Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor

Author:

Mamai Ahmed1,Chau Anh M.1,Wilson Brian J.1,Watson Iain D.1,Joseph Babu B.1,Subramanian Pandiaraju R.1,Morshed Monzur M.1,Morin Justin A.1,Prakesch Michael A.1,Lu Tianbao2ORCID,Connolly Pete2,Kuntz Douglas A.3,Pomroy Neil C.3,Poda Gennady14,Nguyen Kong1,Marcellus Richard1,Strathdee Graig1,Theriault Brigitte1,Subramaniam Ratheesh1,Mohammed Mohammed1,Abibi Ayome1,Chan Manuel1,Winston Jeffrey1,Kiyota Taira1,Undzys Elijus1,Aman Ahmed14ORCID,Austin Nigel2,Du Jardin Marc2,Packman Kathryn2,Phillippar Ulrike5,Attar Riccardo2,Edwards James2,O’Meara Jeff1,Uehling David E.1,Al-awar Rima167,Privé Gilbert G.389,Isaac Methvin B.1ORCID

Affiliation:

1. Drug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, Suite 510, Toronto, OntarioM5G 0A3, Canada

2. Janssen Research & Development, LLC, 1400 McKean Road, Spring House, Pennsylvania19477, United States

3. Princess Margaret Cancer Centre, Toronto, OntarioM5G 2C1, Canada

4. Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, OntarioM5S 3M2, Canada

5. Janssen Research & Development, Turnhoutseweg 30, B-2340Beerse, Belgium

6. Department of Chemistry, University of Toronto, Toronto, OntarioM5S 3H6, Canada

7. Department of Pharmacology and Toxicology, University of Toronto, Toronto, OntarioM5S 1A8, Canada

8. Department of Medical Biophysics, University of Toronto, Toronto, OntarioM5G 1L7, Canada

9. Department of Biochemistry, University of Toronto, Toronto, OntarioM5S 1A8, Canada

Funder

Ministry of Research and Innovation

Ontario Institute for Cancer Research

Johnson and Johnson Research and Development team

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

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