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. 2012 Jan 18;3(3):151–160. doi: 10.1021/cn200117j

Table 9. Pyrimidine Derivatives as LRRK2 Inhibitors.

graphic file with name cn-2011-00117j_0009.jpg

    IC50
        
no. name wild-type LRRK2 LRRK2-G2019S substrate selectivitya in vivo lit.
19 CZC-25146 4.76 nMb 6.87 nMb LRRKtide LRRKtide male CD-1 mice (71)
20 CZC-54252 1.28 nMb 1.85 nMb LRRKtide LRRKtide male CD-1 mice (71)
21 LRRK2-IN-1 13 nMc 6 nMc Nictide Nictide Male C57BL/6 mice (70)
a

Number of all kinases, including LRRK2.

b

Human LRRK2 (wt/G2019S).

c

GST-LRRK2 (1326–2527; wt/G2019S).