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Predictions of ligand selectivity from absolute binding free energy calculations

Abstract:

Binding selectivity is a requirement for the development of a safe drug, and it is a critical property for chemical probes used in preclinical target validation. Engineering selectivity adds considerable complexity to the rational design of new drugs, as it involves the optimization of multiple binding affinities. Computationally, the prediction of binding selectivity is a challenge and general applicable methodologies are still not available to the computational and medicinal chemistry commu...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1021/jacs.6b11467

Authors


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Institution:
University of Oxford
Division:
MSD
Department:
Biochemistry
Role:
Author
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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
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Institution:
University of Oxford
Oxford college:
Lady Margaret Hall
Role:
Author
More from this funder
Funding agency for:
Aldeghi, M
Grant:
EP/G037280/1
More from this funder
Funding agency for:
Aldeghi, M
Grant:
EP/G037280/1
Publisher:
American Chemical Society
Journal:
Journal of the American Chemical Society More from this journal
Volume:
139
Issue:
2
Pages:
946–957
Publication date:
2016-12-23
DOI:
EISSN:
1520-5126
ISSN:
0002-7863
Language:
English
Pubs id:
pubs:667542
UUID:
uuid:2e19242c-28eb-405c-aedd-0ad3b2bd4158
Local pid:
pubs:667542
Source identifiers:
667542
Deposit date:
2017-01-16

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