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. 2015 Jan 13;6(3):254–259. doi: 10.1021/ml5003663

Table 2. 4-Methyl-3-pyridyl Moiety with π-Donating Groups at the 6-Position Improves Cell Potency.

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Cmpd R1 TNKS1 enz IC50 (μM) PARP1 enz IC50 (μM) Wnt cell IC50 (μM) LogD pH 7.4 Aq. Sol. pH 7.4 (μM)
3 H 0.003 2.77 0.024 2.1 11
4 F 0.002 3.74 0.032 3.4 <1
5 Cl 0.006 0.017 0.019 3.9 <1
6 NH2 0.017 0.206 0.004 2.9 <1
7 OCH3 0.006 0.035 0.004 2.8 <1
8 N(CH3)2 0.019   <0.003 >3.5 4