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Results: 1 to 20 of 115

1.

Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.

Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, Kalgutkar AS, Klug-McLeod J, Garcia-Irizarry C, Li J, Lippa B, Price DA, Southers JA, Walker DP, Wei L, Xiao J, Zawistoski MP, Zhao X.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7523-9. doi: 10.1016/j.bmcl.2012.10.039. Epub 2012 Oct 16.

PMID:
23153798
[PubMed - indexed for MEDLINE]
2.

Displacement assay for the detection of stabilizers of inactive kinase conformations.

Klüter S, Grütter C, Naqvi T, Rabiller M, Simard JR, Pawar V, Getlik M, Rauh D.

J Med Chem. 2010 Jan 14;53(1):357-67. doi: 10.1021/jm901297e.

PMID:
19928858
[PubMed - indexed for MEDLINE]
3.

Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design.

Han S, Mistry A, Chang JS, Cunningham D, Griffor M, Bonnette PC, Wang H, Chrunyk BA, Aspnes GE, Walker DP, Brosius AD, Buckbinder L.

J Biol Chem. 2009 May 8;284(19):13193-201. doi: 10.1074/jbc.M809038200. Epub 2009 Feb 25.

PMID:
19244237
[PubMed - indexed for MEDLINE]
Free PMC Article
4.

Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.

Wenglowsky S, Moreno D, Laird ER, Gloor SL, Ren L, Risom T, Rudolph J, Sturgis HL, Voegtli WC.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6237-41. doi: 10.1016/j.bmcl.2012.08.007. Epub 2012 Aug 10.

PMID:
22954737
[PubMed - indexed for MEDLINE]
5.

Identification of small molecule inhibitors of proline-rich tyrosine kinase 2 (Pyk2) with osteogenic activity in osteoblast cells.

Allen JG, Lee MR, Han CY, Scherrer J, Flynn S, Boucher C, Zhao H, O'Connor AB, Roveto P, Bauer D, Graceffa R, Richards WG, Babij P.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4924-8. doi: 10.1016/j.bmcl.2009.07.084. Epub 2009 Jul 22.

PMID:
19648005
[PubMed - indexed for MEDLINE]
6.

Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.

Liu H, Kuhn C, Feru F, Jacques SL, Deshmukh GD, Ye P, Rennie GR, Johnson T, Kazmirski S, Low S, Coli R, Ding YH, Cheng AC, Tecle H, English JM, Stanton R, Wu JC.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4885-91. doi: 10.1016/j.bmcl.2010.06.073. Epub 2010 Jun 17.

PMID:
20620059
[PubMed - indexed for MEDLINE]
7.

Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38α.

Getlik M, Grütter C, Simard JR, Nguyen HD, Robubi A, Aust B, van Otterlo WA, Rauh D.

Eur J Med Chem. 2012 Feb;48:1-15. doi: 10.1016/j.ejmech.2011.11.019. Epub 2011 Nov 18.

PMID:
22154891
[PubMed - indexed for MEDLINE]
8.

Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.

Walker DP, Bi FC, Kalgutkar AS, Bauman JN, Zhao SX, Soglia JR, Aspnes GE, Kung DW, Klug-McLeod J, Zawistoski MP, McGlynn MA, Oliver R, Dunn M, Li JC, Richter DT, Cooper BA, Kath JC, Hulford CA, Autry CL, Luzzio MJ, Ung EJ, Roberts WG, Bonnette PC, Buckbinder L, Mistry A, Griffor MC, Han S, Guzman-Perez A.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6071-7. doi: 10.1016/j.bmcl.2008.10.030. Epub 2008 Oct 11.

PMID:
18951788
[PubMed - indexed for MEDLINE]
9.

Discovery and characterization of novel allosteric FAK inhibitors.

Iwatani M, Iwata H, Okabe A, Skene RJ, Tomita N, Hayashi Y, Aramaki Y, Hosfield DJ, Hori A, Baba A, Miki H.

Eur J Med Chem. 2013 Mar;61:49-60. doi: 10.1016/j.ejmech.2012.06.035. Epub 2012 Jun 26.

PMID:
22819505
[PubMed - indexed for MEDLINE]
10.

Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitors.

Hou Z, Oishi S, Suzuki Y, Kure T, Nakanishi I, Hirasawa A, Tsujimoto G, Ohno H, Fujii N.

Org Biomol Chem. 2013 May 28;11(20):3288-96. doi: 10.1039/c3ob40223a.

PMID:
23535832
[PubMed - indexed for MEDLINE]
11.

Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships.

Wenglowsky S, Ahrendt KA, Buckmelter AJ, Feng B, Gloor SL, Gradl S, Grina J, Hansen JD, Laird ER, Lunghofer P, Mathieu S, Moreno D, Newhouse B, Ren L, Risom T, Rudolph J, Seo J, Sturgis HL, Voegtli WC, Wen Z.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5533-7. doi: 10.1016/j.bmcl.2011.06.097. Epub 2011 Jul 2.

PMID:
21802293
[PubMed - indexed for MEDLINE]
12.

5-amino-pyrazoles as potent and selective p38α inhibitors.

Das J, Moquin RV, Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Newitt JA, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6886-9. doi: 10.1016/j.bmcl.2010.10.034. Epub 2010 Oct 13.

PMID:
21035336
[PubMed - indexed for MEDLINE]
13.

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.

Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6529-33. doi: 10.1016/j.bmcl.2009.10.053. Epub 2009 Oct 24.

PMID:
19857967
[PubMed - indexed for MEDLINE]
14.

A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.

Honma T, Yoshizumi T, Hashimoto N, Hayashi K, Kawanishi N, Fukasawa K, Takaki T, Ikeura C, Ikuta M, Suzuki-Takahashi I, Hayama T, Nishimura S, Morishima H.

J Med Chem. 2001 Dec 20;44(26):4628-40.

PMID:
11741480
[PubMed - indexed for MEDLINE]
15.

Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.

Berger DM, Torres N, Dutia M, Powell D, Ciszewski G, Gopalsamy A, Levin JI, Kim KH, Xu W, Wilhelm J, Hu Y, Collins K, Feldberg L, Kim S, Frommer E, Wojciechowicz D, Mallon R.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6519-23. doi: 10.1016/j.bmcl.2009.10.049. Epub 2009 Oct 26.

PMID:
19864136
[PubMed - indexed for MEDLINE]
16.

The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay.

Tecle H, Feru F, Liu H, Kuhn C, Rennie G, Morris M, Shao J, Cheng AC, Gikunju D, Miret J, Coli R, Xi SH, Clugston SL, Low S, Kazmirski S, Ding YH, Cao Q, Johnson TL, Deshmukh GD, DiNitto JP, Wu JC, English JM.

Chem Biol Drug Des. 2009 Dec;74(6):547-59. doi: 10.1111/j.1747-0285.2009.00884.x. Epub 2009 Oct 20.

PMID:
19843080
[PubMed - indexed for MEDLINE]
17.

Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.

Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. Epub 2007 Sep 8.

PMID:
17904366
[PubMed - indexed for MEDLINE]
18.

Discovery of highly potent and selective type I B-Raf kinase inhibitors.

Wang X, Berger DM, Salaski EJ, Torres N, Hu Y, Levin JI, Powell D, Wojciechowicz D, Collins K, Frommer E.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6571-4. doi: 10.1016/j.bmcl.2009.10.030. Epub 2009 Oct 13.

PMID:
19854649
[PubMed - indexed for MEDLINE]
19.

Discovery of 4-azaindoles as novel inhibitors of c-Met kinase.

Porter J, Lumb S, Franklin RJ, Gascon-Simorte JM, Calmiano M, Riche KL, Lallemand B, Keyaerts J, Edwards H, Maloney A, Delgado J, King L, Foley A, Lecomte F, Reuberson J, Meier C, Batchelor M.

Bioorg Med Chem Lett. 2009 May 15;19(10):2780-4. doi: 10.1016/j.bmcl.2009.03.110. Epub 2009 Mar 27.

PMID:
19369077
[PubMed - indexed for MEDLINE]
20.

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

Dai Y, Hartandi K, Soni NB, Pease LJ, Reuter DR, Olson AM, Osterling DJ, Doktor SZ, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):386-90. Epub 2007 Oct 17.

PMID:
18023347
[PubMed - indexed for MEDLINE]

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