| Compound name | Brutto | MW | CAS | PubChem CID | Action | Reference | Reference |
|---|---|---|---|---|---|---|---|
| BX-517 Analog (compound 7b) | C19H15N5O2 | 345.35 | 11588244 | PDK1 | Islam I. (2007) Bioorganic and Medicinal Chemistry Letters 17 3819-3825 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK |
5
|
0 |
| BRSK2 | 13 | 3 |
| BTK | 86 | 11 |
| CAMK1 | 112 | 12 |
| CAMKK beta | 67 | 7 |
| CDK2-Cyclin A | 63 | 0 |
| CHK1 | 85 | 2 |
| CHK2 |
-1
|
0 |
| CK1 delta | 90 | 0 |
| CK2 | 93 | 17 |
| CSK | 98 | 0 |
| DYRK1A | 42 | 9 |
| DYRK2 | 19 | 3 |
| DYRK3 | 19 | 3 |
| EF2K | 102 | 14 |
| EPH-A2 | 93 | 0 |
| EPH-B3 | 107 | 1 |
| ERK1 | 71 | 7 |
| ERK2 | 81 | 10 |
| ERK8 |
5
|
0 |
| FGF-R1 | 17 | 3 |
| GSK3 beta | 11 | 1 |
| HIPK2 | 33 | 1 |
| IGF-1R | 49 | 49 |
| IKK beta | 75 | 1 |
| IKK epsilon | 51 | 14 |
| IR | 112 | 14 |
| IRR | 35 | 0 |
| JNK1 | 124 | 1 |
| JNK2 | 214 | 172 |
| Lck | 44 | 4 |
| MAPKAP-K2 | 86 | 3 |
| MARK3 | 16 | 3 |
| MELK | 16 | 0 |
| MKK1 |
8
|
1 |
| MNK1 | 80 | 0 |
| MNK2 | 75 | 12 |
| MSK1 | 98 | 1 |
| MST2 |
8
|
0 |
| MST4 | 55 | 32 |
| NEK2a | 100 | 10 |
| NEK6 | 92 | 6 |
| p38 alpha MAPK | 81 | 8 |
| p38 beta MAPK | 103 | 0 |
| p38 delta MAPK | 85 | 9 |
| p38 gamma MAPK | 93 | 6 |
| PAK4 | 64 | 5 |
| PAK5 | 75 | 10 |
| PAK6 | 86 | 1 |
| PDK1 | 20 | 1 |
| PHK | 13 | 0 |
| PIM1 | 43 | 2 |
| PIM2 | 76 | 6 |
| PIM3 | 30 | 0 |
| PKA | 78 | 0 |
| PKB alpha | 85 | 4 |
| PKB beta | 88 | 3 |
| PKC alpha | 106 | 3 |
| PKC zeta | 85 | 4 |
| PKD1 | 30 | 2 |
| PLK1 | 86 | 5 |
| PRAK | 95 | 6 |
| PRK2 | 25 | 11 |
| ROCK 2 | 103 | 25 |
| RSK1 | 24 | 4 |
| RSK2 | 38 | 4 |
| S6K1 | 76 | 0 |
| SGK1 | 77 | 5 |
| SmMLCK | 54 | 7 |
| Src | 41 | 2 |
| SRPK1 | 90 | 4 |
| SYK | 95 | 23 |
| TBK1 | 27 | 17 |
| VEGFR1 |
7
|
0 |
| YES1 | 32 | 4 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK |
6
|
4 |
| BRSK2 |
10
|
3 |
| BTK | 29 | 5 |
| CAMK1 | 69 | 5 |
| CAMKK beta | 41 | 12 |
| CDK2-Cyclin A | 14 | 2 |
| CHK1 |
4
|
0 |
| CHK2 |
-5
|
0 |
| CK1 delta | 59 | 10 |
| CK2 | 65 | 5 |
| CSK | 69 | 6 |
| DYRK1A | 11 | 6 |
| DYRK2 |
2
|
0 |
| DYRK3 |
4
|
1 |
| EF2K | 86 | 3 |
| EPH-A2 | 54 | 5 |
| EPH-B3 | 90 | 11 |
| ERK1 | 60 | 52 |
| ERK2 | 41 | 9 |
| ERK8 |
2
|
0 |
| FGF-R1 |
2
|
0 |
| GSK3 beta |
7
|
3 |
| HIPK2 |
7
|
0 |
| IGF-1R | 33 | 7 |
| IKK beta | 75 | 27 |
| IKK epsilon | 12 | 1 |
| IR | 101 | 11 |
| IRR | 16 | 5 |
| JNK1 | 99 | 1 |
| JNK2 | 43 | 0 |
| Lck |
10
|
0 |
| MAPKAP-K2 | 49 | 6 |
| MARK3 |
5
|
1 |
| MELK |
3
|
0 |
| MKK1 |
1
|
0 |
| MNK1 | 54 | 0 |
| MNK2 | 46 | 5 |
| MSK1 | 73 | 2 |
| MST2 |
2
|
1 |
| MST4 | 18 | 0 |
| NEK2a | 75 | 2 |
| NEK6 | 76 | 10 |
| p38 alpha MAPK | 80 | 4 |
| p38 beta MAPK | 80 | 5 |
| p38 delta MAPK | 62 | 1 |
| p38 gamma MAPK | 86 | 4 |
| PAK4 | 31 | 0 |
| PAK5 | 43 | 0 |
| PAK6 | 77 | 3 |
| PDK1 |
3
|
0 |
| PHK |
1
|
0 |
| PIM1 |
9
|
0 |
| PIM2 | 34 | 0 |
| PIM3 |
9
|
2 |
| PKA | 66 | 0 |
| PKB alpha | 69 | 0 |
| PKB beta | 77 | 7 |
| PKC alpha | 83 | 5 |
| PKC zeta | 66 | 1 |
| PKD1 |
3
|
0 |
| PLK1 | 42 | 4 |
| PRAK | 50 | 6 |
| PRK2 |
5
|
3 |
| ROCK 2 | 37 | 4 |
| RSK1 |
10
|
4 |
| RSK2 | 32 | 14 |
| S6K1 | 32 | 0 |
| SGK1 | 32 | 0 |
| SmMLCK | 11 | 1 |
| Src |
7
|
0 |
| SRPK1 | 75 | 1 |
| SYK | 40 | 1 |
| TBK1 |
7
|
6 |
| VEGFR1 |
3
|
1 |
| YES1 |
8
|
0 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK |
4
|
1 |
| BRSK2 | 18 | 3 |
| BTK |
9
|
6 |
| CAMK1 | 19 | 0 |
| CAMKK beta | 35 | 3 |
| CDK2-Cyclin A |
6
|
0 |
| CHK1 |
1
|
0 |
| CHK2 |
1
|
4 |
| CK1 delta | 20 | 5 |
| CK2 | 21 | 1 |
| CSK | 42 | 6 |
| DYRK1A | 27 | 33 |
| DYRK2 |
0
|
0 |
| DYRK3 |
1
|
0 |
| EF2K | 116 | 7 |
| EPH-A2 | 20 | 1 |
| EPH-B3 | 53 | 8 |
| ERK1 |
4
|
0 |
| ERK2 | 16 | 3 |
| ERK8 |
1
|
0 |
| FGF-R1 |
1
|
0 |
| GSK3 beta |
3
|
2 |
| HIPK2 |
1
|
0 |
| IGF-1R |
1
|
0 |
| IKK beta | 26 | 4 |
| IKK epsilon | 11 | 6 |
| IR | 26 | 6 |
| IRR |
5
|
2 |
| JNK1 | 48 | 4 |
| JNK2 | 17 | 0 |
| Lck |
3
|
0 |
| MAPKAP-K2 |
10
|
6 |
| MARK3 |
3
|
1 |
| MELK |
0
|
0 |
| MKK1 |
2
|
1 |
| MNK1 | 30 | 14 |
| MNK2 | 16 | 2 |
| MSK1 | 30 | 0 |
| MST2 |
0
|
0 |
| MST4 | 21 | 6 |
| NEK2a | 28 | 1 |
| NEK6 | 38 | 2 |
| p38 alpha MAPK | 45 | 6 |
| p38 beta MAPK | 49 | 9 |
| p38 delta MAPK | 22 | 1 |
| p38 gamma MAPK | 75 | 27 |
| PAK4 | 29 | 31 |
| PAK5 |
8
|
0 |
| PAK6 | 38 | 4 |
| PDK1 |
0
|
2 |
| PHK |
0
|
0 |
| PIM1 |
2
|
2 |
| PIM2 |
8
|
0 |
| PIM3 |
7
|
2 |
| PKA | 32 | 5 |
| PKB alpha | 62 | 7 |
| PKB beta | 36 | 4 |
| PKC alpha | 27 | 7 |
| PKC zeta | 21 | 4 |
| PKD1 |
3
|
2 |
| PLK1 | 18 | 6 |
| PRAK |
8
|
1 |
| PRK2 |
6
|
0 |
| ROCK 2 |
7
|
1 |
| RSK1 |
5
|
0 |
| RSK2 | 22 | 3 |
| S6K1 | 12 | 1 |
| SGK1 |
6
|
2 |
| SmMLCK |
1
|
1 |
| Src |
1
|
0 |
| SRPK1 | 36 | 3 |
| SYK |
7
|
0 |
| TBK1 | 11 | 9 |
| VEGFR1 |
1
|
0 |
| YES1 |
3
|
1 |