Inhibitor |
VPS34-IN2 (PIK-III)
Screening Results Tables
Screen Conc:
0.10µM
Kinase |
% Activity Remaining |
Standard Deviation |
ABL
|
95
|
8
|
AMPK (hum)
|
98
|
21
|
ASK1
|
100
|
9
|
Aurora A
|
96
|
11
|
Aurora B
|
65
|
8
|
BRK
|
84
|
3
|
BRSK1
|
91
|
0
|
BRSK2
|
105
|
4
|
BTK
|
104
|
2
|
CAMK1
|
103
|
3
|
CAMKK beta
|
100
|
3
|
CDK2-Cyclin A
|
78
|
9
|
CDK9-Cyclin T1
|
92
|
1
|
CHK1
|
98
|
9
|
CHK2
|
92
|
0
|
CK1 delta
|
92
|
1
|
CK1 gamma 2
|
105
|
21
|
CK2
|
97
|
5
|
CLK2
|
83
|
4
|
CSK
|
109
|
16
|
DAPK1
|
94
|
1
|
DDR2
|
85
|
20
|
DYRK1A
|
90
|
2
|
DYRK2
|
115
|
13
|
DYRK3
|
96
|
1
|
EF2K
|
103
|
9
|
EIF2AK3
|
110
|
5
|
EPH-A2
|
103
|
0
|
EPH-A4
|
100
|
2
|
EPH-B1
|
97
|
4
|
EPH-B2
|
100
|
14
|
EPH-B3
|
93
|
2
|
EPH-B4
|
99
|
9
|
ERK1
|
82
|
5
|
ERK2
|
91
|
1
|
ERK5
|
95
|
11
|
ERK8
|
53
|
2
|
FGF-R1
|
94
|
13
|
GCK
|
78
|
13
|
GSK3 beta
|
87
|
3
|
HER4
|
105
|
2
|
HIPK1
|
81
|
6
|
HIPK2
|
82
|
6
|
HIPK3
|
87
|
0
|
IGF-1R
|
76
|
3
|
IKK beta
|
93
|
4
|
IKK epsilon
|
83
|
5
|
IR
|
87
|
19
|
IRAK1
|
93
|
3
|
IRAK4
|
96
|
6
|
IRR
|
96
|
0
|
JAK2
|
73
|
2
|
JNK1
|
87
|
6
|
JNK2
|
82
|
6
|
JNK3
|
102
|
11
|
Lck
|
87
|
5
|
LKB1
|
92
|
1
|
MAP4K3
|
87
|
15
|
MAP4K5
|
87
|
10
|
MAPKAP-K2
|
96
|
2
|
MAPKAP-K3
|
94
|
1
|
MARK1
|
79
|
5
|
MARK2
|
93
|
10
|
MARK3
|
81
|
5
|
MARK4
|
95
|
5
|
MEKK1
|
83
|
2
|
MELK
|
88
|
3
|
MINK1
|
70
|
0
|
MKK1
|
83
|
0
|
MKK2
|
81
|
7
|
MKK6
|
86
|
11
|
MLK1
|
101
|
10
|
MLK3
|
78
|
4
|
MNK1
|
84
|
6
|
MNK2
|
95
|
6
|
MPSK1
|
105
|
8
|
MSK1
|
95
|
3
|
MST2
|
85
|
13
|
MST3
|
88
|
22
|
MST4
|
82
|
5
|
NEK2a
|
99
|
1
|
NEK6
|
95
|
1
|
NUAK1
|
90
|
3
|
OSR1
|
91
|
2
|
p38 alpha MAPK
|
101
|
3
|
p38 beta MAPK
|
88
|
9
|
p38 delta MAPK
|
89
|
2
|
p38 gamma MAPK
|
79
|
2
|
PAK2
|
96
|
4
|
PAK4
|
113
|
2
|
PAK5
|
84
|
3
|
PAK6
|
101
|
8
|
PDGFRA
|
89
|
6
|
PDK1
|
88
|
11
|
PHK
|
100
|
8
|
PIM1
|
90
|
8
|
PIM2
|
89
|
7
|
PIM3
|
93
|
3
|
PINK
|
92
|
5
|
PKA
|
94
|
6
|
PKB alpha
|
83
|
9
|
PKB beta
|
90
|
9
|
PKC alpha
|
86
|
5
|
PKC gamma
|
100
|
4
|
PKC zeta
|
101
|
4
|
PKD1
|
94
|
10
|
PLK1
|
86
|
13
|
PRAK
|
92
|
6
|
PRK2
|
81
|
1
|
RIPK2
|
85
|
3
|
ROCK 2
|
75
|
3
|
RSK1
|
86
|
11
|
RSK2
|
83
|
6
|
S6K1
|
82
|
6
|
SGK1
|
83
|
14
|
SIK2
|
85
|
1
|
SIK3
|
90
|
1
|
SmMLCK
|
95
|
2
|
Src
|
88
|
10
|
SRPK1
|
85
|
3
|
STK33
|
88
|
14
|
SYK
|
96
|
4
|
TAK1
|
77
|
7
|
TAO1
|
79
|
12
|
TBK1
|
93
|
8
|
TESK1
|
106
|
24
|
TGFBR1
|
82
|
13
|
TIE2
|
77
|
1
|
TLK1
|
93
|
10
|
TrkA
|
85
|
5
|
TSSK1
|
110
|
12
|
TTBK1
|
95
|
10
|
TTBK2
|
83
|
11
|
TTK
|
88
|
6
|
ULK1
|
83
|
3
|
ULK2
|
100
|
10
|
VEGFR1
|
97
|
7
|
WNK1
|
92
|
7
|
YES1
|
93
|
2
|
ZAP70
|
96
|
3
|
Screen Conc:
1.00µM
Kinase |
% Activity Remaining |
Standard Deviation |
ABL
|
92
|
5
|
AMPK (hum)
|
82
|
8
|
ASK1
|
102
|
3
|
Aurora A
|
91
|
24
|
Aurora B
|
39
|
8
|
BRK
|
51
|
5
|
BRSK1
|
76
|
1
|
BRSK2
|
102
|
4
|
BTK
|
84
|
2
|
CAMK1
|
87
|
7
|
CAMKK beta
|
94
|
8
|
CDK2-Cyclin A
|
52
|
2
|
CDK9-Cyclin T1
|
76
|
1
|
CHK1
|
90
|
12
|
CHK2
|
94
|
6
|
CK1 delta
|
63
|
5
|
CK1 gamma 2
|
93
|
4
|
CK2
|
92
|
5
|
CLK2
|
67
|
11
|
CSK
|
136
|
39
|
DAPK1
|
85
|
5
|
DDR2
|
91
|
18
|
DYRK1A
|
85
|
0
|
DYRK2
|
96
|
18
|
DYRK3
|
88
|
7
|
EF2K
|
89
|
6
|
EIF2AK3
|
84
|
2
|
EPH-A2
|
92
|
1
|
EPH-A4
|
92
|
3
|
EPH-B1
|
90
|
7
|
EPH-B2
|
81
|
16
|
EPH-B3
|
97
|
8
|
EPH-B4
|
104
|
3
|
ERK1
|
91
|
7
|
ERK2
|
72
|
6
|
ERK5
|
70
|
1
|
ERK8
|
15
|
1
|
FGF-R1
|
85
|
5
|
GCK
|
73
|
1
|
GSK3 beta
|
67
|
9
|
HER4
|
86
|
14
|
HIPK1
|
74
|
1
|
HIPK2
|
78
|
4
|
HIPK3
|
87
|
4
|
IGF-1R
|
76
|
5
|
IKK beta
|
82
|
4
|
IKK epsilon
|
82
|
2
|
IR
|
79
|
12
|
IRAK1
|
88
|
3
|
IRAK4
|
68
|
9
|
IRR
|
90
|
7
|
JAK2
|
30
|
1
|
JNK1
|
77
|
13
|
JNK2
|
74
|
8
|
JNK3
|
92
|
7
|
Lck
|
83
|
0
|
LKB1
|
85
|
6
|
MAP4K3
|
78
|
7
|
MAP4K5
|
74
|
6
|
MAPKAP-K2
|
99
|
5
|
MAPKAP-K3
|
95
|
7
|
MARK1
|
64
|
3
|
MARK2
|
90
|
15
|
MARK3
|
70
|
8
|
MARK4
|
87
|
0
|
MEKK1
|
91
|
5
|
MELK
|
76
|
2
|
MINK1
|
64
|
8
|
MKK1
|
86
|
3
|
MKK2
|
80
|
3
|
MKK6
|
88
|
23
|
MLK1
|
81
|
13
|
MLK3
|
52
|
9
|
MNK1
|
76
|
10
|
MNK2
|
92
|
4
|
MPSK1
|
84
|
1
|
MSK1
|
86
|
1
|
MST2
|
69
|
4
|
MST3
|
78
|
4
|
MST4
|
74
|
1
|
NEK2a
|
99
|
4
|
NEK6
|
84
|
3
|
NUAK1
|
68
|
6
|
OSR1
|
90
|
1
|
p38 alpha MAPK
|
92
|
1
|
p38 beta MAPK
|
87
|
12
|
p38 delta MAPK
|
83
|
0
|
p38 gamma MAPK
|
76
|
1
|
PAK2
|
85
|
1
|
PAK4
|
75
|
9
|
PAK5
|
83
|
7
|
PAK6
|
93
|
7
|
PDGFRA
|
97
|
2
|
PDK1
|
90
|
3
|
PHK
|
101
|
7
|
PIM1
|
90
|
1
|
PIM2
|
94
|
6
|
PIM3
|
91
|
13
|
PINK
|
85
|
4
|
PKA
|
94
|
7
|
PKB alpha
|
83
|
11
|
PKB beta
|
96
|
5
|
PKC alpha
|
91
|
10
|
PKC gamma
|
94
|
11
|
PKC zeta
|
112
|
8
|
PKD1
|
89
|
10
|
PLK1
|
87
|
8
|
PRAK
|
87
|
2
|
PRK2
|
72
|
1
|
RIPK2
|
58
|
6
|
ROCK 2
|
78
|
7
|
RSK1
|
91
|
4
|
RSK2
|
75
|
9
|
S6K1
|
78
|
3
|
SGK1
|
94
|
1
|
SIK2
|
67
|
4
|
SIK3
|
79
|
4
|
SmMLCK
|
84
|
1
|
Src
|
87
|
10
|
SRPK1
|
81
|
5
|
STK33
|
89
|
6
|
SYK
|
92
|
4
|
TAK1
|
47
|
7
|
TAO1
|
48
|
6
|
TBK1
|
91
|
2
|
TESK1
|
81
|
6
|
TGFBR1
|
79
|
3
|
TIE2
|
72
|
14
|
TLK1
|
83
|
8
|
TrkA
|
92
|
24
|
TSSK1
|
81
|
3
|
TTBK1
|
81
|
7
|
TTBK2
|
87
|
13
|
TTK
|
84
|
1
|
ULK1
|
81
|
10
|
ULK2
|
98
|
10
|
VEGFR1
|
70
|
1
|
WNK1
|
96
|
7
|
YES1
|
80
|
11
|
ZAP70
|
93
|
5
|