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Items: 19

1.

Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.

Harris PA, Faucher N, George N, Eidam PM, King BW, White GV, Anderson NA, Bandyopadhyay D, Beal AM, Beneton V, Berger SB, Campobasso N, Campos S, Capriotti CA, Cox JA, Daugan A, Donche F, Fouchet MH, Finger JN, Geddes B, Gough PJ, Grondin P, Hoffman BL, Hoffman SJ, Hutchinson SE, Jeong JU, Jigorel E, Lamoureux P, Leister LK, Lich JD, Mahajan MK, Meslamani J, Mosley JE, Nagilla R, Nassau PM, Ng SL, Ouellette MT, Pasikanti KK, Potvain F, Reilly MA, Rivera EJ, Sautet S, Schaeffer MC, Sehon CA, Sun H, Thorpe JH, Totoritis RD, Ward P, Wellaway N, Wisnoski DD, Woolven JM, Bertin J, Marquis RW.

J Med Chem. 2019 May 23;62(10):5096-5110. doi: 10.1021/acs.jmedchem.9b00318. Epub 2019 May 2.

PMID:
31013427
2.

Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.

Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J.

J Med Chem. 2017 Feb 23;60(4):1247-1261. doi: 10.1021/acs.jmedchem.6b01751. Epub 2017 Feb 10.

PMID:
28151659
3.

Cell-Based Selection Expands the Utility of DNA-Encoded Small-Molecule Library Technology to Cell Surface Drug Targets: Identification of Novel Antagonists of the NK3 Tachykinin Receptor.

Wu Z, Graybill TL, Zeng X, Platchek M, Zhang J, Bodmer VQ, Wisnoski DD, Deng J, Coppo FT, Yao G, Tamburino A, Scavello G, Franklin GJ, Mataruse S, Bedard KL, Ding Y, Chai J, Summerfield J, Centrella PA, Messer JA, Pope AJ, Israel DI.

ACS Comb Sci. 2015 Dec 14;17(12):722-31. doi: 10.1021/acscombsci.5b00124. Epub 2015 Dec 3.

PMID:
26562224
4.

Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.

Charnley AK, Convery MA, Lakdawala Shah A, Jones E, Hardwicke P, Bridges A, Ouellette M, Totoritis R, Schwartz B, King BW, Wisnoski DD, Kang J, Eidam PM, Votta BJ, Gough PJ, Marquis RW, Bertin J, Casillas L.

Bioorg Med Chem. 2015 Nov 1;23(21):7000-6. doi: 10.1016/j.bmc.2015.09.038. Epub 2015 Sep 25.

PMID:
26455654
5.

Nω-NITRO-Nω'-SUBSTITUTED GUANIDINES: A SIMPLE CLASS OF NITRIC OXIDE SYNTHASE INHIBITORS.

Guillon CD, Wisnoski DD, Saxena J, Heindel ND, Heck DE, Wolff DJ, Laskin JD.

Mod Res Inflamm. 2014 May;3(2):48-58.

6.

Phenoxyacetic acids as PPARδ partial agonists: synthesis, optimization, and in vivo efficacy.

Evans KA, Shearer BG, Wisnoski DD, Shi D, Sparks SM, Sternbach DD, Winegar DA, Billin AN, Britt C, Way JM, Epperly AH, Leesnitzer LM, Merrihew RV, Xu RX, Lambert MH, Jin J.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2345-50. doi: 10.1016/j.bmcl.2011.02.077. Epub 2011 Mar 15.

PMID:
21414782
7.

Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.

Budzik BW, Evans KA, Wisnoski DD, Jin J, Rivero RA, Szewczyk GR, Jayawickreme C, Moncol DL, Yu H.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1363-7. doi: 10.1016/j.bmcl.2010.01.003. Epub 2010 Jan 7.

PMID:
20097073
8.

Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.

Yang FV, Shipe WD, Bunda JL, Nolt MB, Wisnoski DD, Zhao Z, Barrow JC, Ray WJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Hartman GD, Lindsley CW.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):531-6. doi: 10.1016/j.bmcl.2009.11.100. Epub 2009 Nov 24.

PMID:
20004574
9.

Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.

Evans KA, Budzik BW, Ross SA, Wisnoski DD, Jin J, Rivero RA, Vimal M, Szewczyk GR, Jayawickreme C, Moncol DL, Rimele TJ, Armour SL, Weaver SP, Griffin RJ, Tadepalli SM, Jeune MR, Shearer TW, Chen ZB, Chen L, Anderson DL, Becherer JD, De Los Frailes M, Colilla FJ.

J Med Chem. 2009 Dec 24;52(24):7962-5. doi: 10.1021/jm901434t.

PMID:
19902954
10.

Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.

Wolkenberg SE, Zhao Z, Wisnoski DD, Leister WH, O'Brien J, Lemaire W, Williams DL Jr, Jacobson MA, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Gibson C, Ma BK, Polsky-Fisher SL, Lindsley CW, Hartman GD.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1492-5. doi: 10.1016/j.bmcl.2009.01.015. Epub 2009 Jan 10.

PMID:
19181525
11.

Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.

Zhao Z, Wisnoski DD, O'Brien JA, Lemaire W, Williams DL Jr, Jacobson MA, Wittman M, Ha SN, Schaffhauser H, Sur C, Pettibone DJ, Duggan ME, Conn PJ, Hartman GD, Lindsley CW.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1386-91. Epub 2006 Dec 3.

PMID:
17210250
12.

p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones.

Natarajan SR, Wisnoski DD, Thompson JE, O'Neill EA, O'Keefe SJ.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4400-4. Epub 2006 Jun 5.

PMID:
16750629
13.

Acetonitrile/water gas-phase reaction products observed by use of atmospheric pressure chemical ionization: adducts formed with sulfonamides.

Ross CW 3rd, Coddington AB, Murphy JS, Wisnoski DD, Zartman CB, Ramjit HG.

Rapid Commun Mass Spectrom. 2005;19(5):667-73.

PMID:
15700234
14.

A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

Kinney GG, O'Brien JA, Lemaire W, Burno M, Bickel DJ, Clements MK, Chen TB, Wisnoski DD, Lindsley CW, Tiller PR, Smith S, Jacobson MA, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2005 Apr;313(1):199-206. Epub 2004 Dec 17.

PMID:
15608073
15.

Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.

Lindsley CW, Wisnoski DD, Leister WH, O'brien JA, Lemaire W, Williams DL Jr, Burno M, Sur C, Kinney GG, Pettibone DJ, Tiller PR, Smith S, Duggan ME, Hartman GD, Conn PJ, Huff JR.

J Med Chem. 2004 Nov 18;47(24):5825-8.

PMID:
15537338
16.

Efficient synthesis of imidazoles from aldehydes and 1,2-diketones using microwave irradiation.

Wolkenberg SE, Wisnoski DD, Leister WH, Wang Y, Zhao Z, Lindsley CW.

Org Lett. 2004 Apr 29;6(9):1453-6.

PMID:
15101765
17.

A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain.

O'Brien JA, Lemaire W, Wittmann M, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Schaffhauser HJ, Rowe B, Sur C, Duggan ME, Pettibone DJ, Conn PJ, Williams DL Jr.

J Pharmacol Exp Ther. 2004 May;309(2):568-77. Epub 2004 Jan 27.

PMID:
14747613
18.

Difference in mGluR5 interaction between positive allosteric modulators from two structural classes.

Williams DL Jr, O'Brien JA, Lemaire W, Chen TB, Chang RS, Jacobson MA, Ha SN, Wisnoski DD, Lindsley CW, Sur C, Duggan ME, Pettibone DJ, Conn PJ.

Ann N Y Acad Sci. 2003 Nov;1003:481-4. No abstract available.

PMID:
14684495
19.

p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.

Natarajan SR, Wisnoski DD, Singh SB, Stelmach JE, O'Neill EA, Schwartz CD, Thompson CM, Fitzgerald CE, O'Keefe SJ, Kumar S, Hop CE, Zaller DM, Schmatz DM, Doherty JB.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):273-6.

PMID:
12482438

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