dexamethasone [Ligand Id: 2768] activity data from GtoPdb and ChEMBL

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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)
  • 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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  • Inducible NOS/Nitric oxide synthase, inducible in Mouse [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
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  • Pregnane X receptor in Mouse [GtoPdb: 606] [UniProtKB: O54915]
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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 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]
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 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]
ChEMBL Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with CCL2-promoter luciferase plasmid construct assessed as reduction in IL-1 beta induced inflammation by luciferase reporter gene assay B 8.2 pIC50 6.31 nM IC50 ACS Med Chem Lett (2021) 12: 1568-1577 [PMID:34676039]
ChEMBL Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with 3XGRE-promoter luciferase plasmid construct assessed as induction of receptor transactivation by luciferase reporter gene assay B 8.7 pEC50 2 nM EC50 ACS Med Chem Lett (2021) 12: 1568-1577 [PMID:34676039]
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]
GtoPdb - - 9 pIC50 - - - Eur J Pharmacol (1993) 247: 145-54 [PMID:8282004];
FEBS Lett (1999) 464: 9-13 [PMID:10611474]
Inducible NOS/Nitric oxide synthase, inducible in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
ChEMBL Inhibition of LPS induced NO-dependent iNOS activity in mouse RAW 264.7 cells preincubated for 1 hrs followed by LPS stimulation and measured after 24 hrs by Griess reagent based assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2021) 213: 113174-113174 [PMID:33515864]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Binding affinity to progesterone receptor (unknown origin) by fluorescence polarization assay B 6.11 pKi 778 nM Ki Bioorg Med Chem Lett (2014) 24: 3268-3273 [PMID:24980053]
ChEMBL Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells B 6.25 pKi 561 nM Ki J Med Chem (2014) 57: 849-860 [PMID:24446728]
ChEMBL Inhibition of tetramethylrhodamine labeled RU486 binding to PR by FP assay B 5.7 pIC50 >2000 nM IC50 J Med Chem (2006) 49: 7887-7896 [PMID:17181172]
ChEMBL Inhibition of human PR B 5.7 pIC50 >2000 nM IC50 Bioorg Med Chem Lett (2007) 17: 315-319 [PMID:17118655]
ChEMBL Displacement of TAMRA labeled Dexamethasone at human progesterone receptor in insect cell B 5.7 pIC50 >2000 nM IC50 Bioorg Med Chem Lett (2007) 17: 5025-5031 [PMID:17692519]
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 competitive binding assay B 5.7 pIC50 >2000 nM IC50 Bioorg Med Chem Lett (2013) 23: 6640-6644 [PMID:24215891]
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 Binding affinity to human recombinant progesterone 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 progesterone receptor expressed in baculovirus infected sf9 cells B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2017) 27: 437-442 [PMID:28043796]
ChEMBL Binding affinity to PR (unknown origin) by FP assay B 6.36 pIC50 440 nM IC50 Bioorg Med Chem Lett (2016) 26: 5741-5748 [PMID:27810243]
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0]
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 5.52 pKi 3038 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) B 4.63 pIC50 23292 nM IC50 DrugMatrix in vitro pharmacology data
Pregnane X receptor in Mouse [GtoPdb: 606] [UniProtKB: O54915]
GtoPdb - - 6.1 pEC50 - - - Cell (1998) 92: 73-82 [PMID:9489701]

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]