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Items: 1 to 20 of 85

1.

HTS reporter displacement assay for fragment screening and fragment evolution toward leads with optimized binding kinetics, binding selectivity, and thermodynamic signature.

Neumann L, von K├Ânig K, Ullmann D.

Methods Enzymol. 2011;493:299-320. doi: 10.1016/B978-0-12-381274-2.00012-1.

PMID:
21371596
2.

Thermodynamic characterization of pyrazole and azaindole derivatives binding to p38 mitogen-activated protein kinase using Biacore T100 technology and van't Hoff analysis.

Papalia GA, Giannetti AM, Arora N, Myszka DG.

Anal Biochem. 2008 Dec 15;383(2):255-64. doi: 10.1016/j.ab.2008.08.010. Epub 2008 Aug 19.

PMID:
18774767
3.

Technological advances in high-throughput screening.

Liu B, Li S, Hu J.

Am J Pharmacogenomics. 2004;4(4):263-76. Review.

PMID:
15287820
4.

Lead generation and examples opinion regarding how to follow up hits.

Orita M, Ohno K, Warizaya M, Amano Y, Niimi T.

Methods Enzymol. 2011;493:383-419. doi: 10.1016/B978-0-12-381274-2.00015-7.

PMID:
21371599
5.

Fragment screening: an introduction.

Leach AR, Hann MM, Burrows JN, Griffen EJ.

Mol Biosyst. 2006 Sep;2(9):430-46.

PMID:
17153140
6.

Discovery of highly selective inhibitors of p38alpha.

Popa-Burke I, Birkos S, Blackwell L, Cheatham L, Clark J, Dickson JK Jr, Galasinski S, Janzen WP, Mendoza J, Miller JL, Mohney RP, Steed PM, Hodge CN.

Curr Top Med Chem. 2005;5(10):941-51. Review.

PMID:
16178739
7.

Biomolecular interaction analysis in drug discovery using surface plasmon resonance technology.

Huber W, Mueller F.

Curr Pharm Des. 2006;12(31):3999-4021. Review.

PMID:
17100609
8.

Effective progression of nuclear magnetic resonance-detected fragment hits.

Eaton HL, Wyss DF.

Methods Enzymol. 2011;493:447-68. doi: 10.1016/B978-0-12-381274-2.00017-0.

PMID:
21371601
9.

Thermodynamics of protein-ligand interactions: history, presence, and future aspects.

Perozzo R, Folkers G, Scapozza L.

J Recept Signal Transduct Res. 2004 Feb;24(1-2):1-52. Review.

PMID:
15344878
10.

Structure-guided fragment screening for lead discovery.

Verdonk ML, Hartshorn MJ.

Curr Opin Drug Discov Devel. 2004 Jul;7(4):404-10. Review.

PMID:
15338949
11.

The discovery of novel protein kinase inhibitors by using fragment-based high-throughput x-ray crystallography.

Gill A, Cleasby A, Jhoti H.

Chembiochem. 2005 Mar;6(3):506-12. Review.

PMID:
15696598
12.

The application of high-throughput screening to novel lead discovery.

Kenny BA, Bushfield M, Parry-Smith DJ, Fogarty S, Treherne JM.

Prog Drug Res. 1998;51:245-69. Review.

PMID:
9949864
14.

From experimental design to validated hits a comprehensive walk-through of fragment lead identification using surface plasmon resonance.

Giannetti AM.

Methods Enzymol. 2011;493:169-218. doi: 10.1016/B978-0-12-381274-2.00008-X.

PMID:
21371592
15.

Electron density guided fragment-based drug design--a lead generation example.

Abad MC, Gibbs AC, Zhang X.

Methods Enzymol. 2011;493:487-508. doi: 10.1016/B978-0-12-381274-2.00019-4.

PMID:
21371603
16.

The SeeDs approach: integrating fragments into drug discovery.

Hubbard RE, Davis B, Chen I, Drysdale MJ.

Curr Top Med Chem. 2007;7(16):1568-81. Review.

PMID:
17979768
17.

An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes.

Albert JS, Blomberg N, Breeze AL, Brown AJ, Burrows JN, Edwards PD, Folmer RH, Geschwindner S, Griffen EJ, Kenny PW, Nowak T, Olsson LL, Sanganee H, Shapiro AB.

Curr Top Med Chem. 2007;7(16):1600-29. Review.

PMID:
17979771
18.

Adopting a practical statistical approach for evaluating assay agreement in drug discovery.

Sun D, Whitty A, Papadatos J, Newman M, Donnelly J, Bowes S, Josiah S.

J Biomol Screen. 2005 Aug;10(5):508-16.

PMID:
16093560
19.

Affinity-based screening techniques for enhancing lead discovery.

Comess KM, Schurdak ME.

Curr Opin Drug Discov Devel. 2004 Jul;7(4):411-6. Review.

PMID:
15338950
20.

Using computational techniques in fragment-based drug discovery.

Desjarlais RL.

Methods Enzymol. 2011;493:137-55. doi: 10.1016/B978-0-12-381274-2.00006-6.

PMID:
21371590

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