A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

Author:

Cox Oakley B.12345,Krojer Tobias1234,Collins Patrick6784,Monteiro Octovia12345,Talon Romain1234,Bradley Anthony1234,Fedorov Oleg12345,Amin Jahangir91011124,Marsden Brian D.123413,Spencer John91011124ORCID,von Delft Frank12346,Brennan Paul E.12345ORCID

Affiliation:

1. Structural Genomics Consortium (SGC)

2. University of Oxford

3. Oxford OX3 7DQ

4. UK

5. Target Discovery Institute (TDI)

6. Diamond Light Source (DLS)

7. Harwell Science and Innovation Campus

8. Didcot

9. Department of Chemistry

10. School of Life Sciences

11. University of Sussex

12. Brighton

13. Kennedy Institute of Rheumatology

Abstract

High concentration crystal soaking of poised fragments and one-step elaboration identified compound 17 as an inhibitor of the PHIP(2) bromodomain.

Funder

Takeda Pharmaceutical Company

Novartis

Merck

Janssen Pharmaceuticals

European Commission

Bayer

Worldwide Cancer Research

Wellcome Trust

Engineering and Physical Sciences Research Council

AbbVie

Boehringer Ingelheim

Canada Foundation for Innovation

Genome Canada

Ontario Ministry of Economic Development and Innovation

Pfizer

Fundação de Amparo à Pesquisa do Estado de São Paulo

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

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