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Figure 1b
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3
Kinome assay analysis (2.5 μM LP-182)
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% InhibitionAvg.
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KinaseAssay[ATP] (μM)Point 1Point 2
% Inhibition
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PI4K2A (PI4K2 alpha)Activity Km app-61-63-62
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SPHK2Activity10-39-38-38
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CAMK4 (CaMKIV)Activity Km app-31-34-32
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MYLK2 (skMLCK)Activity Km app-16-22-19
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LRRK2 R1441CActivity Km app-18-20-19
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MAP4K2 (GCK)Activity Km app-21-16-19
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CDK6/cyclin D1Activity10-16-13-15
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PI4K2B (PI4K2 beta)Activity Km app-15-14-14
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SPHK1Activity Km app-15-9-12
15
LRRK2 FLActivity Km app-9-15-12
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CDK7/cyclin H/MNAT1Activity Km app-10-10-10
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LRRK2 G2019SActivity Km app1-20-9
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LRRK2 I2020TActivity Km app-9-5-7
19
ERBB2 (HER2)Activity Km app-3-9-6
20
PKN1 (PRK1)Activity Km app2-12-5
21
LRRK2Activity Km app-8-1-5
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CDK4/cyclin D3Activity10-3-5-4
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CDK4/cyclin D1Activity10-5-4-4
24
CAMK1 (CaMK1)Activity10-3-4-4
25
MAPK14 (p38 alpha) DirectActivity Km app0-7-3
26
KIT T670IActivity Km app4-10-3
27
CHEK1 (CHK1)Activity Km app2-6-2
28
RPS6KB1 (p70S6K)Activity Km app-3-1-2
29
NEK9Activity Km app-2-2-2
30
PAK6Activity Km app-1-3-2
31
RET V804EActivity Km app-2-1-2
32
PTK2 (FAK)Activity Km app-52-2
33
NUAK1 (ARK5)Activity Km app8-10-1
34
STK3 (MST2)Activity Km app0-2-1
35
ADRBK2 (GRK3)Activity Km app0-2-1
36
DYRK1BActivity Km app000
37
PEAK1Activity Km app5-60
38
TBK1Activity Km app-440
39
TNK1Activity Km app100
40
CDC42 BPB (MRCKB)Activity Km app3-20
41
ROCK1Activity Km app010
42
CSKActivity Km app-120
43
FGFR3Activity Km app010
44
DYRK4Activity Km app-231
45
ROCK2Activity Km app111
46
PDK1 DirectActivity Km app-241
47
LTK (TYK1)Activity Km app3-21
48
CSNK2A1 (CK2 alpha 1)Activity Km app021
49
PAK2 (PAK65)Activity Km app3-11
50
SRC N1Activity Km app211
51
LYN AActivity Km app301
52
SRPK2Activity Km app121
53
CHEK2 (CHK2)Activity Km app122
54
CAMK1G (CAMKI gamma)Activity Km app222
55
ERBB4 (HER4)Activity Km app312
56
MAPK9 (JNK2)Activity100212
57
ABL1 F317IActivity Km app132
58
PRKG1Activity Km app132
59
NIM1KActivity Km app412
60
CDK2/cyclin AActivity Km app312
61
CAMK1D (CaMKI delta)Activity Km app-262
62
FGFR3 V555MActivity Km app232
63
RPS6KB2 (p70S6Kb)Activity Km app6-12
64
EGFR (ErbB1)Activity Km app322
65
DYRK1AActivity Km app233
66
IGF1RActivity Km app243
67
EGFR (ErbB1) T790MActivity Km app413
68
PRKD1 (PKC mu)Activity Km app233
69
ADRBK1 (GRK2)Activity Km app333
70
PIM2Activity Km app323
71
EEF2KActivity Km app323
72
CDK5/p25Activity Km app333
73
CDC42 BPA (MRCKA)Activity Km app513
74
BLKActivity Km app423
75
DCAMKL2 (DCK2)Activity Km app7-13
76
SRPK1Activity Km app7-13
77
MAPKAPK3Activity Km app153
78
MAP3K9 (MLK1)Activity Km app523
79
PIP4K2AActivity10163
80
EGFR (ErbB1) C797SActivity Km app253
81
PLK1Activity Km app333
82
JAK2 JH1 JH2 V617FActivity Km app613
83
PTK6 (Brk)Activity Km app523
84
FGFR2Activity Km app333
85
FGFR2 N549HActivity Km app343
86
CDC42 BPG (MRCKG)Activity Km app433
87
SNF1LK2Activity Km app343
88
HIPK3 (YAK1)Activity Km app434
89
ITKActivity Km app254
90
JAK2Activity Km app524
91
ABL1 T315IActivity Km app444
92
CLK2Activity Km app444
93
PRKCG (PKC gamma)Activity Km app804
94
PAK7 (KIAA1264)Activity Km app534
95
LRRK2 G2019S FLActivity Km app11-34
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PDGFRA D842VActivity Km app354
97
FRK (PTK5)Activity Km app544
98
DCAMKL1 (DCLK1)Activity Km app274
99
CAMK2A (CaMKII alpha)Activity Km app634
100
JAK1Activity Km app724