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Glucocorticoid receptor
A glucocorticoid receptor that is encoded in the genome of rat. [OMA:P06536, PRO:DNx]
Synonyms
GR;
Nuclear receptor subfamily 3 group C member 1
Research
Bioassay Publications (15)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (13.33) | 18.2507 |
| 2000's | 6 (40.00) | 29.6817 |
| 2010's | 7 (46.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (9)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| prednisolone | Rattus norvegicus (Norway rat) | EC50 | 0.0196 | 1 | 1 |
| mifepristone | Rattus norvegicus (Norway rat) | EC50 | 0.0025 | 1 | 1 |
| fluticasone propionate | Rattus norvegicus (Norway rat) | EC50 | 0.0008 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| mifepristone | Rattus norvegicus (Norway rat) | Activity | 0.2700 | 1 | 1 |
Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.Journal of medicinal chemistry, , 03-08, Volume: 61, Issue:5, 2018
Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.Journal of medicinal chemistry, , Mar-13, Volume: 46, Issue:6, 2003
Design and synthesis of tricyclic tetrahydroquinolines as a new series of nonsteroidal selective androgen receptor modulators (SARMs).Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Tetrahydroquinolines as a novel series of nonsteroidal selective androgen receptor modulators: structural requirements for better physicochemical and biological properties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases.Journal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
Anti-inflammatory 17beta-thioalkyl-16alpha,17alpha-ketal and -acetal androstanes: a new class of airway selective steroids for the treatment of asthma.Journal of medicinal chemistry, , Dec-06, Volume: 39, Issue:25, 1996