Inhibitor |
BML-258 (SK1-I)
Screening Results Tables
Screen Conc:
0.10µM
Kinase |
% Activity Remaining |
Standard Deviation |
ABL
|
110
|
3
|
AMPK
|
104
|
9
|
ASK1
|
115
|
8
|
Aurora A
|
116
|
3
|
Aurora B
|
100
|
2
|
BRK
|
104
|
4
|
BRSK1
|
114
|
4
|
BRSK2
|
130
|
7
|
BTK
|
107
|
25
|
CAMK1
|
106
|
13
|
CAMKK beta
|
97
|
4
|
CDK2-Cyclin A
|
98
|
4
|
CHK1
|
96
|
1
|
CHK2
|
92
|
3
|
CK1 delta
|
88
|
9
|
CK2
|
78
|
12
|
CLK2
|
106
|
4
|
CSK
|
104
|
1
|
DAPK1
|
109
|
7
|
DYRK1A
|
83
|
4
|
DYRK2
|
116
|
3
|
DYRK3
|
93
|
6
|
EF2K
|
93
|
13
|
EPH-A2
|
103
|
8
|
EPH-A4
|
100
|
4
|
EPH-B1
|
126
|
14
|
EPH-B2
|
115
|
5
|
EPH-B3
|
104
|
0
|
EPH-B4
|
122
|
7
|
ERK1
|
108
|
23
|
ERK2
|
98
|
2
|
ERK8
|
82
|
1
|
FGF-R1
|
115
|
6
|
GCK
|
86
|
2
|
GSK3 beta
|
83
|
8
|
HER4
|
127
|
6
|
HIPK1
|
92
|
6
|
HIPK2
|
108
|
8
|
HIPK3
|
118
|
13
|
IGF-1R
|
87
|
12
|
IKK beta
|
91
|
1
|
IKK epsilon
|
106
|
3
|
IR
|
107
|
7
|
IRAK4
|
72
|
6
|
IRR
|
99
|
6
|
JAK2
|
118
|
14
|
JNK1
|
98
|
6
|
JNK2
|
85
|
6
|
JNK3
|
93
|
6
|
Lck
|
106
|
11
|
LKB1
|
93
|
5
|
MAPKAP-K2
|
98
|
12
|
MAPKAP-K3
|
115
|
13
|
MARK1
|
114
|
12
|
MARK2
|
89
|
5
|
MARK3
|
101
|
7
|
MARK4
|
90
|
11
|
MEKK1
|
93
|
8
|
MELK
|
108
|
2
|
MINK1
|
107
|
14
|
MKK1
|
97
|
16
|
MKK2
|
104
|
10
|
MKK6
|
102
|
5
|
MLK1
|
105
|
6
|
MLK3
|
102
|
8
|
MNK1
|
101
|
3
|
MNK2
|
111
|
3
|
MPSK1
|
104
|
2
|
MSK1
|
110
|
6
|
MST2
|
96
|
2
|
MST4
|
116
|
7
|
NEK2a
|
110
|
3
|
NEK6
|
92
|
4
|
NUAK1
|
105
|
2
|
p38 alpha MAPK
|
95
|
8
|
p38 beta MAPK
|
99
|
9
|
p38 delta MAPK
|
90
|
9
|
p38 gamma MAPK
|
93
|
4
|
PAK2
|
113
|
2
|
PAK4
|
91
|
4
|
PAK5
|
104
|
3
|
PAK6
|
105
|
11
|
PDK1
|
107
|
4
|
PHK
|
99
|
5
|
PIM1
|
100
|
0
|
PIM2
|
103
|
6
|
PIM3
|
118
|
4
|
PKA
|
110
|
2
|
PKB alpha
|
99
|
5
|
PKB beta
|
85
|
2
|
PKC alpha
|
96
|
0
|
PKC gamma
|
101
|
6
|
PKC zeta
|
106
|
2
|
PKD1
|
107
|
4
|
PLK1
|
106
|
1
|
PRAK
|
89
|
2
|
PRK2
|
78
|
4
|
RIPK2
|
119
|
8
|
ROCK 2
|
110
|
1
|
RSK1
|
95
|
1
|
RSK2
|
87
|
3
|
S6K1
|
114
|
8
|
SGK1
|
83
|
5
|
SmMLCK
|
90
|
2
|
Src
|
105
|
11
|
SRPK1
|
92
|
4
|
STK33
|
100
|
0
|
SYK
|
134
|
4
|
TAK1
|
100
|
7
|
TAO1
|
102
|
11
|
TBK1
|
111
|
13
|
TIE2
|
141
|
5
|
TrkA
|
103
|
1
|
TTK
|
95
|
4
|
VEGFR1
|
95
|
2
|
YES1
|
123
|
1
|
ZAP70
|
116
|
2
|
Screen Conc:
1.00µM
Kinase |
% Activity Remaining |
Standard Deviation |
ABL
|
106
|
11
|
AMPK
|
96
|
0
|
ASK1
|
99
|
3
|
Aurora A
|
105
|
4
|
Aurora B
|
102
|
4
|
BRK
|
93
|
8
|
BRSK1
|
111
|
0
|
BRSK2
|
108
|
1
|
BTK
|
103
|
5
|
CAMK1
|
101
|
11
|
CAMKK beta
|
81
|
15
|
CDK2-Cyclin A
|
79
|
7
|
CHK1
|
92
|
7
|
CHK2
|
84
|
4
|
CK1 delta
|
87
|
7
|
CK2
|
87
|
12
|
CLK2
|
104
|
12
|
CSK
|
101
|
15
|
DAPK1
|
101
|
11
|
DYRK1A
|
91
|
6
|
DYRK2
|
124
|
3
|
DYRK3
|
98
|
1
|
EF2K
|
76
|
0
|
EPH-A2
|
91
|
9
|
EPH-A4
|
101
|
8
|
EPH-B1
|
108
|
7
|
EPH-B2
|
105
|
10
|
EPH-B3
|
100
|
9
|
EPH-B4
|
101
|
8
|
ERK1
|
97
|
9
|
ERK2
|
90
|
9
|
ERK8
|
86
|
1
|
FGF-R1
|
111
|
12
|
GCK
|
72
|
2
|
GSK3 beta
|
88
|
3
|
HER4
|
107
|
20
|
HIPK1
|
112
|
6
|
HIPK2
|
106
|
6
|
HIPK3
|
112
|
2
|
IGF-1R
|
86
|
2
|
IKK beta
|
97
|
7
|
IKK epsilon
|
95
|
6
|
IR
|
103
|
20
|
IRAK4
|
66
|
0
|
IRR
|
94
|
3
|
JAK2
|
98
|
3
|
JNK1
|
94
|
3
|
JNK2
|
90
|
2
|
JNK3
|
103
|
7
|
Lck
|
92
|
8
|
LKB1
|
89
|
0
|
MAPKAP-K2
|
95
|
6
|
MAPKAP-K3
|
119
|
1
|
MARK1
|
112
|
17
|
MARK2
|
97
|
9
|
MARK3
|
107
|
7
|
MARK4
|
89
|
8
|
MEKK1
|
99
|
4
|
MELK
|
99
|
7
|
MINK1
|
93
|
11
|
MKK1
|
102
|
5
|
MKK2
|
103
|
12
|
MKK6
|
98
|
4
|
MLK1
|
108
|
6
|
MLK3
|
106
|
4
|
MNK1
|
92
|
16
|
MNK2
|
98
|
3
|
MPSK1
|
98
|
8
|
MSK1
|
104
|
18
|
MST2
|
90
|
0
|
MST4
|
96
|
9
|
NEK2a
|
103
|
2
|
NEK6
|
86
|
12
|
NUAK1
|
108
|
6
|
p38 alpha MAPK
|
87
|
13
|
p38 beta MAPK
|
106
|
2
|
p38 delta MAPK
|
99
|
5
|
p38 gamma MAPK
|
80
|
11
|
PAK2
|
103
|
1
|
PAK4
|
91
|
9
|
PAK5
|
100
|
8
|
PAK6
|
108
|
7
|
PDK1
|
106
|
2
|
PHK
|
86
|
0
|
PIM1
|
95
|
11
|
PIM2
|
109
|
3
|
PIM3
|
121
|
6
|
PKA
|
106
|
2
|
PKB alpha
|
97
|
8
|
PKB beta
|
90
|
13
|
PKC alpha
|
88
|
5
|
PKC gamma
|
109
|
8
|
PKC zeta
|
108
|
3
|
PKD1
|
112
|
4
|
PLK1
|
94
|
7
|
PRAK
|
99
|
12
|
PRK2
|
70
|
1
|
RIPK2
|
95
|
3
|
ROCK 2
|
94
|
5
|
RSK1
|
98
|
4
|
RSK2
|
95
|
1
|
S6K1
|
108
|
6
|
SGK1
|
87
|
3
|
SmMLCK
|
95
|
12
|
Src
|
100
|
3
|
SRPK1
|
89
|
3
|
STK33
|
100
|
11
|
SYK
|
105
|
6
|
TAK1
|
108
|
4
|
TAO1
|
108
|
9
|
TBK1
|
82
|
39
|
TIE2
|
118
|
3
|
TrkA
|
110
|
9
|
TTK
|
91
|
4
|
VEGFR1
|
81
|
5
|
YES1
|
100
|
9
|
ZAP70
|
106
|
10
|
Screen Conc:
10.00µM
Kinase |
% Activity Remaining |
Standard Deviation |
ABL
|
109
|
10
|
AMPK
|
94
|
6
|
ASK1
|
94
|
0
|
Aurora A
|
92
|
15
|
Aurora B
|
93
|
0
|
BRK
|
104
|
2
|
BRSK1
|
97
|
1
|
BRSK2
|
108
|
7
|
BTK
|
103
|
15
|
CAMK1
|
89
|
5
|
CAMKK beta
|
90
|
2
|
CDK2-Cyclin A
|
88
|
3
|
CHK1
|
86
|
9
|
CHK2
|
82
|
8
|
CK1 delta
|
81
|
4
|
CK2
|
83
|
2
|
CLK2
|
97
|
11
|
CSK
|
98
|
5
|
DAPK1
|
103
|
18
|
DYRK1A
|
84
|
6
|
DYRK2
|
119
|
7
|
DYRK3
|
93
|
9
|
EF2K
|
69
|
1
|
EPH-A2
|
91
|
6
|
EPH-A4
|
96
|
7
|
EPH-B1
|
115
|
18
|
EPH-B2
|
108
|
5
|
EPH-B3
|
86
|
0
|
EPH-B4
|
123
|
13
|
ERK1
|
85
|
4
|
ERK2
|
100
|
5
|
ERK8
|
77
|
0
|
FGF-R1
|
104
|
1
|
GCK
|
71
|
9
|
GSK3 beta
|
71
|
2
|
HER4
|
105
|
6
|
HIPK1
|
94
|
18
|
HIPK2
|
106
|
5
|
HIPK3
|
102
|
3
|
IGF-1R
|
93
|
14
|
IKK beta
|
100
|
6
|
IKK epsilon
|
86
|
4
|
IR
|
99
|
2
|
IRAK4
|
67
|
1
|
IRR
|
100
|
5
|
JAK2
|
100
|
10
|
JNK1
|
90
|
21
|
JNK2
|
88
|
5
|
JNK3
|
98
|
8
|
Lck
|
84
|
11
|
LKB1
|
98
|
4
|
MAPKAP-K2
|
91
|
4
|
MAPKAP-K3
|
123
|
7
|
MARK1
|
104
|
6
|
MARK2
|
83
|
6
|
MARK3
|
105
|
0
|
MARK4
|
93
|
10
|
MEKK1
|
89
|
0
|
MELK
|
98
|
14
|
MINK1
|
111
|
13
|
MKK1
|
97
|
9
|
MKK2
|
109
|
19
|
MKK6
|
99
|
1
|
MLK1
|
100
|
3
|
MLK3
|
109
|
12
|
MNK1
|
93
|
1
|
MNK2
|
102
|
14
|
MPSK1
|
100
|
4
|
MSK1
|
95
|
1
|
MST2
|
94
|
7
|
MST4
|
108
|
13
|
NEK2a
|
108
|
7
|
NEK6
|
84
|
9
|
NUAK1
|
101
|
5
|
p38 alpha MAPK
|
80
|
9
|
p38 beta MAPK
|
95
|
2
|
p38 delta MAPK
|
90
|
1
|
p38 gamma MAPK
|
87
|
5
|
PAK2
|
113
|
8
|
PAK4
|
85
|
5
|
PAK5
|
101
|
4
|
PAK6
|
103
|
5
|
PDK1
|
122
|
9
|
PHK
|
76
|
0
|
PIM1
|
95
|
10
|
PIM2
|
97
|
2
|
PIM3
|
107
|
2
|
PKA
|
107
|
12
|
PKB alpha
|
107
|
24
|
PKB beta
|
86
|
2
|
PKC alpha
|
89
|
5
|
PKC gamma
|
96
|
1
|
PKC zeta
|
92
|
5
|
PKD1
|
115
|
15
|
PLK1
|
96
|
3
|
PRAK
|
90
|
3
|
PRK2
|
58
|
1
|
RIPK2
|
100
|
4
|
ROCK 2
|
116
|
3
|
RSK1
|
81
|
8
|
RSK2
|
81
|
11
|
S6K1
|
100
|
0
|
SGK1
|
78
|
4
|
SmMLCK
|
91
|
15
|
Src
|
111
|
13
|
SRPK1
|
83
|
9
|
STK33
|
89
|
16
|
SYK
|
92
|
13
|
TAK1
|
111
|
2
|
TAO1
|
91
|
6
|
TBK1
|
93
|
1
|
TIE2
|
113
|
4
|
TrkA
|
86
|
0
|
TTK
|
86
|
4
|
VEGFR1
|
83
|
4
|
YES1
|
109
|
2
|
ZAP70
|
92
|
0
|