| Compound name | Brutto | MW | CAS | PubChem CID | Action | Reference | Reference |
|---|---|---|---|---|---|---|---|
| Wyeth PDK1 Inhibitor Compound 1 | C19H22Cl4N4O2 | 480.21 | PDK1 | Gopalsamy A. (2007) Journal of Medicinal Chemistry 50 (23) 5547-5549 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK | 46 | 1 |
| ASK1 | 67 | 7 |
| Aurora A | 103 | 8 |
| Aurora B | 97 | 5 |
| BRSK1 | 82 | 1 |
| BRSK2 | 84 | 5 |
| BTK | 87 | 1 |
| CAMK1 | 91 | 1 |
| CAMKK beta | 87 | 5 |
| CDK2-Cyclin A | 74 | 2 |
| CHK1 | 53 | 3 |
| CHK2 | 46 | 14 |
| CK1 delta | 83 | 1 |
| CK2 | 89 | 7 |
| CLK2 | 61 | 4 |
| CSK | 85 | 5 |
| DAPK1 | 81 | 1 |
| DYRK1A | 100 | 1 |
| DYRK2 | 91 | 11 |
| DYRK3 | 89 | 2 |
| EF2K | 83 | 3 |
| EPH-A2 | 109 | 14 |
| EPH-A4 | 95 | 2 |
| EPH-B1 | 105 | 3 |
| EPH-B2 | 112 | 3 |
| EPH-B3 | 93 | 13 |
| EPH-B4 | 98 | 0 |
| ERK1 | 72 | 3 |
| ERK2 | 69 | 3 |
| ERK8 | 85 | 6 |
| FGF-R1 | 76 | 0 |
| GCK | 11 | 0 |
| GSK3 beta | 64 | 2 |
| HER4 | 73 | 5 |
| HIPK1 | 78 | 1 |
| HIPK2 | 56 | 1 |
| HIPK3 | 98 | 0 |
| IGF-1R | 99 | 4 |
| IKK beta | 56 | 6 |
| IKK epsilon |
8
|
0 |
| IR | 65 | 12 |
| IRAK4 | 61 | 0 |
| IRR | 73 | 2 |
| JAK2 | 14 | 1 |
| JNK1 | 90 | 3 |
| JNK2 | 91 | 10 |
| JNK3 | 97 | 6 |
| Lck | 84 | 11 |
| LKB1 | 77 | 4 |
| MAPKAP-K2 | 101 | 5 |
| MAPKAP-K3 | 94 | 6 |
| MARK1 | 55 | 3 |
| MARK2 | 73 | 3 |
| MARK3 | 35 | 0 |
| MARK4 | 65 | 7 |
| MEKK1 | 51 | 9 |
| MELK | 71 | 3 |
| MINK1 | 15 | 2 |
| MKK1 |
10
|
0 |
| MKK2 | 34 | 4 |
| MKK6 | 95 | 2 |
| MLK1 | 26 | 2 |
| MLK3 |
8
|
1 |
| MNK1 | 114 | 9 |
| MNK2 | 123 | 3 |
| MSK1 | 82 | 5 |
| MST2 | 15 | 1 |
| MST4 | 32 | 0 |
| NEK2a | 55 | 6 |
| NEK6 | 99 | 6 |
| NUAK1 | 30 | 1 |
| p38 alpha MAPK | 100 | 3 |
| p38 beta MAPK | 95 | 4 |
| p38 delta MAPK | 92 | 1 |
| p38 gamma MAPK | 98 | 9 |
| PAK2 | 77 | 7 |
| PAK4 | 72 | 3 |
| PAK5 | 76 | 7 |
| PAK6 | 64 | 0 |
| PDK1 | 35 | 4 |
| PHK | 69 | 2 |
| PIM1 | 94 | 7 |
| PIM2 | 91 | 7 |
| PIM3 | 72 | 6 |
| PKA | 86 | 1 |
| PKB alpha | 94 | 9 |
| PKB beta | 86 | 3 |
| PKC alpha | 79 | 4 |
| PKC zeta | 89 | 3 |
| PKD1 | 19 | 5 |
| PLK1 | 79 | 5 |
| PRAK | 86 | 3 |
| PRK2 | 71 | 2 |
| RIPK2 | 82 | 6 |
| ROCK 2 | 54 | 1 |
| RSK1 | 14 | 1 |
| RSK2 | 15 | 1 |
| S6K1 | 82 | 5 |
| SGK1 | 98 | 2 |
| SmMLCK | 77 | 2 |
| Src | 86 | 2 |
| SRPK1 | 96 | 7 |
| SYK | 74 | 5 |
| TAK1 | 41 | 7 |
| TAO1 | 59 | 2 |
| TBK1 | 11 | 0 |
| TrkA | 73 | 4 |
| TTK | 68 | 1 |
| VEGFR1 | 47 | 5 |
| YES1 | 81 | 1 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK | 20 | 3 |
| ASK1 | 21 | 1 |
| Aurora A | 82 | 3 |
| Aurora B | 68 | 6 |
| BRSK1 | 67 | 6 |
| BRSK2 | 77 | 6 |
| BTK | 70 | 7 |
| CAMK1 | 82 | 3 |
| CAMKK beta | 91 | 2 |
| CDK2-Cyclin A | 69 | 8 |
| CHK1 | 20 | 1 |
| CHK2 |
7
|
2 |
| CK1 delta | 70 | 5 |
| CK2 | 75 | 1 |
| CLK2 | 27 | 0 |
| CSK | 88 | 1 |
| DAPK1 | 59 | 8 |
| DYRK1A | 55 | 2 |
| DYRK2 | 78 | 1 |
| DYRK3 | 71 | 2 |
| EF2K | 77 | 3 |
| EPH-A2 | 99 | 7 |
| EPH-A4 | 87 | 2 |
| EPH-B1 | 102 | 0 |
| EPH-B2 | 105 | 8 |
| EPH-B3 | 91 | 1 |
| EPH-B4 | 95 | 1 |
| ERK1 | 31 | 2 |
| ERK2 | 58 | 7 |
| ERK8 | 48 | 1 |
| FGF-R1 | 49 | 0 |
| GCK |
4
|
1 |
| GSK3 beta | 32 | 2 |
| HER4 | 46 | 3 |
| HIPK1 | 53 | 3 |
| HIPK2 | 23 | 7 |
| HIPK3 | 69 | 5 |
| IGF-1R | 72 | 10 |
| IKK beta | 31 | 0 |
| IKK epsilon |
9
|
1 |
| IR | 32 | 4 |
| IRAK4 | 46 | 4 |
| IRR | 54 | 2 |
| JAK2 |
6
|
1 |
| JNK1 | 80 | 8 |
| JNK2 | 94 | 8 |
| JNK3 | 63 | 4 |
| Lck | 65 | 11 |
| LKB1 | 84 | 11 |
| MAPKAP-K2 | 97 | 0 |
| MAPKAP-K3 | 79 | 3 |
| MARK1 | 34 | 2 |
| MARK2 | 72 | 9 |
| MARK3 | 18 | 3 |
| MARK4 | 40 | 7 |
| MEKK1 | 40 | 11 |
| MELK | 61 | 3 |
| MINK1 |
7
|
2 |
| MKK1 |
2
|
3 |
| MKK2 | 16 | 3 |
| MKK6 | 100 | 1 |
| MLK1 | 27 | 2 |
| MLK3 |
4
|
1 |
| MNK1 | 90 | 3 |
| MNK2 | 115 | 2 |
| MSK1 | 71 | 5 |
| MST2 |
4
|
1 |
| MST4 | 14 | 1 |
| NEK2a | 18 | 3 |
| NEK6 | 95 | 3 |
| NUAK1 | 25 | 7 |
| p38 alpha MAPK | 116 | 7 |
| p38 beta MAPK | 90 | 1 |
| p38 delta MAPK | 84 | 13 |
| p38 gamma MAPK | 109 | 8 |
| PAK2 | 50 | 1 |
| PAK4 | 42 | 5 |
| PAK5 | 38 | 0 |
| PAK6 | 56 | 3 |
| PDK1 | 14 | 1 |
| PHK | 26 | 1 |
| PIM1 | 69 | 3 |
| PIM2 | 95 | 1 |
| PIM3 | 29 | 4 |
| PKA | 77 | 1 |
| PKB alpha | 84 | 0 |
| PKB beta | 64 | 2 |
| PKC alpha | 62 | 5 |
| PKC zeta | 115 | 4 |
| PKD1 |
10
|
1 |
| PLK1 | 45 | 2 |
| PRAK | 82 | 8 |
| PRK2 | 34 | 3 |
| RIPK2 | 70 | 6 |
| ROCK 2 | 15 | 4 |
| RSK1 |
2
|
1 |
| RSK2 |
9
|
0 |
| S6K1 | 57 | 6 |
| SGK1 | 86 | 2 |
| SmMLCK | 56 | 2 |
| Src | 89 | 10 |
| SRPK1 | 105 | 10 |
| SYK | 43 | 4 |
| TAK1 |
5
|
2 |
| TAO1 | 28 | 6 |
| TBK1 | 17 | 7 |
| TrkA | 56 | 4 |
| TTK | 44 | 1 |
| VEGFR1 | 23 | 1 |
| YES1 | 57 | 0 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK | 25 | 21 |
| BRSK2 | 74 | 5 |
| BTK | 49 | 1 |
| CAMK1 | 17 | 5 |
| CAMKK beta | 71 | 4 |
| CDK2-Cyclin A | 58 | 3 |
| CHK1 |
2
|
1 |
| CHK2 | 13 | 2 |
| CK1 delta | 46 | 2 |
| CK2 | 80 | 2 |
| CSK | 78 | 5 |
| DYRK1A | 55 | 5 |
| DYRK2 | 51 | 5 |
| DYRK3 | 53 | 3 |
| EF2K | 103 | 7 |
| EPH-A2 | 70 | 1 |
| EPH-B3 | 34 | 0 |
| ERK1 | 48 | 1 |
| ERK2 | 49 | 7 |
| ERK8 | 18 | 1 |
| FGF-R1 | 30 | 0 |
| GSK3 beta | 24 | 0 |
| HIPK2 | 41 | 0 |
| IGF-1R | 38 | 7 |
| IKK beta | 50 | 1 |
| IKK epsilon |
6
|
0 |
| IR | 53 | 2 |
| IRR | 36 | 4 |
| JNK1 | 80 | 19 |
| JNK2 | 86 | 1 |
| Lck | 24 | 2 |
| MAPKAP-K2 | 105 | 55 |
| MARK3 |
5
|
0 |
| MELK | 34 | 13 |
| MKK1 |
6
|
4 |
| MNK1 | 99 | 12 |
| MNK2 | 93 | 2 |
| MSK1 | 59 | 8 |
| MST2 |
1
|
0 |
| MST4 | 35 | 7 |
| NEK2a |
6
|
1 |
| NEK6 | 79 | 8 |
| p38 alpha MAPK | 108 | 7 |
| p38 beta MAPK | 84 | 15 |
| p38 delta MAPK | 87 | 8 |
| p38 gamma MAPK | 86 | 3 |
| PAK4 | 21 | 0 |
| PAK5 | 25 | 1 |
| PAK6 | 54 | 2 |
| PDK1 |
3
|
1 |
| PHK | 13 | 0 |
| PIM1 | 36 | 12 |
| PIM2 | 88 | 4 |
| PIM3 | 21 | 1 |
| PKA | 53 | 8 |
| PKB alpha | 93 | 5 |
| PKB beta | 88 | 5 |
| PKC alpha | 23 | 1 |
| PKC zeta | 37 | 2 |
| PKD1 |
2
|
2 |
| PLK1 | 26 | 5 |
| PRAK | 36 | 0 |
| PRK2 | 16 | 1 |
| ROCK 2 | 14 | 2 |
| RSK1 |
3
|
0 |
| RSK2 |
4
|
0 |
| S6K1 | 34 | 0 |
| SGK1 | 58 | 3 |
| SmMLCK | 33 | 5 |
| Src | 70 | 0 |
| SRPK1 | 82 | 0 |
| SYK | 37 | 2 |
| TBK1 | 18 | 2 |
| VEGFR1 | 20 | 12 |
| YES1 | 64 | 9 |