Inhibitor |
PLX 4720 (Raf Kinase Inhibitor V)
Screening Results Tables
Screen Conc:
0.10µM
Kinase |
% Activity Remaining |
Standard Deviation |
AMPK
|
91
|
17
|
Aurora B
|
86
|
0
|
BRSK2
|
109
|
4
|
BTK
|
102
|
4
|
CAMK1
|
107
|
13
|
CAMKK beta
|
92
|
1
|
CDK2-Cyclin A
|
80
|
12
|
CHK1
|
87
|
6
|
CHK2
|
78
|
19
|
CK1 delta
|
92
|
0
|
CK2
|
88
|
25
|
CSK
|
95
|
18
|
DYRK1A
|
96
|
2
|
DYRK2
|
87
|
16
|
DYRK3
|
97
|
4
|
EF2K
|
97
|
6
|
EPH-A2
|
100
|
2
|
EPH-B3
|
105
|
18
|
ERK1
|
115
|
44
|
ERK2
|
81
|
17
|
ERK8
|
91
|
10
|
FGF-R1
|
101
|
0
|
GSK3 beta
|
95
|
3
|
HIPK2
|
92
|
8
|
IGF-1R
|
90
|
3
|
IKK beta
|
100
|
14
|
IKK epsilon
|
84
|
3
|
IR
|
99
|
0
|
IRR
|
88
|
10
|
JNK1
|
104
|
5
|
JNK2
|
90
|
9
|
Lck
|
77
|
7
|
MAPKAP-K2
|
102
|
12
|
MARK3
|
92
|
8
|
MELK
|
81
|
7
|
MKK1
|
116
|
28
|
MNK1
|
82
|
6
|
MNK2
|
77
|
5
|
MSK1
|
90
|
10
|
MST2
|
85
|
6
|
MST4
|
104
|
3
|
NEK2a
|
84
|
13
|
NEK6
|
94
|
2
|
p38 alpha MAPK
|
84
|
13
|
p38 beta MAPK
|
85
|
13
|
p38 delta MAPK
|
106
|
8
|
p38 gamma MAPK
|
95
|
8
|
PAK4
|
79
|
5
|
PAK5
|
119
|
8
|
PAK6
|
101
|
13
|
PDK1
|
96
|
1
|
PHK
|
97
|
22
|
PIM1
|
106
|
11
|
PIM2
|
115
|
13
|
PIM3
|
109
|
9
|
PKA
|
94
|
6
|
PKB alpha
|
92
|
13
|
PKB beta
|
100
|
10
|
PKC alpha
|
96
|
2
|
PKC zeta
|
102
|
6
|
PKD1
|
97
|
2
|
PLK1
|
94
|
0
|
PRAK
|
98
|
11
|
PRK2
|
93
|
5
|
ROCK 2
|
99
|
1
|
RSK1
|
105
|
0
|
RSK2
|
93
|
17
|
S6K1
|
93
|
13
|
SGK1
|
88
|
9
|
SmMLCK
|
93
|
1
|
Src
|
71
|
4
|
SRPK1
|
89
|
8
|
SYK
|
98
|
1
|
TBK1
|
94
|
9
|
VEGFR1
|
87
|
3
|
YES1
|
74
|
4
|
Screen Conc:
1.00µM
Kinase |
% Activity Remaining |
Standard Deviation |
AMPK
|
114
|
2
|
ASK1
|
100
|
7
|
Aurora A
|
84
|
0
|
Aurora B
|
71
|
8
|
BRSK1
|
97
|
3
|
BRSK2
|
107
|
10
|
BTK
|
116
|
12
|
CAMK1
|
84
|
2
|
CAMKK beta
|
98
|
7
|
CDK2-Cyclin A
|
110
|
4
|
CHK1
|
81
|
5
|
CHK2
|
115
|
14
|
CK1 delta
|
98
|
3
|
CK2
|
109
|
10
|
CLK2
|
84
|
14
|
CSK
|
59
|
2
|
DAPK1
|
98
|
3
|
DYRK1A
|
99
|
10
|
DYRK2
|
106
|
2
|
DYRK3
|
98
|
6
|
EF2K
|
122
|
11
|
EPH-A2
|
105
|
2
|
EPH-A4
|
113
|
5
|
EPH-B1
|
94
|
0
|
EPH-B2
|
114
|
0
|
EPH-B3
|
126
|
13
|
EPH-B4
|
125
|
1
|
ERK1
|
116
|
0
|
ERK2
|
112
|
6
|
ERK8
|
88
|
3
|
FGF-R1
|
80
|
14
|
GCK
|
94
|
8
|
GSK3 beta
|
97
|
12
|
HER4
|
96
|
0
|
HIPK1
|
109
|
1
|
HIPK2
|
95
|
3
|
HIPK3
|
104
|
4
|
IGF-1R
|
110
|
9
|
IKK beta
|
89
|
3
|
IKK epsilon
|
102
|
8
|
IR
|
116
|
0
|
IRAK4
|
107
|
1
|
IRR
|
95
|
11
|
JAK2
|
95
|
11
|
JNK1
|
106
|
3
|
JNK2
|
98
|
0
|
JNK3
|
75
|
7
|
Lck
|
58
|
8
|
LKB1
|
109
|
5
|
MAPKAP-K2
|
112
|
12
|
MAPKAP-K3
|
115
|
5
|
MARK1
|
97
|
0
|
MARK2
|
93
|
3
|
MARK3
|
93
|
15
|
MARK4
|
98
|
1
|
MEKK1
|
96
|
2
|
MELK
|
116
|
10
|
MINK1
|
105
|
13
|
MKK1
|
84
|
8
|
MKK2
|
79
|
2
|
MKK6
|
125
|
11
|
MLK1
|
88
|
10
|
MLK3
|
84
|
7
|
MNK1
|
107
|
7
|
MNK2
|
113
|
7
|
MSK1
|
111
|
3
|
MST2
|
76
|
13
|
MST4
|
109
|
1
|
NEK2a
|
98
|
8
|
NEK6
|
112
|
3
|
NUAK1
|
83
|
6
|
p38 alpha MAPK
|
83
|
2
|
p38 beta MAPK
|
88
|
3
|
p38 delta MAPK
|
92
|
9
|
p38 gamma MAPK
|
108
|
5
|
PAK2
|
83
|
5
|
PAK4
|
77
|
1
|
PAK5
|
108
|
2
|
PAK6
|
107
|
13
|
PDK1
|
94
|
0
|
PHK
|
111
|
3
|
PIM1
|
104
|
13
|
PIM2
|
102
|
1
|
PIM3
|
97
|
3
|
PKA
|
112
|
1
|
PKB alpha
|
105
|
3
|
PKB beta
|
82
|
14
|
PKC alpha
|
104
|
7
|
PKC zeta
|
101
|
2
|
PKD1
|
93
|
15
|
PLK1
|
126
|
4
|
PRAK
|
93
|
5
|
PRK2
|
99
|
2
|
RIPK2
|
21
|
7
|
ROCK 2
|
91
|
3
|
RSK1
|
92
|
2
|
RSK2
|
111
|
7
|
S6K1
|
93
|
1
|
SGK1
|
103
|
4
|
SmMLCK
|
90
|
4
|
Src
|
62
|
3
|
SRPK1
|
101
|
4
|
SYK
|
114
|
9
|
TAK1
|
96
|
11
|
TAO1
|
109
|
9
|
TBK1
|
102
|
3
|
TrkA
|
107
|
12
|
TTK
|
88
|
1
|
VEGFR1
|
49
|
4
|
YES1
|
43
|
2
|
Screen Conc:
10.00µM
Kinase |
% Activity Remaining |
Standard Deviation |
AMPK
|
56
|
4
|
ASK1
|
95
|
15
|
Aurora A
|
23
|
1
|
Aurora B
|
20
|
4
|
BRSK1
|
82
|
6
|
BRSK2
|
73
|
8
|
BTK
|
69
|
0
|
CAMK1
|
27
|
1
|
CAMKK beta
|
71
|
6
|
CDK2-Cyclin A
|
102
|
3
|
CHK1
|
28
|
0
|
CHK2
|
77
|
0
|
CK1 delta
|
96
|
4
|
CK2
|
77
|
3
|
CLK2
|
20
|
2
|
CSK
|
84
|
2
|
DAPK1
|
83
|
13
|
DYRK1A
|
77
|
6
|
DYRK2
|
81
|
4
|
DYRK3
|
68
|
1
|
EF2K
|
100
|
2
|
EPH-A2
|
97
|
2
|
EPH-A4
|
96
|
3
|
EPH-B1
|
85
|
3
|
EPH-B2
|
76
|
1
|
EPH-B3
|
83
|
12
|
EPH-B4
|
97
|
0
|
ERK1
|
103
|
7
|
ERK2
|
90
|
6
|
ERK8
|
42
|
3
|
FGF-R1
|
30
|
3
|
GCK
|
26
|
2
|
GSK3 beta
|
53
|
3
|
HER4
|
49
|
3
|
HIPK1
|
93
|
3
|
HIPK2
|
48
|
7
|
HIPK3
|
90
|
14
|
IGF-1R
|
80
|
3
|
IKK beta
|
71
|
3
|
IKK epsilon
|
81
|
10
|
IR
|
117
|
9
|
IRAK4
|
87
|
4
|
IRR
|
64
|
6
|
JAK2
|
45
|
1
|
JNK1
|
89
|
1
|
JNK2
|
88
|
6
|
JNK3
|
85
|
4
|
Lck
|
34
|
6
|
LKB1
|
64
|
4
|
MAPKAP-K2
|
100
|
7
|
MAPKAP-K3
|
89
|
2
|
MARK1
|
70
|
0
|
MARK2
|
87
|
2
|
MARK3
|
74
|
0
|
MARK4
|
65
|
3
|
MEKK1
|
65
|
3
|
MELK
|
24
|
0
|
MINK1
|
15
|
0
|
MKK1
|
45
|
1
|
MKK2
|
25
|
3
|
MKK6
|
94
|
10
|
MLK1
|
34
|
4
|
MLK3
|
33
|
3
|
MNK1
|
79
|
13
|
MNK2
|
98
|
10
|
MSK1
|
91
|
3
|
MST2
|
40
|
1
|
MST4
|
66
|
4
|
NEK2a
|
52
|
0
|
NEK6
|
114
|
13
|
NUAK1
|
61
|
7
|
p38 alpha MAPK
|
58
|
6
|
p38 beta MAPK
|
57
|
2
|
p38 delta MAPK
|
79
|
6
|
p38 gamma MAPK
|
94
|
2
|
PAK2
|
40
|
8
|
PAK4
|
46
|
1
|
PAK5
|
49
|
4
|
PAK6
|
79
|
2
|
PDK1
|
85
|
12
|
PHK
|
110
|
1
|
PIM1
|
68
|
5
|
PIM2
|
92
|
3
|
PIM3
|
61
|
3
|
PKA
|
104
|
1
|
PKB alpha
|
101
|
6
|
PKB beta
|
78
|
15
|
PKC alpha
|
84
|
4
|
PKC zeta
|
93
|
7
|
PKD1
|
87
|
13
|
PLK1
|
95
|
1
|
PRAK
|
93
|
2
|
PRK2
|
89
|
12
|
RIPK2
|
7
|
1
|
ROCK 2
|
66
|
1
|
RSK1
|
98
|
4
|
RSK2
|
80
|
3
|
S6K1
|
84
|
1
|
SGK1
|
88
|
11
|
SmMLCK
|
36
|
1
|
Src
|
21
|
0
|
SRPK1
|
79
|
3
|
SYK
|
96
|
14
|
TAK1
|
92
|
9
|
TAO1
|
63
|
3
|
TBK1
|
96
|
7
|
TrkA
|
54
|
4
|
TTK
|
75
|
11
|
VEGFR1
|
10
|
0
|
YES1
|
13
|
3
|