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OICR-40155 A chemical handle for DCAF1.

overview
references
co-crystal structures

overview

A collaboration between the Drug Discovery Program at the Ontario Institute for Cancer Research (OICR) and the Structural Genomics Consortium (SGC) has resulted in the discovery of OICR-40155, a handle for DCAF1 (DDB1-Cul4 associated factor 1).

The enantiomer is a suitable negative control for the handle. The supporting information may be obtained from the probe OICR-41103 , and OICR41114 in Reference 1 (Mabanglo et al.).

properties

selectivity profile

in vitro potency

cell based assay data

references

Mark F Mabanglo et al., Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity. https://pubmed.ncbi.nlm.nih.gov/39580491/

pk properties

co-crystal structures

https://www.rcsb.org/structure/9BHR

synthetic schemes

materials and methods