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ChEMBL ligand: CHEMBL131 (Cortalone, Dekotil, Delta-cortef, Deltacortril, Deltalone, Desowen, Dilacort, Equisolon, Fernisolone-p, Hydeltra, Hydeltra-Tba, Meticortelone, Meti-derm, Neo-Delta-Cortef, NSC-9120, NSC-9900, Pevanti, Poly-Pred, Precortisyl, Precortisyl fte, Pred-G, Prednisolone, Prelone, Scheriproct, Servisone, Sterane, Tridesilon, Verdeso) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |