| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T72168 | ||||
| Target Name | Mineralocorticoid receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | ONAPRISTONE | Drug Info | IC50 = 470 nM | [526633] | |
| EPIERENONE | Drug Info | Ki = 124 nM | [529171] | ||
| LG-120838 | Drug Info | IC50 < 20 nM | [534728] | ||
| AL-43 | Drug Info | Ki = 46 nM | [526567] | ||
| LGD-5552 | Drug Info | Ki = 149 nM | [529166] | ||
| WAY-255348 | Drug Info | IC50 = 3700 nM | [529352] | ||
| References | |||||
| Ref 526633 | Bioorg 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 529171 | J 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 534728 | J 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 526567 | J Med Chem. 2003 Mar 13;46(6):1016-30.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. | ||||
| Ref 529166 | Proc 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 529352 | J Med Chem. 2008 Mar 27;51(6):1861-73. Epub 2008 Mar 5.Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348). | ||||
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