptor (GR) was determined using [3H]dexamethasone as radioligand in SF-1 cells B 8.62 pKi 2.4 nM Ki J. Med. Chem. (2003) 46: 1016-1030 [PMID:12620078]
ChEMBL Binding affinity towards glucocorticoid receptor (GR) by displacing [3H]dexamethasone B 8.62 pKi 2.4 nM Ki J. Med. Chem. (2001) 44: 4481-4491 [PMID:11728194]
ChEMBL Binding affinity for glucocorticoid receptor B 8.62 pKi 2.4 nM Ki J. Med. Chem. (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL Displacement of [3H]DEX from human glucocorticoid receptor B 8.62 pKi 2.4 nM Ki J. Med. Chem. (2010) 53: 3065-3074 [PMID:20334371]
GtoPdb - - 8.62 pKi 2.4 nM Ki J Med Chem (2001) 44: 2879-85 [PMID:11520196]
ChEMBL Displacement of GS-red from GRapha by fluorescence polarization assay B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assay B 8.82 pKi 1.5 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2139-2143 [PMID:19321341]
ChEMBL Displacement of GS-red from glucocorticoid receptor by fluorescence polarization assay B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells B 8.94 pKi 1.14 nM Ki J. Med. Chem. (2014) 57: 849-860 [PMID:24446728]
ChEMBL Antagonist activity at GR assessed as inhibition of dexamethasone-induced GRE activation F 6 pIC50 >1000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4158-4162 [PMID:17553679]
ChEMBL Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition after 18 hrs by AlphaLISA method B 6.52 pIC50 300 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Glucocorticoid-induced aromatase activity in human skin fibroblasts F 7.39 pIC50 41 nM IC50 J. Med. Chem. (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay B 7.4 pIC50 40 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA B 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 168-171 [PMID:21115247]
ChEMBL Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression by ELISA B 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1654-1657 [PMID:21324689]
ChEMBL Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone F 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1697-1700 [PMID:21316964]
ChEMBL Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA B 7.64 pIC50 23 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1658-1662 [PMID:21349714]
ChEMBL DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) B 7.8 pIC50 16 nM IC50 DrugMatrix in vitro pharmacology data
GtoPdb - - 7.8 pIC50 15.8 nM IC50 J Biol Chem (2000) 275: 19041-9 [PMID:10747884]
ChEMBL Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2010) 53: 6681-6698 [PMID:20735001]
ChEMBL Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assay B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1934-1940 [PMID:24656565]
ChEMBL Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay B 7.82 pIC50 15 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay B 7.82 pIC50 15 nM IC50 J. Med. Chem. (2006) 49: 7887-7896 [PMID:17181172]
ChEMBL Inhibition of human glucocorticoid receptor alpha by displacement of [3H]dexamethasone B 7.86 pIC50 13.8 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2163-2167 [PMID:15808489]
ChEMBL Inhibition of human Glucocorticoid receptor B 7.86 pIC50 13.8 nM IC50 J. Med. Chem. (2004) 47: 2441-2452 [PMID:15115388]
ChEMBL Displacement of [3H]dexamethasone from GR in human IM9 cells after 6 hrs by scintillation counting method B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2019) 161: 354-363 [PMID:30384041]
ChEMBL Displacement of fluorescent labelled Dexamethasone from glucocorticoid receptor B 7.9 pIC50 12.59 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 158-162 [PMID:19019676]
ChEMBL Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay F 8.07 pIC50 8.51 nM IC50 J. Med. Chem. (2007) 50: 6519-6534 [PMID:18038970]
ChEMBL Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells F 8.07 pIC50 8.51 nM IC50 J. Med. Chem. (2006) 49: 4216-4231 [PMID:16821781]
ChEMBL Inhibition of transcriptional activation in CV-1 cells expressing glucocorticoid receptor F 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1721-1727 [PMID:15026058]
ChEMBL Transcriptional activation in CV-1 cells expressing glucocorticoid receptor F 8.1 pIC50 8 nM IC50 J. Med. Chem. (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-stimulated IL-8 production B 8.11 pIC50 7.7 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1086-1090 [PMID:22197391]
GtoPdb Binding to human GR in vitro. - 8.15 pIC50 7 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay B 8.15 pIC50 7 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL1-induced IL-6 production after 18 to 24 hrs F 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL Binding affinity to human glucocorticoid receptor by fluorescence polarization competitive binding assay B 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 3017-3020 [PMID:20427184]
ChEMBL Transrepression activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 18 to 24 hrs by ELISA B 8.18 pIC50 6.6 nM IC50 J. Med. Chem. (2010) 53: 6681-6698 [PMID:20735001]
ChEMBL Binding affinity to GR (unknown origin) by FP assay B 8.21 pIC50 6.1 nM IC50 Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
ChEMBL Agonist activity at glucocorticoid receptor in human foreskin fibroblasts assessed as inhibition of IL-1-induced IL-6 production by trans-repression assay B 8.22 pIC50 6 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1934-1940 [PMID:24656565]
ChEMBL Activity at glucocorticoid receptor assessed as repression of TNFalpha and IL1 beta-induced E-selectin expression B 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3504-3508 [PMID:18513967]
ChEMBL Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay B 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 168-171 [PMID:21115247]
ChEMBL Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone F 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1697-1700 [PMID:21316964]
ChEMBL Activity at GR assessed as repression of TNFalpha and IL 1-beta induced E-selectin response F 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 4158-4162 [PMID:17553679]
ChEMBL Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-selectin repression by luciferase reporter gene assay B 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1654-1657 [PMID:21324689]
ChEMBL Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay B 8.39 pIC50 4.1 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1658-1662 [PMID:21349714]
ChEMBL Repression activity of GR ligand with interleukin-6 receptor in native cell assay using Dexamethasone was determined as maximal potency F 8.42 pIC50 3.8 nM IC50 J. Med. Chem. (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL Transcriptional repression activity in HEP G2 cells expressing glucocorticoid receptor compared to Dexamethasone F 8.68 pIC50 2.1 nM IC50 J. Med. Chem. (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL Inhibition of transcriptional repression in CV-1 cells expressing glucocorticoid receptor F 8.68 pIC50 2.1 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1721-1727 [PMID:15026058]
ChEMBL Antagonist activity at glucocorticoid receptor assessed as inhibition of dexamethasone-induced glucose response element transcriptional transactivation by luciferase assay F 9 pIC50 >1 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 3504-3508 [PMID:18513967]
ChEMBL Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR. B 9.28 pIC50 0.53 nM IC50 US-8901310-B2. Tricyclic compounds, compositions, and methods (2014)
ChEMBL Glucocorticoid induced transactivation of human tyrosine amino transferase in HepG2 cells F 6.68 pEC50 211 nM EC50 J. Med. Chem. (2004) 47: 2441-2452 [PMID:15115388]
ChEMBL Transactivation activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells incubated for 24 hrs by beta-galactosidase reporter gene assay B 6.96 pEC50 110 nM EC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay B 7.08 pEC50 82.7 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2139-2143 [PMID:19321341]
ChEMBL Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay B 7.08 pEC50 82.7 nM EC50 J. Med. Chem. (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay B 7.13 pEC50 73.9 nM EC50 J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry B 7.19 pEC50 64 nM EC50 J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs B 7.24 pEC50 57.4 nM EC50 J. Med. Chem. (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL Agonist activity at glucocorticoid receptor in human MDA-kb2 cells transfected with MMTV-LUC assessed as induction of MMTV-LTR/promoter linked LUC gene by luciferase transactivation assay F 7.26 pEC50 55 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 3017-3020 [PMID:20427184]
ChEMBL Agonist activity at human glucocorticoid receptor in human A549 cells assessed as transcriptional activity by MMTV luciferase reporter gene assay F 7.3 pEC50 50.12 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 158-162 [PMID:19019676]
ChEMBL Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay F 7.5 pEC50 31.62 nM EC50 J. Med. Chem. (2007) 50: 6519-6534 [PMID:18038970]
ChEMBL Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone F 7.5 pEC50 31.62 nM EC50 J. Med. Chem. (2006) 49: 4216-4231 [PMID:16821781]
ChEMBL Agonist activity at GR expressed in rat H4IIEC3 cells assessed as induction of PEPCK transactivation by luciferase reporter gene assay F 7.59 pEC50 26 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1658-1662 [PMID:21349714]
ChEMBL Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with PEPCK assessed as GRE activation by luciferase reporter gene assay F 7.59 pEC50 26 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1654-1657 [PMID:21324689]
ChEMBL Inhibition of concanavalin A stimulated T-cell proliferation in human PBMCs F 7.6 pEC50 25 nM EC50 J. Med. Chem. (2003) 46: 1016-1030 [PMID:12620078]
ChEMBL Inhibition of GR-mediated tyrosine amino transferase activity in human HepG2 cells B 7.62 pEC50 24 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2163-2167 [PMID:15808489]
ChEMBL Activity at human glucocorticoid receptor in human HepG2 cells assessed as tyrosine amino transferase activity B 7.62 pEC50 24 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3354-3361 [PMID:17467988]
ChEMBL Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Transactivation activity of glucocorticoid receptor in HFF assessed as induction of aromatase activity by measuring beta-estradiol activity after 18 to 24 hrs by ELISA B 7.72 pEC50 19 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay B 7.79 pEC50 16.1 nM EC50 J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity F 7.8 pEC50 16 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay B 7.8 pEC50 15.8 nM EC50 J. Med. Chem. (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity B 7.8 pEC50 15.8 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2139-2143 [PMID:19321341]
ChEMBL Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay B 7.84 pEC50 14.4 nM EC50 J. Med. Chem. (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay B 7.87 pEC50 13.6 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2139-2143 [PMID:19321341]
ChEMBL Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay B 7.87 pEC50 13.6 nM EC50 J. Med. Chem. (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL Transcriptional activation in CV-1 cells expressing human glucocorticoid receptor F 8.1 pEC50 8 nM EC50 J. Med. Chem. (2003) 46: 1016-1030 [PMID:12620078]
ChEMBL Activity at human glucocorticoid receptor in C57BI/6 mouse peritoneal exudate cells assessed as repression of mouse IL6 B 8.24 pEC50 5.7 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3354-3361 [PMID:17467988]
ChEMBL Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity relative to Dexamethasone F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1697-1700 [PMID:21316964]
ChEMBL Agonist activity at GR by GRE activation assay F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4158-4162 [PMID:17553679]
ChEMBL Agonist activity at glucocorticoid receptor assessed as glucose response element transcriptional transactivation by luciferase assay F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 3504-3508 [PMID:18513967]
ChEMBL Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 168-171 [PMID:21115247]
ChEMBL Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1658-1662 [PMID:21349714]
ChEMBL Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as GRE activation by luciferase reporter gene assay F 8.28 pEC50 5.3 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1654-1657 [PMID:21324689]
ChEMBL Ability to induce human IL-6 assay in A549 lung carcinoma cell line. F 8.35 pEC50 4.5 nM EC50 J. Med. Chem. (2004) 47: 2441-2452 [PMID:15115388]
ChEMBL GR-mediated transrepression of IL-6 in human A549 lung carcinoma cells F 8.35 pEC50 4.5 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2163-2167 [PMID:15808489]
ChEMBL Activity at human glucocorticoid receptor in human A549 cells assessed as repression of human IL6 B 8.35 pEC50 4.5 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3354-3361 [PMID:17467988]
ChEMBL Activity at human glucocorticoid receptor in C2C12 cells assessed as mouse glutamine synthetase activity B 8.47 pEC50 3.4 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3354-3361 [PMID:17467988]
ChEMBL The effective concentration in CV-1 cells for glucocorticoid response element activation (GRE). F 8.48 pEC50 3.3 nM EC50 J. Med. Chem. (2001) 44: 4481-4491 [PMID:11728194]
ChEMBL Agonist activity at glucocorticoid receptor in human fibroblast assessed as inhibition of IL-1-beta-induced IL6 production treated 1 hr before IL1-beta challenge measured after 24 hrs by transrepression assay F 8.52 pEC50 3 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 3017-3020 [PMID:20427184]
ChEMBL Effective concentration in HepG2 cells transfected with LUC gene (E-sel-Luc). F 8.59 pEC50 2.6 nM EC50 J. Med. Chem. (2001) 44: 4481-4491 [PMID:11728194]
ChEMBL Transcriptional repression in HepG2 cells expressing human glucocorticoid receptor F 8.68 pEC50 2.1 nM EC50 J. Med. Chem. (2003) 46: 1016-1030 [PMID:12620078]
Glucocorticoid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3144] [GtoPdb: 625] [UniProtKB: P06537]
ChEMBL GR-mediated transrepression of IL-6 in peritoneal exudate cells harvested from C57BI/6 mice B 8.24 pEC50 5.7 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2163-2167 [PMID:15808489]
ChEMBL Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells B 8.47 pEC50 3.4 nM EC50 Bioorg. Med. Chem. Lett. (2005) 15: 2163-2167 [PMID:15808489]
Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536]
ChEMBL Modulation of glucocorticoid receptor in rat whole blood B 7.28 pIC50 52 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Modulation of glucocorticoid receptor in rat plasma B 7.28 pIC50 52 nM IC50 J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL Inhibition of concanavalin A stimulated rat splenocyte proliferation F 7.71 pEC50 19.6 nM EC50 J. Med. Chem. (2003) 46: 1016-1030 [PMID:12620078]
Glutamine synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4612] [UniProtKB: P15104]
ChEMBL Ability to induce human glutamine synthetase in skeletal muscle cells B 7.49 pEC50 32 nM EC50 J. Med. Chem. (2004) 47: 2441-2452 [PMID:15115388]
GPBA receptor/G-protein coupled bile acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6]
ChEMBL Agonist activity at TGR5 in human whole blood assessed as inhibition of LPS-induced TNF-alpha release B 6.6 pIC50 251 nM IC50 ACS Med. Chem. Lett. (2016) 7: 51-55 [PMID:26819665]
Interleukin-6 in Human (target type: SINGLE PROTEIN) [ChEMBL: