Target Validation Information
Target ID T30687
Target Name mRNA of glucocorticoid receptor
Target Type
Clinical Trial
Drug Potency against Target CP-394531 Drug Info Ki = 0.1 nM [1]
A-348441 Drug Info IC50 = 1.2 nM [2]
EPIERENONE Drug Info Ki = 1758 nM [3]
AL-43 Drug Info IC50 = 13 nM [4]
LGD-5552 Drug Info Ki = 2.4 nM [5]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [6]
OXDEX Drug Info IC50 = 600 nM [7]
ONAPRISTONE Drug Info IC50 = 27 nM [8]
LG-120838 Drug Info IC50 = 1050 nM [9]
1-(3-CHLORO-4-FLUOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) Drug Info IC50 = 49 nM [10]
2,2,2-TRIFLUORO-1-(4-FLUOROPHENYL)-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (DIASTEREOMERIC MIX) Drug Info IC50 = 161 nM [10]
1-(2,3-DICHLOROPHENYL)-2,2,2-TRIFLUORO-1-(1-(4-FLUOROPHENYL)-1H-INDAZOL-5-YL)ETHANOL (ENANTIOMERIC MIX) Drug Info IC50 = 34 nM [10]
1-Methoxy-6-phenyl-6H-benzo[c]chromene Drug Info IC50 = 10000 nM [11]
RU-43044 Drug Info Ki = 0.1 nM [1]
CP-409069 Drug Info Ki = 0.17 nM [1]
1-Methoxy-6-phenyl-6H-benzo[c]chromen-8-ylamine Drug Info IC50 = 1937 nM [11]
ENDIANDRIN A Drug Info IC50 = 900 nM [12]
WAY-252623 Drug Info IC50 = 1000 nM [13]
DI-O-METHYLENDIANDRIN A Drug Info IC50 = 13000 nM [12]
WAY-214950 Drug Info IC50 = 7200 nM [13]
References
REF 1J Med Chem. 2010 Apr 22;53(8):3065-74.Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators.
REF 2Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. Epub 2006 Sep 20.Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
REF 3J Med Chem. 2007 Dec 27;50(26):6443-5. Epub 2007 Nov 27.(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of themineralocorticoid receptor.
REF 4Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.
REF 5Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
REF 6J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
REF 7J Med Chem. 2009 Aug 13;52(15):4604-12.Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides.
REF 8Bioorg Med Chem Lett. 2003 Jun 16;13(12):2075-8.Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
REF 9J Med Chem. 1998 Oct 22;41(22):4354-9.5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.
REF 10Bioorg Med Chem Lett. 2010 May 15;20(10):3017-20. Epub 2010 Apr 11.5-Functionalized indazoles as glucocorticoid receptor agonists.
REF 11Bioorg Med Chem Lett. 2004 May 3;14(9):2079-82.Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
REF 12J Nat Prod. 2007 Jul;70(7):1118-21. Epub 2007 Jun 21.Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum.
REF 13J Med Chem. 2008 Nov 27;51(22):7161-8.Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis.

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