Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T72168 | ||||
Target Name | Mineralocorticoid receptor (MR) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | AL-43 | Drug Info | Ki = 46 nM | [1] | |
Epierenone | Drug Info | Ki = 124 nM | [4] | ||
LG-120838 | Drug Info | IC50 < 20 nM | [6] | ||
LGD-5552 | Drug Info | Ki = 149 nM | [3] | ||
ONAPRISTONE | Drug Info | IC50 = 470 nM | [2] | ||
WAY-255348 | Drug Info | IC50 = 3700 nM | [5] | ||
References | |||||
REF 1 | Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dih... J Med Chem. 2003 Mar 13;46(6):1016-30. | ||||
REF 2 | 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 3 | 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 4 | (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 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-... J Med Chem. 2008 Mar 27;51(6):1861-73. | ||||
REF 6 | 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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