5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit-Reference-Cited by-同舟云学术

5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit

Published:2020-10-30 Issue:21 Volume:63 Page:12942-12956
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Mahy William¹,Willis Nicky J.¹,Zhao Yuguang²^ORCID,Woodward Hannah L.¹^ORCID,Svensson Fredrik¹³^ORCID,Sipthorp James¹³,Vecchia Luca²,Ruza Reinis R.²,Hillier James²,Kjær Svend³,Frew Sarah¹,Monaghan Amy¹,Bictash Magda¹,Salinas Patricia C.⁴,Whiting Paul¹,Vincent Jean-Paul³,Jones E. Yvonne²,Fish Paul V.¹³^ORCID

Affiliation:

1. Alzheimer’s Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.

2. Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.

3. The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.

4. Department of Cell and Developmental Biology, Laboratory for Molecular and Cellular Biology, University College London, London WC1E 6BT, U.K.

Funder

Medical Research Council

Wellcome Trust

Cancer Research UK

Alzheimer's Research UK

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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