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Items: 1 to 20 of 30

1.

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.

Wood MR, Noetzel MJ, Tarr JC, Rodriguez AL, Lamsal A, Chang S, Foster JJ, Smith E, Chase P, Hodder PS, Engers DW, Niswender CM, Brandon NJ, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4282-6. doi: 10.1016/j.bmcl.2016.07.042. Epub 2016 Jul 21.

2.

Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.

Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3029-3033. doi: 10.1016/j.bmcl.2016.05.010. Epub 2016 May 5.

3.

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.

Cell. 2015 Jun 4;161(6):1252-65. doi: 10.1016/j.cell.2015.05.023. Review.

4.

Development of a Novel, Orthosteric M5 Antagonist Possessing a High Degree of Muscarinic Subtype Selectivity.

Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Wood MR, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

5.

Development of the First CNS penetrant M5 Positive Allosteric Modulator (PAM) Based on a Novel, non-Isatin Core.

Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Lindsley CW, Wood MR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

6.

Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.

Chang JW, Zuhl AM, Speers AE, Niessen S, Brown SJ, Mulvihill MM, Fan YC, Spicer TP, Southern M, Scampavia L, Fernandez-Vega V, Dix MM, Cameron MD, Hodder PS, Rosen H, Nomura DK, Kwon O, Hsu KL, Cravatt BF.

ACS Chem Biol. 2015 Apr 17;10(4):925-32. doi: 10.1021/cb500893q. Epub 2015 Jan 20.

7.

Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM).

Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Wood MR, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 9 [updated 2014 Sep 18].

8.

Target-based screen against a periplasmic serine protease that regulates intrabacterial pH homeostasis in Mycobacterium tuberculosis.

Zhao N, Darby CM, Small J, Bachovchin DA, Jiang X, Burns-Huang KE, Botella H, Ehrt S, Boger DL, Anderson ED, Cravatt BF, Speers AE, Fernandez-Vega V, Hodder PS, Eberhart C, Rosen H, Spicer TP, Nathan CF.

ACS Chem Biol. 2015 Feb 20;10(2):364-71. doi: 10.1021/cb500746z. Epub 2014 Dec 5.

9.

Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.

Spicer TP, Jiang J, Taylor AB, Choi JY, Hart PJ, Roush WR, Fields GB, Hodder PS, Minond D.

J Med Chem. 2014 Nov 26;57(22):9598-611. doi: 10.1021/jm501284e. Epub 2014 Nov 11.

10.

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).

Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR.

J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. Epub 2014 Sep 3.

11.

Development of high throughput screening assays and pilot screen for inhibitors of metalloproteases meprin α and β.

Madoux F, Tredup C, Spicer TP, Scampavia L, Chase PS, Hodder PS, Fields GB, Becker-Pauly C, Minond D.

Biopolymers. 2014 Sep;102(5):396-406. doi: 10.1002/bip.22527.

12.

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.

Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW.

ChemMedChem. 2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1.

13.

Transitioning pharmacoperones to therapeutic use: in vivo proof-of-principle and design of high throughput screens.

Conn PM, Smithson DC, Hodder PS, Stewart MD, Behringer RR, Smith E, Ulloa-Aguirre A, Janovick JA.

Pharmacol Res. 2014 May;83:38-51. doi: 10.1016/j.phrs.2013.12.004. Epub 2013 Dec 25. Review.

14.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW.

J Med Chem. 2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13.

15.

Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.

Guerrero M, Poddutoori R, Urbano M, Peng X, Spicer TP, Chase PS, Hodder PS, Schaeffer MT, Brown S, Rosen H, Roberts E.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6346-9. doi: 10.1016/j.bmcl.2013.09.075. Epub 2013 Oct 1.

16.

Development and characterization of a highly selective M5 PAM probe molecule with improved potency.

Gentry PR, Bridges TM, Daniels JS, Lamsal A, Vinson PN, Niswender CM, Hodder PS, Rosen H, Conn PJ, Engers J, Lindsley CW, Wood MR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 13 [updated 2013 Mar 22].

17.

Discovery of ML326: The first sub-micromolar, selective M5 PAM.

Gentry PR, Bridges TM, Lamsal A, Vinson PN, Smith E, Chase P, Hodder PS, Engers JL, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW.

Bioorg Med Chem Lett. 2013 May 15;23(10):2996-3000. doi: 10.1016/j.bmcl.2013.03.032. Epub 2013 Mar 16.

18.

Probe Development Efforts to Identify Novel Inhibitors of Protein Phosphatase Methylesterase-1 (PME-1).

Bachovchin DA, Speers AE, Brown SJ, Spicer TP, Fernandez-Vega V, Ferguson J, Mohr JT, Murphy J, Fu GC, Cravatt BF, Hodder PS, Rosen H.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Aug 31 [updated 2011 Dec 12].

19.

Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes.

Adibekian A, Martin BR, Chang JW, Hsu KL, Tsuboi K, Bachovchin DA, Speers AE, Brown SJ, Spicer T, Fernandez-Vega V, Ferguson J, Hodder PS, Rosen H, Cravatt BF.

J Am Chem Soc. 2012 Jun 27;134(25):10345-8. doi: 10.1021/ja303400u. Epub 2012 Jun 12.

20.

A high-throughput assay for the identification of drugs against late-stage Plasmodium falciparum gametocytes.

Peatey CL, Spicer TP, Hodder PS, Trenholme KR, Gardiner DL.

Mol Biochem Parasitol. 2011 Dec;180(2):127-31. doi: 10.1016/j.molbiopara.2011.09.002. Epub 2011 Sep 16.

PMID:
21939693

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