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Probe stories

Chemical Probe Stories

Open access chemical probes have an impact on preclinical research!​

OICR-9429 led to a preclinical candidate for treating leukemia. ​

2006: WDR5 apo structure deposited​

2011-2014: Library screen, scaffold optimization, first-in-class WDR5 antagonist discovered and put in the public domain​

SGC

2019: Celgene purchased rights to a preclinical candidate

The chemical probe inspires further research.

The chemical series SGC-SMARCA-BRDVIII was initially discovered by Genentech/Constellation and then developed and characterized further by the chemical probe platform at the SGC Frankfurt.

SMARCA2/4 BRD inhibitors lack efficacy killing SMARCA4-mutated cancers as suggested by genetic KO studies. When combined with an E3 ligase VHL ligand SMARCA2/4 inhibitors serve as potent PROTAC degraders such as ACBI-1, developed by Boehringer Ingelheim and the University of Dundee which phenocopied the RNAi results. Ref: U.S. Patent WO 2016138114 A1 ​