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Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.
Schreiber SL, Kotz JD, Li M, Aubé J, Austin CP, Reed JC, Rosen H, White EL, Sklar LA, Lindsley CW, Alexander BR, Bittker JA, Clemons PA, de Souza A, Foley MA, Palmer M, Shamji AF, Wawer MJ, McManus O, Wu M, Zou B, Yu H, Golden JE, Schoenen FJ, Simeonov A, Jadhav A, Jackson MR, Pinkerton AB, Chung TD, Griffin PR, Cravatt BF, Hodder PS, Roush WR, Roberts E, Chung DH, Jonsson CB, Noah JW, Severson WE, Ananthan S, Edwards B, Oprea TI, Conn PJ, Hopkins CR, Wood MR, Stauffer SR, Emmitte KA; NIH Molecular Libraries Project Team. Schreiber SL, et al. Among authors: emmitte ka. Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Cell. 2015. PMID: 26046436 Free PMC article. Review.
A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.
Cho HP, Engers DW, Venable DF, Niswender CM, Lindsley CW, Conn PJ, Emmitte KA, Rodriguez AL. Cho HP, et al. Among authors: emmitte ka. ACS Chem Neurosci. 2014 Jul 16;5(7):597-610. doi: 10.1021/cn5000343. Epub 2014 May 15. ACS Chem Neurosci. 2014. PMID: 24798819 Free PMC article.
Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM).
Wenthur CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, Daniels JS, Emmitte KA, Conn PJ, Lindsley CW. Wenthur CJ, et al. Among authors: emmitte ka. J Med Chem. 2013 Jun 27;56(12):5208-12. doi: 10.1021/jm400439t. Epub 2013 Jun 13. J Med Chem. 2013. PMID: 23718281 Free PMC article.
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Felts AS, Rodriguez AL, Morrison RD, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Emmitte KA. Felts AS, et al. Among authors: emmitte ka. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1679-1685. doi: 10.1016/j.bmcl.2018.04.053. Epub 2018 Apr 22. Bioorg Med Chem Lett. 2018. PMID: 29705142 Free PMC article.
Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.
Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, Olsen CM, Winder DG, Emmitte KA, Lindsley CW. Mueller R, et al. Among authors: emmitte ka. ChemMedChem. 2012 Mar 5;7(3):406-14. doi: 10.1002/cmdc.201100510. Epub 2012 Jan 20. ChemMedChem. 2012. PMID: 22267125 Free PMC article. No abstract available.
64 results