ChEMBL ligand: CHEMBL131 (Cortalone, Dekotil, Delta-cortef, Deltacortril, Deltalone, Desowen, Dilacort, 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)
ADAM17 in Human [ChEMBL: CHEMBL3706] [GtoPdb: 1662] [UniProtKB: P78536] There should be some charts here, you may need to enable JavaScript!
Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] There should be some charts here, you may need to enable JavaScript!
Corticosteroid binding globulin in Human [ChEMBL: CHEMBL2421] [UniProtKB: P08185] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] There should be some charts here, you may need to enable JavaScript!
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692] There should be some charts here, you may need to enable JavaScript!
Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] Glucocorticoid receptor in Mouse [ChEMBL: CHEMBL3144] [GtoPdb: 625] [UniProtKB: P06537] Glucocorticoid receptor in Rat [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536] There should be some charts here, you may need to enable JavaScript!
Glutamine synthetase in Human [ChEMBL: CHEMBL4612] [UniProtKB: P15104] There should be some charts here, you may need to enable JavaScript!
GPBA receptor/G-protein coupled bile acid receptor 1 in Human [ChEMBL: CHEMBL5409] [GtoPdb: 37] [UniProtKB: Q8TDU6] There should be some charts here, you may need to enable JavaScript!
Interleukin-6 in Human [ChEMBL: CHEMBL1795129] [UniProtKB: P05231] There should be some charts here, you may need to enable JavaScript!
Mineralocorticoid receptor in Human [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235] There should be some charts here, you may need to enable JavaScript!
Progesterone receptor in Human [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] There should be some charts here, you may need to enable JavaScript!

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: CHEMBL1795129] [UniProtKB: P05231]
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	8.38	pIC50	4.2	nM	IC50	US-8901310-B2. Tricyclic compounds, compositions, and methods (2014)
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
GtoPdb	-	-	7.43	pKi	37	nM	Ki	J Med Chem (2001) 44: 2879-85 [PMID:11520196]
ChEMBL	Binding affinity for mineralocorticoid receptor	B	7.43	pKi	37	nM	Ki	J Med Chem (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL	Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells	B	9.54	pKi	0.29	nM	Ki	J Med Chem (2014) 57: 849-860 [PMID:24446728]
ChEMBL	Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay	B	7.36	pIC50	44	nM	IC50	J Med Chem (2010) 53: 6681-6698 [PMID:20735001]
ChEMBL	Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay	B	7.36	pIC50	44	nM	IC50	Bioorg Med Chem Lett (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL	Displacement of TAMRA-labeled dexamethasone from mineralocorticoid receptor (unknown origin) by fluorescence polarization assay	B	7.36	pIC50	44	nM	IC50	Bioorg Med Chem Lett (2014) 24: 1934-1940 [PMID:24656565]
ChEMBL	Displacement of 3H-aldosterone from MR (unknown origin) ligand binding domain by SPA assay	B	7.74	pIC50	18	nM	IC50	Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
ChEMBL	Displacement of [3H]-aldosterone from human mineralocorticoid receptor LBD (729 to 984 residues) after 1 hr by scintillation proximity assay	B	7.96	pIC50	11	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
GtoPdb	-	-	7.96	pIC50	11	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL	Agonist activity at mineralocorticoid receptor in human A549 cells	F	8.7	pEC50	2	nM	EC50	J Med Chem (2010) 53: 8241-8251 [PMID:21073190]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL	Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells	B	5	pKi	>10000	nM	Ki	J Med Chem (2014) 57: 849-860 [PMID:24446728]
ChEMBL	Binding affinity to progesterone receptor by fluorescence polarization assay	B	5.22	pKi	>6000	nM	Ki	J Med Chem (2010) 53: 8241-8251 [PMID:21073190]
ChEMBL	Displacement of fluorescently labeled ligand from progesterone receptor by fluorescence polarization assay	B	5.22	pKi	>6000	nM	Ki	J Med Chem (2011) 54: 7318-7333 [PMID:21899328]
ChEMBL	Binding affinity towards progesterone receptor (PR) by displacing [3H]progesterone.	B	5.3	pKi	>5000	nM	Ki	J Med Chem (2001) 44: 4481-4491 [PMID:11728194]
ChEMBL	Binding affinity for progesterone receptor	B	5.3	pKi	>5000	nM	Ki	J Med Chem (2001) 44: 2879-2885 [PMID:11520196]
ChEMBL	Displacement of [3H]progesterone from human Progesterone receptor A	B	5.3	pKi	>5000	nM	Ki	J Med Chem (2003) 46: 1016-1030 [PMID:12620078]
ChEMBL	Binding affinity at progesterone receptor	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2008) 18: 3504-3508 [PMID:18513967]
ChEMBL	Displacement of [3H]progesterone from progesterone receptor in human T47D cells after 1200 mins by scintillation counting method	B	4.57	pIC50	27000	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL	Binding affinity to PR (unknown origin) by FP assay	B	5.68	pIC50	2080	nM	IC50	Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
ChEMBL	Binding affinity to progesterone receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled RU-486 by fluorescence polarization microplate assay	B	5.7	pIC50	>2000	nM	IC50	J Med Chem (2010) 53: 6681-6698 [PMID:20735001]
ChEMBL	Displacement of tetramethylrhodamine-labeled RU-486 from human recombinant progesterone receptor expressed in baculovirus infected insect cells by fluorescence polarization assay	B	5.7	pIC50	>2000	nM	IC50	Bioorg Med Chem Lett (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL	Displacement of TAMRA-labeled mifepristone from progesterone receptor (unknown origin) by fluorescence polarization assay	B	5.7	pIC50	>2000	nM	IC50	Bioorg Med Chem Lett (2014) 24: 1934-1940 [PMID:24656565]

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]