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

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