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

Table 8. Anthracene and Phenanthrene Derivatives as LRRK2 Inhibitors.

graphic file with name cn-2011-00117j_0008.jpg

    IC50
       
no. name wild-type LRRK2 LRRK2-G2019S substrate substrate selectivitya in vivo lit.
15 SP600125 3100 nMb 5000 nMb MBPc 2   (58)
16 Damnacanthal 7810 nMb 9450 nMb MBPc 2   (58)
17 LDN-73794 3500 nMd   PLK-peptide 2   (68)
18 LDN-22684e 6900 nMf 6100 nMf PLK-peptide     (69)
a

Number of all kinases, including LRRK2.

b

GST-LRRK2 (wt/G2019S).

c

Myelin basic protein (MBP).

d

Purified from BAC-transgenic mouse brain.

e

Non-ATP competitive.

f

Human LRRK2 (970-2527; wt/G2019S).