Table 1 In vitro and cellular potency of BBI-2779 and of reference compounds

From: Enhancing transcription–replication conflict targets ecDNA-positive cancers

 

BBI-2779

GDC-0575

SRA737

CHK1 biochemical potency (IC50), nM

0.3

12

85

CHK1/CHK2 selectivity

160×

1.5×

2,000×

CHK1 cellular potency AlphaLisa (IC50), nM

3

122

1,500

CTG proliferation ecDNA+ (IC50), nM

6

105

1,010

  1. AlphaLISA pCHK1-S345 activity was assessed in HT29 cells, while antiproliferation potency was evaluated in COLO320DM cells.
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