[3H]dexamethasone [Ligand Id: 3447] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL384467 (Aeroseb-dex, Dexafree, Spersadex comp, Kortico Injection, Dexair, Decaspray, Dexamethasone metasulfobenzoate sodium, Dexone 0.5, Hexadrol, Dexamethasone, Dalalone, Decaderm, Oradexon, Dexone 0.75, Ozurdex, Dexone, Decadron, ISV-305, Maxidex, Mymethasone, Dextenza, Dexacort, Dexamethasone valerate, Otomize, Sofradex, Tobradex, Dexamethasone palmitate, Neodecadron, Decadron-75, NSC-34521, Dexone 4, Gppe ear spy, Dexacortisyl, Dexsol, Dexone 1.5, Dexamethasone intensol, Fluormethylprednisolone, Hemady, OTO-104, Decadron-LA, Dexacen-4, Dexycu kit, Maxitrol, Dropodex, Martapan)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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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 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 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 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 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 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 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 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-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 Inhibition of glucocorticoid receptor B 8.3 pIC50 5 nM IC50 Bioorg. Med. Chem. (2008) 16: 5853-5861 [PMID:18490170]
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 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 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 [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 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 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 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 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 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 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 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 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 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 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]
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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 B 10 pEC50 0.1 nM EC50 Eur J Med Chem (2019) 161: 192-204 [PMID:30359818]
Glucocorticoid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3368] [GtoPdb: 625] [UniProtKB: P06536]
ChEMBL Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation counting B 7.66 pIC50 22 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 1744-1747 [PMID:21349712]
ChEMBL Displacement of [3H]Dex from glucocorticoid receptor in Sprague-Dawley rat liver after 2 hrs by liquid scintillation counting B 7.66 pIC50 22 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6310-6313 [PMID:21944856]
Mineralocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1994] [GtoPdb: 626] [UniProtKB: P08235]
ChEMBL Binding affinity to MR B 8.14 pKi 7.2 nM Ki J. Med. Chem. (2007) 50: 4699-4709 [PMID:17705362]
ChEMBL Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells B 9.44 pKi 0.36 nM Ki J. Med. Chem. (2014) 57: 849-860 [PMID:24446728]
ChEMBL Binding affinity to human recombinant mineralocorticoid 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 mineralocorticoid receptor expressed in baculovirus infected sf9 cells B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2017) 27: 437-442 [PMID:28043796]
ChEMBL Displacement of 3H-aldosterone from MR (unknown origin) ligand binding domain by SPA assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
ChEMBL Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay B 7.48 pIC50 33 nM IC50 J. Med. Chem. (2010) 53: 6681-6698 [PMID:20735001]
ChEMBL Inhibition of tetramethylrhodamine labeled dexamethasone binding to MR by FP assay B 7.48 pIC50 33 nM IC50 J. Med. Chem. (2006) 49: 7887-7896 [PMID:17181172]
ChEMBL Binding affinity to mineralocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assay B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 6640-6644 [PMID:24215891]
ChEMBL Displacement of TAMRA-labeled dexamethasone from mineralocorticoid receptor (unknown origin) by fluorescence polarization assay B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 1934-1940 [PMID:24656565]
ChEMBL Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6842-6851 [PMID:21963986]
ChEMBL Inhibition of human MR B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 315-319 [PMID:17118655]
ChEMBL Displacement of TAMRA labeled mifepristone at human mineralocorticoid receptor in insect cell B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 5025-5031 [PMID:17692519]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]