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ChEMBL ligand: CHEMBL384467 (Aeroseb-dex, Dalalone, Decaderm, Decadron, Decadron-75, Decadron-LA, Decaspray, Dexacen-4, Dexacort, Dexacortisyl, Dexafree, Dexair, Dexamethasone, Dexamethasone intensol, Dexamethasone metasulfobenzoate sodium, Dexamethasone palmitate, Dexamethasone valerate, Dexone, Dexone 0.5, Dexone 0.75, Dexone 1.5, Dexone 4, Dexsol, Dextenza, Dexycu, Dexycu kit, Dropodex, Fluormethylprednisolone, Gppe ear spy, Hemady, Hexadrol, ISV-305, Kortico Injection, Martapan, Maxidex, Maxitrol, Mymethasone, Neodecadron, NSC-34521, Oradexon, OTO-104, Otomize, Ozurdex, Sofradex, Spersadex comp, Tobradex) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells | B | 5.85 | pKi | 1410 | nM | Ki | J Med Chem (2014) 57: 849-860 [PMID:24446728] |
ChEMBL | Binding affinity to AR (unknown origin) by FP assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243] |
ChEMBL | Binding affinity to androgen receptor | B | 5.4 | pIC50 | >4000 | nM | IC50 | J Med Chem (2010) 53: 1270-1280 [PMID:20047280] |
ChEMBL | Binding affinity to human recombinant androgen receptor expressed in baculovirus infected Sf9 cells | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743] |
ChEMBL | Binding affinity to recombinant human androgen receptor expressed in baculovirus infected sf9 cells | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 437-442 [PMID:28043796] |
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 4.79 | pKi | 16371 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881) | B | 4.09 | pIC50 | 81283.05 | nM | IC50 | J Med Chem (2005) 48: 5666-5674 [PMID:16134935] |
ChEMBL | DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) | B | 4.61 | pIC50 | 24556 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527] | ||||||||
ChEMBL | Inhibition of rat basophilic leukemia cell 5-lipoxygenase | B | 4.6 | pIC50 | >25000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 711-716 |
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 low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | B | 4.38 | pKi | 41300 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
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 | 4.66 | pKi | 22100 | 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 | Binding affinity to glucocorticoid receptor | B | 7.72 | pKd | 19 | nM | Kd | J Med Chem (2010) 53: 3349-3360 [PMID:20355713] |
ChEMBL | Inhibition of glucocorticoid receptor (unknown origin) | B | 7.72 | pKd | 19 | nM | Kd | J Med Chem (2019) 62: 10005-10025 [PMID:31188592] |
ChEMBL | Induction of translocation of human glucocorticoid receptor expressed in HEK293T cells transduced with lentiviral vector expressing H2B-mCherry and GFP-GR assessed as effective dissociation constant measured every 130 sec for 22 mins by fluorescence imaging analysis | B | 8.55 | pKd | 2.8 | nM | Kd | RSC Med Chem (2021) 12: 203-212 [PMID:34046609] |
ChEMBL | Binding affinity to GR (unknown origin) | B | 8.7 | pKd | 2 | nM | Kd | Bioorg Med Chem (2019) 27: 2508-2520 [PMID:30929949] |
ChEMBL | Binding affinity was determined for human glucocorticoid receptor(hGR). | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (1996) 39: 1778-1789 [PMID:8627601] |
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 8.44 | pKi | 3.66 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of radiolabeled Dexamethasone from human glucocorticoid receptor | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Binding affinity to GR | B | 8.68 | pKi | 2.1 | nM | Ki | J Med Chem (2007) 50: 4699-4709 [PMID:17705362] |
ChEMBL | Binding affinity to human glucocorticoid receptor by radioligand displacement assay | B | 8.82 | pKi | 1.5 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assay | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 3268-3273 [PMID:24980053] |
ChEMBL | Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence assay | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5448-5451 [PMID:23916594] |
ChEMBL | Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assay | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5442-5447 [PMID:23953070] |
ChEMBL | Displacement of GS-red from human glucocorticoid receptor by fluorescent polarization assay | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2010) 53: 1270-1280 [PMID:20047280] |
ChEMBL | Binding affinity to glucocorticoid receptor-LBD (unknown origin) by fluorescence polarization assay | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5571-5574 [PMID:24011644] |
ChEMBL | Displacement of GS-red from GRapha by fluorescence polarization assay | B | 8.96 | pKi | 1.1 | 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 | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 2139-2143 [PMID:19321341] |
ChEMBL | Displacement of [3H]DEX from human glucocorticoid receptor | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2010) 53: 3065-3074 [PMID:20334371] |
ChEMBL | Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells | B | 9.16 | pKi | 0.69 | nM | Ki | J Med Chem (2014) 57: 849-860 [PMID:24446728] |
ChEMBL | Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM | F | 5 | pIC50 | <10000 | nM | IC50 | J Med Chem (2005) 48: 4507-4510 [PMID:15999989] |
ChEMBL | Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cells | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
ChEMBL | Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2007) 50: 6519-6534 [PMID:18038970] |
ChEMBL | Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation | F | 6 | pIC50 | <1000 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
ChEMBL | Transrepression activity at glucocorticoid receptor in human whole blood assessed as repression of IL-1-induced TNF-alpha production after 4 hrs by ELISA | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2015) 58: 2658-2677 [PMID:25706100] |
ChEMBL | Displacement of fluorescent-labelled Dexamethasone from glucocorticoid receptor | B | 7.9 | pIC50 | 12.59 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1126-1133 [PMID:21257309] |
ChEMBL | Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells | B | 7.9 | pIC50 | 12.59 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 437-442 [PMID:28043796] |
ChEMBL | Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells | B | 7.9 | pIC50 | 12.59 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743] |
ChEMBL | Displacement of fluoromone from human glucocorticoid receptor LBD assessed as reduction of maximum polarization by fluorescence polarization assay relative to control | B | 7.94 | pIC50 | 11.4 | nM | IC50 | J Med Chem (2010) 53: 3065-3074 [PMID:20334371] |
ChEMBL | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | B | 8.09 | pIC50 | 8.06 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Displacement of fluorescent labeled Dexamethasone from glucocorticoid receptor | B | 8.1 | pIC50 | 7.94 | nM | IC50 | J Med Chem (2007) 50: 6519-6534 [PMID:18038970] |
ChEMBL | Inhibition of fluorescent-labeled Dexamethasone binding to GR | B | 8.1 | pIC50 | 7.94 | nM | IC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
ChEMBL | Binding affinity to glucocorticoid receptor | B | 8.12 | pIC50 | 7.59 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
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 | Displacement of radiolabeled Dexamethasone from human glucocorticoid receptor | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Displacement of fluormone from human recombinant glucocorticoid receptor ligand binding domain by fluorescence polarization assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2009) 52: 4604-4612 [PMID:19610652] |
ChEMBL | Inhibition of glucocorticoid receptor | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2008) 16: 5853-5861 [PMID:18490170] |
ChEMBL | Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Nat Prod (2008) 71: 1063-1065 [PMID:18412397] |
ChEMBL | Modulation of glucocorticoid receptor (unknown origin) transfected in human HeLa cells assessed as transrepression by measuring inhibition of TNF-alpha induced NF-kappaB signalling incubated for 18 hrs by dual-luciferase reporter based assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2022) 65: 15710-15724 [PMID:36399795] |
ChEMBL | Inhibition of human glucocorticoid receptor | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
ChEMBL | Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
ChEMBL | Binding affinity to glucocorticoid receptor (unknown origin) by Lanthascreen TR-FRET competition binding assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2022) 65: 15710-15724 [PMID:36399795] |
ChEMBL | Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity | F | 8.4 | pIC50 | 3.98 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1126-1133 [PMID:21257309] |
ChEMBL | Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
ChEMBL | Displacement of [3H]dexamethasone from GR receptor in human IM9 cells | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
ChEMBL | Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6640-6644 [PMID:24215891] |
ChEMBL | Binding affinity to human GR | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2015) 58: 2658-2677 [PMID:25706100] |
ChEMBL | Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2010) 53: 6681-6698 [PMID:20735001] |
ChEMBL | Inhibition of human GR | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 315-319 [PMID:17118655] |
ChEMBL | Displacement of TAMRA labeled Dexamethasone at human glucocorticoid receptor in insect cell | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5025-5031 [PMID:17692519] |
ChEMBL | Modulation of glucocorticoid receptor (unknown origin) transfected in human HeLa cells assessed as transrepression by measuring inhibition of PMA-induced AP-1 signalling incubated for 18 hrs by dual-luciferase reporter based assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 15710-15724 [PMID:36399795] |
ChEMBL | Binding affinity to human glucocorticoid receptor by radioligand displacement assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2006) 49: 7887-7896 [PMID:17181172] |
ChEMBL | Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assay | B | 8.52 | pIC50 | 3 | 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 | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6842-6851 [PMID:21963986] |
ChEMBL | Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production | B | 8.6 | pIC50 | 2.51 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743] |
ChEMBL | Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production | B | 8.6 | pIC50 | 2.51 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 437-442 [PMID:28043796] |
ChEMBL | Binding affinity to human glucocorticoid receptor by radioligand displacement assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
ChEMBL | Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay | B | 8.63 | pIC50 | 2.35 | nM | IC50 | Eur J Med Chem (2018) 157: 791-804 [PMID:30144697] |
ChEMBL | Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA | B | 8.74 | pIC50 | 1.8 | nM | IC50 | J Med Chem (2015) 58: 2658-2677 [PMID:25706100] |
ChEMBL | Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay | B | 8.8 | pIC50 | 1.58 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743] |
ChEMBL | Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay | B | 8.8 | pIC50 | 1.58 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 437-442 [PMID:28043796] |
ChEMBL | Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2007) 50: 4699-4709 [PMID:17705362] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay | F | 8.93 | pIC50 | 1.18 | 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 | 8.93 | pIC50 | 1.18 | nM | IC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
GtoPdb | - | - | 9 | pIC50 | - | - | - |
Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004]; FEBS Lett (1999) 464: 9-13 [PMID:10611474]; J Biol Chem (2000) 275: 19041-9 [PMID:10747884] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay | F | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1126-1133 [PMID:21257309] |
ChEMBL | Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2014) 5: 1318-1323 [PMID:25516791] |
ChEMBL | Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay | F | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4846-4850 [PMID:19592247] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay | F | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
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 | 9.29 | pIC50 | 0.51 | nM | IC50 | J Med Chem (2010) 53: 6681-6698 [PMID:20735001] |
ChEMBL | Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL1-induced IL-6 production after 18 to 24 hrs | F | 9.29 | pIC50 | 0.51 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6842-6851 [PMID:21963986] |
ChEMBL | Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay | F | 9.29 | pIC50 | 0.51 | nM | IC50 | J Med Chem (2010) 53: 6947-6953 [PMID:20812681] |
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 | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1934-1940 [PMID:24656565] |
ChEMBL | Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 24 hrs | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6640-6644 [PMID:24215891] |
ChEMBL | Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay | F | 4.8 | pEC50 | <15848.93 | nM | EC50 | J Med Chem (2010) 53: 6947-6953 [PMID:20812681] |
ChEMBL | Agonist activity at human GR expressed in CHO-K1 cells by PathHunter assay | B | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2022) 65: 9974-10000 [PMID:35797110] |
ChEMBL | Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity | F | 7.77 | pEC50 | 17 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 6842-6851 [PMID:21963986] |
ChEMBL | Agonist activity at glucocorticoid receptor (unknown origin) transfected in human HeLa cells assessed as transactivation of receptor incubated for 18 hrs by firefly luciferase assay | B | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (2022) 65: 15710-15724 [PMID:36399795] |
ChEMBL | Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting | B | 7.9 | pEC50 | 12.5 | nM | EC50 | Bioorg Med Chem (2013) 21: 321-332 [PMID:23199485] |
ChEMBL | Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay | B | 8.01 | pEC50 | 9.7 | nM | EC50 | Bioorg Med Chem (2013) 21: 321-332 [PMID:23199485] |
ChEMBL | Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay | B | 8.1 | pEC50 | 7.94 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 5835-5838 [PMID:20727743] |
ChEMBL | Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay | B | 8.14 | pEC50 | 7.2 | nM | EC50 | J Nat Prod (2009) 72: 1944-1948 [PMID:19863083] |
ChEMBL | Agonist activity at glucocorticoid receptor in human whole blood assessed as inhibition of LPS-induced TNF production incubated for 20 hrs prior to LPS challenge measured after 5 hrs by ELISA | B | 8.16 | pEC50 | 6.9 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 3268-3273 [PMID:24980053] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay | F | 8.27 | pEC50 | 5.37 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4737-4745 [PMID:17616395] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay | F | 8.3 | pEC50 | 5.01 | 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 | 8.3 | pEC50 | 5.01 | nM | EC50 | J Med Chem (2006) 49: 4216-4231 [PMID:16821781] |
ChEMBL | Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2010) 53: 8241-8251 [PMID:21073190] |
ChEMBL | Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay | B | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5442-5447 [PMID:23953070] |
ChEMBL | Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay | B | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 3268-3273 [PMID:24980053] |
ChEMBL | Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay | B | 8.35 | pEC50 | 4.5 | nM | EC50 | J Med Chem (2010) 53: 1270-1280 [PMID:20047280] |
ChEMBL | Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay | B | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5448-5451 [PMID:23916594] |
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 | 8.38 | pEC50 | 4.2 | 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 | 8.38 | pEC50 | 4.2 | nM | EC50 | J Med Chem (2010) 53: 8241-8251 [PMID:21073190] |
ChEMBL | Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay | B | 8.43 | pEC50 | 3.7 | nM | EC50 | Bioorg Med Chem (2013) 21: 321-332 [PMID:23199485] |
ChEMBL | Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | J Med Chem (2010) 53: 1270-1280 [PMID:20047280] |
ChEMBL | Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity | B | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2139-2143 [PMID:19321341] |
ChEMBL | Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5571-5574 [PMID:24011644] |
ChEMBL | Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5448-5451 [PMID:23916594] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 3268-3273 [PMID:24980053] |
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 | 8.6 | pEC50 | 2.5 | nM | EC50 | J Med Chem (2010) 53: 8241-8251 [PMID:21073190] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay | B | 8.6 | pEC50 | 2.5 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5442-5447 [PMID:23953070] |
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 | 8.74 | pEC50 | 1.8 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 6842-6851 [PMID:21963986] |
ChEMBL | Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay | B | 8.89 | pEC50 | 1.3 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay | B | 8.96 | pEC50 | 1.1 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5442-5447 [PMID:23953070] |
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 | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2010) 53: 8241-8251 [PMID:21073190] |
ChEMBL | Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay | B | 8.96 | pEC50 | 1.1 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 3268-3273 [PMID:24980053] |
ChEMBL | Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay | B | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2010) 53: 1270-1280 [PMID:20047280] |
ChEMBL | Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay | B | 8.96 | pEC50 | 1.1 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 5448-5451 [PMID:23916594] |
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 | 8.96 | pEC50 | 1.1 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 2139-2143 [PMID:19321341] |
ChEMBL | Effective agonist concentration for transcriptional repression of IL-6 production in IL-1 stimulated human foreskin fibroblasts | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 4761-4769 [PMID:16112571] |
ChEMBL | Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay | B | 9 | pEC50 | 1 | nM | EC50 | J Nat Prod (2006) 69: 707-709 [PMID:16643060] |
ChEMBL | Agonist activity at human GR expressed in CV1 cells by GRE activation assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2007) 50: 4699-4709 [PMID:17705362] |
ChEMBL | Agonist activity at recombinant human glucocorticoid receptor expressed in African green monkey CV1 cells by MMTV luciferase reporter gene assay |