1
|
Breast tumor cells with PI3K mutation or HER2 amplification are selectively addicted to Akt signaling.
|
PLoS One
|
2008
|
4.12
|
2
|
Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors.
|
Biochem J
|
2005
|
3.58
|
3
|
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
|
Bioorg Med Chem Lett
|
2005
|
3.50
|
4
|
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members.
|
Mol Cancer Ther
|
2005
|
2.23
|
5
|
An allosteric Akt inhibitor effectively blocks Akt signaling and tumor growth with only transient effects on glucose and insulin levels in vivo.
|
Cancer Biol Ther
|
2010
|
1.77
|
6
|
Inhibition of a mitotic motor protein: where, how, and conformational consequences.
|
J Mol Biol
|
2004
|
1.58
|
7
|
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
|
Bioorg Med Chem Lett
|
2008
|
1.44
|
8
|
Characterization of Notch1 antibodies that inhibit signaling of both normal and mutated Notch1 receptors.
|
PLoS One
|
2010
|
1.41
|
9
|
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
|
Bioorg Med Chem Lett
|
2005
|
1.27
|
10
|
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
|
Bioorg Med Chem Lett
|
2005
|
1.19
|
11
|
Glycoengineered Pichia produced anti-HER2 is comparable to trastuzumab in preclinical study.
|
MAbs
|
2011
|
1.08
|
12
|
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
|
J Med Chem
|
2008
|
1.02
|
13
|
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
|
Bioorg Med Chem Lett
|
2007
|
0.98
|
14
|
Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.
|
Bioorg Med Chem Lett
|
2006
|
0.86
|
15
|
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
|
Bioorg Med Chem Lett
|
2008
|
0.86
|
16
|
Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.
|
J Med Chem
|
2003
|
0.86
|
17
|
Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.
|
Bioorg Med Chem Lett
|
2007
|
0.86
|
18
|
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
|
Bioorg Med Chem Lett
|
2006
|
0.83
|
19
|
3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.
|
J Med Chem
|
2002
|
0.81
|
20
|
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
|
Bioorg Med Chem Lett
|
2007
|
0.80
|
21
|
Rapid assembly of diverse and potent allosteric Akt inhibitors.
|
Bioorg Med Chem Lett
|
2007
|
0.80
|
22
|
Development of pyridopyrimidines as potent Akt1/2 inhibitors.
|
Bioorg Med Chem Lett
|
2008
|
0.79
|
23
|
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
|
Bioorg Med Chem Lett
|
2002
|
0.78
|
24
|
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
|
Bioorg Med Chem Lett
|
2007
|
0.77
|
25
|
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
|
Bioorg Med Chem Lett
|
2002
|
0.75
|
26
|
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
|
Bioorg Med Chem Lett
|
2004
|
0.75
|