Activity against kinases |
Molecule Id: EGIN0004339 |
S.No. |
Kinase |
Mutant |
IC50 |
Ki |
Kd |
Enz. inhib. (%) |
Inhib. Conc. |
Cellular IC50 |
Cell line |
Growth Factor |
1 | Lck | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 1 | 10 µM | - | - | - |
2 | YES1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 4 | 10 µM | - | - | - |
3 | EPH-B3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 5 | 10 µM | - | - | - |
4 | RIPK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 10 | 10 µM | - | - | - |
5 | MINK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 12 | 10 µM | - | - | - |
6 | Src | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 13 | 10 µM | - | - | - |
7 | PKD1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 14 | 10 µM | - | - | - |
8 | MNK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 21 | 10 µM | - | - | - |
9 | MELK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 25 | 10 µM | - | - | - |
10 | EPH-A2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 26 | 10 µM | - | - | - |
11 | PHK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 26 | 10 µM | - | - | - |
12 | CHK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 27 | 10 µM | - | - | - |
13 | CAMK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 30 | 10 µM | - | - | - |
14 | GCK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 30 | 10 µM | - | - | - |
15 | p38a | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 30 | 10 µM | - | - | - |
16 | FGF-R1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 31 | 10 µM | - | - | - |
17 | DYRK3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 32 | 10 µM | - | - | - |
18 | AuroraB | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 33 | 10 µM | - | - | - |
19 | BRSK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 36 | 10 µM | - | - | - |
20 | BTK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 36 | 10 µM | - | - | - |
21 | PRK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 36 | 10 µM | - | - | - |
22 | VEGFR | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 36 | 10 µM | - | - | - |
23 | NUAK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 37 | 10 µM | - | - | - |
24 | CK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 44 | 10 µM | - | - | - |
25 | MKK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 45 | 10 µM | - | - | - |
26 | BRSK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 46 | 10 µM | - | - | - |
27 | PIM1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 46 | 10 µM | - | - | - |
28 | SmMLCK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 48 | 10 µM | - | - | - |
29 | JNK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 49 | 10 µM | - | - | - |
30 | JNK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 50 | 10 µM | - | - | - |
31 | DYRK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 52 | 10 µM | - | - | - |
32 | SYK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 57 | 10 µM | - | - | - |
33 | PKBb | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 61 | 10 µM | - | - | - |
34 | IKKB | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 62 | 10 µM | - | - | - |
35 | JNK3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 62 | 10 µM | - | - | - |
36 | p38b | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 63 | 10 µM | - | - | - |
37 | MetNK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 64 | 10 µM | - | - | - |
38 | PIM3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 66 | 10 µM | - | - | - |
39 | PAK5 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 68 | 10 µM | - | - | - |
40 | IRAK4 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 70 | 10 µM | - | - | - |
41 | IGF-1R | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 71 | 10 µM | - | - | - |
42 | MAPKAP-K3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 72 | 10 µM | - | - | - |
43 | CSK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 73 | 10 µM | - | - | - |
44 | CAMKKb | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 74 | 10 µM | - | - | - |
45 | RSK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 74 | 10 µM | - | - | - |
46 | MARK4 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 75 | 10 µM | - | - | - |
47 | PIM2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 75 | 10 µM | - | - | - |
48 | SRPK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 75 | 10 µM | - | - | - |
49 | p38d | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 76 | 10 µM | - | - | - |
50 | MARK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 77 | 10 µM | - | - | - |
51 | PDK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 78 | 10 µM | - | - | - |
52 | IRR | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 79 | 10 µM | - | - | - |
53 | MLK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 79 | 10 µM | - | - | - |
54 | PAK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 79 | 10 µM | - | - | - |
55 | PAK4 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 79 | 10 µM | - | - | - |
56 | MST4 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 80 | 10 µM | - | - | - |
57 | MST2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 81 | 10 µM | - | - | - |
58 | PKCa | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 82 | 10 µM | - | - | - |
59 | SGK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 82 | 10 µM | - | - | - |
60 | CHK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 83 | 10 µM | - | - | - |
61 | ERK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 83 | 10 µM | - | - | - |
62 | PAK6 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 83 | 10 µM | - | - | - |
63 | AMPK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 84 | 10 µM | - | - | - |
64 | MLK3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 84 | 10 µM | - | - | - |
65 | PRAK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 84 | 10 µM | - | - | - |
66 | TBK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 84 | 10 µM | - | - | - |
67 | DYRK1A | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 85 | 10 µM | - | - | - |
68 | ERK8 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 85 | 10 µM | - | - | - |
69 | IR-HIS | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 85 | 10 µM | - | - | - |
70 | NEK6 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 85 | 10 µM | - | - | - |
71 | TTK | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 85 | 10 µM | - | - | - |
72 | MAPKAP-K2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 86 | 10 µM | - | - | - |
73 | PKA | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 86 | 10 µM | - | - | - |
74 | PKCz | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 86 | 10 µM | - | - | - |
75 | S6K1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 87 | 10 µM | - | - | - |
76 | AuroraA | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 88 | 10 µM | - | - | - |
77 | CDK2-CycA | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 88 | 10 µM | - | - | - |
78 | ERK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 88 | 10 µM | - | - | - |
79 | ROCK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 88 | 10 µM | - | - | - |
80 | GSK3b | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 89 | 10 µM | - | - | - |
81 | RSK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 89 | 10 µM | - | - | - |
82 | CK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 90 | 10 µM | - | - | - |
83 | IKKe | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 92 | 10 µM | - | - | - |
84 | LKB1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 94 | 10 µM | - | - | - |
85 | MARK3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 94 | 10 µM | - | - | - |
86 | p38g | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 94 | 10 µM | - | - | - |
87 | NEK2a | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 95 | 10 µM | - | - | - |
88 | HIPK3 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 96 | 10 µM | - | - | - |
89 | MSK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 96 | 10 µM | - | - | - |
90 | EF2K | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 99 | 10 µM | - | - | - |
91 | PKBa | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 100 | 10 µM | - | - | - |
92 | HIPK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 103 | 10 µM | - | - | - |
93 | HIPK2 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 104 | 10 µM | - | - | - |
94 | PLK1 | %ACTIVITY RELATIVE TO 100%DMSO | - | - | - | 109 | 10 µM | - | - | - |