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Items: 45

1.

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

Fell JB, Fischer JP, Baer BR, Ballard J, Blake JF, Bouhana K, Brandhuber BJ, Briere DM, Burgess LE, Burkard MR, Chiang H, Chicarelli MJ, Davidson K, Gaudino JJ, Hallin J, Hanson L, Hee K, Hicken EJ, Hinklin RJ, Marx MA, Mejia MJ, Olson P, Savechenkov P, Sudhakar N, Tang TP, Vigers GP, Zecca H, Christensen JG.

ACS Med Chem Lett. 2018 Nov 7;9(12):1230-1234. doi: 10.1021/acsmedchemlett.8b00382. eCollection 2018 Dec 13.

PMID:
30613331
2.

Use of QSPR Modeling to Characterize In Vitro Binding of Drugs to a Gut-Restricted Polymer.

Brew CT, Blake JF, Mistry A, Liu F, Carreno D, Madsen D, Mu Y, Mayo M, Stahl W, Matthews D, Maclean D, Harrison S.

Pharm Res. 2018 Mar 8;35(4):89. doi: 10.1007/s11095-018-2356-y.

3.

A Next-Generation TRK Kinase Inhibitor Overcomes Acquired Resistance to Prior TRK Kinase Inhibition in Patients with TRK Fusion-Positive Solid Tumors.

Drilon A, Nagasubramanian R, Blake JF, Ku N, Tuch BB, Ebata K, Smith S, Lauriault V, Kolakowski GR, Brandhuber BJ, Larsen PD, Bouhana KS, Winski SL, Hamor R, Wu WI, Parker A, Morales TH, Sullivan FX, DeWolf WE, Wollenberg LA, Gordon PR, Douglas-Lindsay DN, Scaltriti M, Benayed R, Raj S, Hanusch B, Schram AM, Jonsson P, Berger MF, Hechtman JF, Taylor BS, Andrews S, Rothenberg SM, Hyman DM.

Cancer Discov. 2017 Sep;7(9):963-972. doi: 10.1158/2159-8290.CD-17-0507. Epub 2017 Jun 3.

4.

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.

Blake JF, Burkard M, Chan J, Chen H, Chou KJ, Diaz D, Dudley DA, Gaudino JJ, Gould SE, Grina J, Hunsaker T, Liu L, Martinson M, Moreno D, Mueller L, Orr C, Pacheco P, Qin A, Rasor K, Ren L, Robarge K, Shahidi-Latham S, Stults J, Sullivan F, Wang W, Yin J, Zhou A, Belvin M, Merchant M, Moffat J, Schwarz JB.

J Med Chem. 2016 Jun 23;59(12):5650-60. doi: 10.1021/acs.jmedchem.6b00389. Epub 2016 Jun 7.

PMID:
27227380
5.

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

Ren L, Grina J, Moreno D, Blake JF, Gaudino JJ, Garrey R, Metcalf AT, Burkard M, Martinson M, Rasor K, Chen H, Dean B, Gould SE, Pacheco P, Shahidi-Latham S, Yin J, West K, Wang W, Moffat JG, Schwarz JB.

J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11.

PMID:
25603482
6.

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB.

Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068. Epub 2014 Apr 29.

PMID:
24813737
7.

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ.

J Med Chem. 2012 Sep 27;55(18):8110-27. Epub 2012 Sep 18.

PMID:
22934575
8.

Single-agent inhibition of Chk1 is antiproliferative in human cancer cell lines in vitro and inhibits tumor xenograft growth in vivo.

Davies KD, Humphries MJ, Sullivan FX, von Carlowitz I, Le Huerou Y, Mohr PJ, Wang B, Blake JF, Lyon MA, Gunawardana I, Chicarelli M, Wallace E, Gross S.

Oncol Res. 2011;19(7):349-63.

PMID:
21936404
9.

Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Xu R, Banka A, Blake JF, Mitchell IS, Wallace EM, Bencsik JR, Kallan NC, Spencer KL, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26.

PMID:
21420856
10.

Discovery and SAR of spirochromane Akt inhibitors.

Kallan NC, Spencer KL, Blake JF, Xu R, Heizer J, Bencsik JR, Mitchell IS, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18.

PMID:
21392984
11.

Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Bencsik JR, Xiao D, Blake JF, Kallan NC, Mitchell IS, Spencer KL, Xu R, Gloor SL, Martinson M, Risom T, Woessner RD, Dizon F, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ, Prior WW, Murray LJ.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7037-41. doi: 10.1016/j.bmcl.2010.09.112. Epub 2010 Sep 29.

PMID:
20971641
12.

Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.

PMID:
20810279
13.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides.

de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Adjabeng G, Elworthy TR, Li J, Wang B, Bamberg JT, Harris SF, Wong A, Leveque VJ, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Larrabee S, Brandl M, Briggs A, Sukhtankar S, Farrell R.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5652-6. doi: 10.1016/j.bmcl.2009.08.022. Epub 2009 Aug 8.

PMID:
19709881
14.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: synthesis and optimization studies of benzothiazine-substituted tetramic acids.

de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Zhao J, Elworthy TR, Tracy J, Chin E, Li J, Lui A, Wang B, Oshiro C, Harris SF, Ghate M, Leveque VJ, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Fitch B, Brandl M, Masjedizadeh M, Wu SY, de Keczer S, Voronin T.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5648-51. doi: 10.1016/j.bmcl.2009.08.023. Epub 2009 Aug 8.

PMID:
19700319
15.

Non-nucleoside inhibitors of HCV polymerase NS5B. Part 2: Synthesis and structure-activity relationships of benzothiazine-substituted quinolinediones.

de Vicente J, Hendricks RT, Smith DB, Fell JB, Fischer J, Spencer SR, Stengel PJ, Mohr P, Robinson JE, Blake JF, Hilgenkamp RK, Yee C, Adjabeng G, Elworthy TR, Tracy J, Chin E, Li J, Wang B, Bamberg JT, Stephenson R, Oshiro C, Harris SF, Ghate M, Leveque V, Najera I, Le Pogam S, Rajyaguru S, Ao-Ieong G, Alexandrova L, Larrabee S, Brandl M, Briggs A, Sukhtankar S, Farrell R, Xu B.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3642-6. doi: 10.1016/j.bmcl.2009.05.004. Epub 2009 May 7.

PMID:
19457662
16.

Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors.

Hendricks RT, Fell JB, Blake JF, Fischer JP, Robinson JE, Spencer SR, Stengel PJ, Bernacki AL, Leveque VJ, Le Pogam S, Rajyaguru S, Najera I, Josey JA, Harris JR, Swallow S.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3637-41. doi: 10.1016/j.bmcl.2009.04.119. Epub 2009 May 3.

PMID:
19447623
17.

3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase.

Hendricks RT, Spencer SR, Blake JF, Fell JB, Fischer JP, Stengel PJ, Leveque VJ, Lepogam S, Rajyaguru S, Najera I, Josey JA, Swallow S.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):410-4. doi: 10.1016/j.bmcl.2008.11.060. Epub 2008 Nov 20.

PMID:
19070486
18.

Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors.

Eary CT, Jones ZS, Groneberg RD, Burgess LE, Mareska DA, Drew MD, Blake JF, Laird ER, Balachari D, O'Sullivan M, Allen A, Marsh V.

Bioorg Med Chem Lett. 2007 May 1;17(9):2608-13. Epub 2007 Feb 8.

PMID:
17331716
19.
20.

Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.

Wallace EM, Lyssikatos J, Blake JF, Seo J, Yang HW, Yeh TC, Perrier M, Jarski H, Marsh V, Poch G, Livingston MG, Otten J, Hingorani G, Woessner R, Lee P, Winkler J, Koch K.

J Med Chem. 2006 Jan 26;49(2):441-4.

PMID:
16420026
21.

Integrating cheminformatic analysis in combinatorial chemistry.

Blake JF.

Curr Opin Chem Biol. 2004 Aug;8(4):407-11. Review.

PMID:
15288251
22.

Structure-based generation of viable leads from small combinatorial libraries.

Laird ER, Blake JF.

Curr Opin Drug Discov Devel. 2004 May;7(3):354-9. Review.

PMID:
15216940
23.
24.

Consensus scoring for ligand/protein interactions.

Clark RD, Strizhev A, Leonard JM, Blake JF, Matthew JB.

J Mol Graph Model. 2002 Jan;20(4):281-95.

PMID:
11858637
25.
26.

Quinazolin-4-one alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists: structure-activity relationship of the C-2 side chain tether.

Chenard BL, Welch WM, Blake JF, Butler TW, Reinhold A, Ewing FE, Menniti FS, Pagnozzi MJ.

J Med Chem. 2001 May 24;44(11):1710-7.

PMID:
11356106
27.

Visualizing substructural fingerprints.

Clark RD, Patterson DE, Soltanshahi F, Blake JF, Matthew JB.

J Mol Graph Model. 2000 Aug-Oct;18(4-5):404-11, 527-32.

PMID:
11143558
28.

Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.

Robinson RP, Laird ER, Blake JF, Bordner J, Donahue KM, Lopresti-Morrow LL, Mitchell PG, Reese MR, Reeves LM, Stam EJ, Yocum SA.

J Med Chem. 2000 Jun 15;43(12):2293-6. No abstract available.

PMID:
10882354
29.

Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.

Allen MP, Blake JF, Bryce DK, Haggan ME, Liras S, McLean S, Segelstein BE.

Bioorg Med Chem Lett. 2000 Mar 20;10(6):523-6.

PMID:
10741545
30.

Chemoinformatics - predicting the physicochemical properties of 'drug-like' molecules.

Blake JF.

Curr Opin Biotechnol. 2000 Feb;11(1):104-7. Review.

PMID:
10679344
31.

Inclusion complexation of ziprasidone mesylate with beta-cyclodextrin sulfobutyl ether.

Kim Y, Oksanen DA, Massefski W Jr, Blake JF, Duffy EM, Chrunyk B.

J Pharm Sci. 1998 Dec;87(12):1560-7.

PMID:
10189267
32.

Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.

Reiter LA, Rizzi JP, Pandit J, Lasut MJ, McGahee SM, Parikh VD, Blake JF, Danley DE, Laird ER, Lopez-Anaya A, Lopresti-Morrow LL, Mansour MN, Martinelli GJ, Mitchell PG, Owens BS, Pauly TA, Reeves LM, Schulte GK, Yocum SA.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):127-32.

PMID:
10021913
33.

(3R,4S)-3-[4-(4-fluorophenyl)-4-hydroxypiperidin-1-yl]chroman-4,7-diol: a conformationally restricted analogue of the NR2B subtype-selective NMDA antagonist (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)- 1-propanol.

Butler TW, Blake JF, Bordner J, Butler P, Chenard BL, Collins MA, DeCosta D, Ducat MJ, Eisenhard ME, Menniti FS, Pagnozzi MJ, Sands SB, Segelstein BE, Volberg W, White WF, Zhao D.

J Med Chem. 1998 Mar 26;41(7):1172-84.

PMID:
9544217
34.

Glucose transport-enhancing and hypoglycemic activity of 2-methyl-2-phenoxy-3-phenylpropanoic acids.

Sarges R, Hank RF, Blake JF, Bordner J, Bussolotti DL, Hargrove DM, Treadway JL, Gibbs EM.

J Med Chem. 1996 Nov 22;39(24):4783-803.

PMID:
8941393
35.

Computation of brain-blood partitioning of organic solutes via free energy calculations.

Lombardo F, Blake JF, Curatolo WJ.

J Med Chem. 1996 Nov 22;39(24):4750-5.

PMID:
8941388
36.

Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.

Villalobos A, Blake JF, Biggers CK, Butler TW, Chapin DS, Chen YL, Ives JL, Jones SB, Liston DR, Nagel AA, et al.

J Med Chem. 1994 Aug 19;37(17):2721-34.

PMID:
8064800
37.

Antagonism of baclofen-induced depression of whole-cell synaptic currents in spinal dorsal horn neurones by the potent GABAB antagonist CGP55845.

Blake JF, Cao CQ, Headley PM, Collingridge GL, Brugger F, Evans RH.

Neuropharmacology. 1993 Dec;32(12):1437-40.

PMID:
8152534
38.

Involvement of excitatory amino acid receptors in long-term potentiation in the Schaffer collateral-commissural pathway of rat hippocampal slices.

Collingridge GL, Blake JF, Brown MW, Bashir ZI, Ryan E.

Can J Physiol Pharmacol. 1991 Jul;69(7):1084-90. Review.

PMID:
1659488
39.

Electrogenic uptake contributes a major component of the depolarizing action of L-glutamate in rat hippocampal slices.

Frenguelli BG, Blake JF, Brown MW, Collingridge GL.

Br J Pharmacol. 1991 Feb;102(2):355-62.

40.

Hill coefficients and the logistic equation.

Barlow R, Blake JF.

Trends Pharmacol Sci. 1989 Nov;10(11):440-1. No abstract available.

PMID:
2609430
41.

6-Cyano-7-nitroquinoxaline-2,3-dione as an excitatory amino acid antagonist in area CA1 of rat hippocampus.

Blake JF, Yates RG, Brown MW, Collingridge GL.

Br J Pharmacol. 1989 May;97(1):71-6.

42.
43.
44.

The effect of nicotine on motoneurones of the immature rat spinal cord in vitro.

Blake JF, Evans RH, Smith DA.

Br J Pharmacol. 1987 Jan;90(1):167-73.

45.

ON THE ORIGIN OF ANCIENT QUARTZ ROCKS.

Blake JF.

Science. 1894 Mar 16;23(580):141-2. No abstract available.

PMID:
17753030

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