1
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The crystal structure of the quorum sensing protein TraR bound to its autoinducer and target DNA.
|
EMBO J
|
2002
|
3.11
|
2
|
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
|
J Med Chem
|
2008
|
3.09
|
3
|
In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor.
|
J Virol
|
2003
|
2.55
|
4
|
Molecular insights into quorum sensing in the human pathogen Pseudomonas aeruginosa from the structure of the virulence regulator LasR bound to its autoinducer.
|
J Biol Chem
|
2007
|
1.89
|
5
|
A novel, inducible, eukaryotic gene expression system based on the quorum-sensing transcription factor TraR.
|
EMBO Rep
|
2003
|
1.06
|
6
|
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
|
J Med Chem
|
2006
|
0.94
|
7
|
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
|
J Med Chem
|
2007
|
0.91
|
8
|
Identification of substituted pyrazolo[1,5-a]quinazolin-5(4H)-one as potent poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors.
|
Bioorg Med Chem Lett
|
2009
|
0.88
|
9
|
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
|
J Med Chem
|
2007
|
0.88
|
10
|
A functionally orthogonal estrogen receptor-based transcription switch specifically induced by a nonsteroid synthetic ligand.
|
Chem Biol
|
2005
|
0.86
|
11
|
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
|
J Med Chem
|
2006
|
0.85
|
12
|
Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.
|
J Med Chem
|
2009
|
0.81
|
13
|
Crystallization and preliminary X-ray diffraction studies of the transcriptional regulator TraR bound to its cofactor and to a specific DNA sequence.
|
Acta Crystallogr D Biol Crystallogr
|
2002
|
0.77
|
14
|
Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.
|
Bioorg Med Chem Lett
|
2009
|
0.76
|
15
|
Novel, potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures.
|
Bioorg Med Chem Lett
|
2003
|
0.76
|
16
|
Identification of aminoethyl pyrrolo dihydroisoquinolinones as novel poly(ADP-ribose) polymerase-1 inhibitors.
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
17
|
Development of substituted 6-[4-fluoro-3-(piperazin-1-ylcarbonyl)benzyl]-4,5-dimethylpyridazin-3(2H)-ones as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors active in BRCA deficient cells.
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
18
|
Evolution, synthesis and SAR of tripeptide alpha-ketoacid inhibitors of the hepatitis C virus NS3/NS4A serine protease.
|
Bioorg Med Chem Lett
|
2002
|
0.75
|
19
|
Identification and SAR of novel pyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1).
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
20
|
Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center.
|
Bioorg Med Chem Lett
|
2009
|
0.75
|
21
|
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
|
Bioorg Med Chem Lett
|
2008
|
0.75
|
22
|
(1)H, (13)C and (15)N backbone assignments for the ligand binding domain of the Pseudomonas aeruginosa virulence regulator LasR.
|
Biomol NMR Assign
|
2007
|
0.75
|