Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen-Reference-Cited by-同舟云学术

Discovery of 2-phenoxyacetamides as inhibitors of the Wnt-depalmitoleating enzyme NOTUM from an X-ray fragment screen

Published:2019 Issue:8 Volume:10 Page:1361-1369
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Atkinson Benjamin N.¹²³⁴^ORCID,Steadman David¹²³⁴^ORCID,Zhao Yuguang⁵⁶⁷⁸⁴,Sipthorp James¹²³⁴⁹^ORCID,Vecchia Luca⁵⁶⁷⁸⁴^ORCID,Ruza Reinis R.⁵⁶⁷⁸⁴^ORCID,Jeganathan Fiona¹²³⁴,Lines Georgie¹²³⁴,Frew Sarah¹²³⁴,Monaghan Amy¹²³⁴,Kjær Svend⁹³⁴,Bictash Magda¹²³⁴,Jones E. Yvonne⁵⁶⁷⁸⁴^ORCID,Fish Paul V.¹²³⁴⁹^ORCID

Affiliation:

1. Alzheimer's Research UK UCL Drug Discovery Institute

2. University College London

3. London

4. UK

5. Division of Structural Biology

6. Wellcome Centre for Human Genetics

7. University of Oxford

8. Oxford

9. The Francis Crick Institute

Abstract

Optimization of fragment hit 3 identified isoquinoline 45 as a potent inhibitor of NOTUM with an unexpected flipped binding mode.