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. Author manuscript; available in PMC: 2014 Aug 16.
Published in final edited form as: J Med Chem. 2010 Aug 12;53(15):5439–5448. doi: 10.1021/jm901808w

Table 1.

In vitro potency profiling for 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one on Bcr-Abl

Anti-proliferative activity (IC50, nM) on Ba/F3 cell lines Enzymatic activity (IC50, nM)
Structure & Code Ba/F3 wtBcr-Abl G250E E255V T315I F317L M351T c-Abl G250E E255V T315I M351T
graphic file with name nihms576381t1.jpg
GNF-6		 1799 <5 294 <5 303 (243*) <5 <5 <5 N/A <5 1567 <5
graphic file with name nihms576381t2.jpg
GNF-8		 2690 <5 12 27 21 (151*) 6 <5 133 136 122 61 <5
graphic file with name nihms576381t3.jpg
GNF-7		 612 <5 <5 10 11 (40*) <5 <5 135 206 <5 130 <5
graphic file with name nihms576381t4.jpg
GNF-9		 630 3 3 30 43 3 3 <5 720 <5 <5 N/A
*

Inhibitory potency (IC50, nM) against cellular kinase autophosphorylation (Elisa)