Skip to main content
. 2019 Sep 25;10(10):1486–1491. doi: 10.1021/acsmedchemlett.9b00354

Table 1. Characterization of CSK Inhibitors 1–6a,b.

Cpd CSK IC50 (nM) LCK IC50 (nM) ZAP-70 EC50 (nM) (Ymax) HLM/MsLM %Rem.
1 5600 >50000 7900(73%) 2/33
2 79 24000 5700(180%) 65/15
3 80 31000 4050(350%) 68/9
4 70 43000 2000(350%) 53/78
5 430 34000 2700(280%) 72/1
6 8 26000 420(270%) 61/59
a

For assay conditions and replicate numbers, see the Supporting Information

b

HLM: Human liver microsomes. MsLM: Mouse liver microsomes.%Rem: Percent remaining at 10 min.