Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe-Reference-Cited by-同舟云学术

Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe

Published:2018 Issue:45 Volume:9 Page:8608-8618
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Lebraud Honorine¹²³,Surova Olga¹²³⁴⁵,Courtin Aurélie¹²³,O'Reilly Marc¹²³,Valenzano Chiara R.¹²³,Nordlund Pär⁴⁵⁶⁷⁸,Heightman Tom D.¹²³^ORCID

Affiliation:

1. Astex Pharmaceuticals

2. Cambridge

3. UK

4. Department of Oncology-Pathology

5. Karolinska Institute

6. CCK R8:01

7. Karolinska Hospital

8. 171 76 Stockholm

Abstract

Target engagement is a key concept in drug discovery and its direct measurement can provide a quantitative understanding of drug efficacy and/or toxicity.

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2018/SC/C8SC02754D

Reference27 articles.

1. Can the flow of medicines be improved? Fundamental pharmacokinetic and pharmacological principles toward improving Phase II survival

2. Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework

3. Target validation using chemical probes

4. Determining target engagement in living systems

5. Small-Molecule Target Engagement in Cells

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