SGC-NSP2hel-1 A chemical probe for CHIKV nsp2 helicase.

  • overview
  • selectivity profile
  • in vitro potency
  • cell based assay data
overview

SGC-UNC has developed a chemical probe for CHIKV nsp2 helicase (SGC-NSP2hel-1). The chemical probe SGC-NSP2hel-1 potently inhibits viral replication, nsP2hel ATPase activity, and dsRNA unwinding, while the (S)- enantiomer was >100-fold less active.

 

properties
selectivity profile

 

in vitro potency

 

cell based assay data

 

 

references
pk properties
co-crystal structures
synthetic schemes
materials and methods
Protein: TP53
PDB ID: 9FZB
Deposition Date: Friday 5th July 2024
Authors: Yuksel, B., Balourdas, D.I., Muenick, P., Knapp, S., Doetsch, V., Joerger, A.C.

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
  1. 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
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