| Compound name | Brutto | MW | CAS | PubChem CID | Action | Reference | Reference |
|---|---|---|---|---|---|---|---|
| Princeton's TrkA inhibitor compound 20h | C24H24BrF3N6O4S2 | 661.52 | Trk A | Kim S.H. Tokarski J.S. (2008) Bioorg. Med. Chem. Lett. 18 634-639 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK | 63 | 5 |
| ASK1 | 106 | 1 |
| Aurora A |
3
|
0 |
| Aurora B | 65 | 0 |
| BRSK1 | 82 | 13 |
| BRSK2 | 88 | 5 |
| BTK | 96 | 1 |
| CAMK1 | 62 | 9 |
| CAMKK beta | 22 | 0 |
| CDK2-Cyclin A | 35 | 2 |
| CHK1 | 54 | 1 |
| CHK2 | 20 | 1 |
| CK1 delta | 99 | 6 |
| CK2 | 119 | 11 |
| CLK2 |
3
|
0 |
| CSK | 103 | 12 |
| DAPK1 | 99 | 5 |
| DYRK1A | 103 | 8 |
| DYRK2 | 101 | 9 |
| DYRK3 | 89 | 11 |
| EF2K | 113 | 8 |
| EPH-A2 | 46 | 13 |
| EPH-A4 | 22 | 6 |
| EPH-B1 | 53 | 0 |
| EPH-B2 | 11 | 1 |
| EPH-B3 | 22 | 3 |
| EPH-B4 | 15 | 1 |
| ERK1 | 103 | 9 |
| ERK2 | 99 | 6 |
| ERK8 |
1
|
0 |
| FGF-R1 | 47 | 4 |
| GCK | 101 | 4 |
| GSK3 beta | 46 | 1 |
| HER4 | 69 | 8 |
| HIPK1 | 45 | 2 |
| HIPK2 | 14 | 2 |
| HIPK3 | 30 | 2 |
| IGF-1R |
2
|
0 |
| IKK beta | 107 | 3 |
| IKK epsilon | 91 | 3 |
| IR | 19 | 3 |
| IRAK4 |
5
|
2 |
| IRR | 69 | 9 |
| JAK2 | 84 | 9 |
| JNK1 | 98 | 8 |
| JNK2 | 98 | 1 |
| JNK3 | 94 | 4 |
| Lck | 43 | 9 |
| LKB1 | 64 | 4 |
| MAPKAP-K2 | 98 | 4 |
| MAPKAP-K3 | 91 | 6 |
| MARK1 | 70 | 11 |
| MARK2 | 81 | 10 |
| MARK3 | 103 | 8 |
| MARK4 | 101 | 8 |
| MEKK1 | 46 | 1 |
| MELK | 42 | 9 |
| MINK1 | 69 | 12 |
| MKK1 | 96 | 2 |
| MKK2 | 86 | 7 |
| MKK6 | 94 | 14 |
| MLK1 | 78 | 4 |
| MLK3 | 84 | 3 |
| MNK1 | 97 | 9 |
| MNK2 | 120 | 5 |
| MSK1 | 59 | 3 |
| MST2 | 16 | 0 |
| MST4 | 50 | 0 |
| NEK2a | 108 | 2 |
| NEK6 | 103 | 5 |
| NUAK1 | 40 | 4 |
| p38 alpha MAPK | 101 | 9 |
| p38 beta MAPK | 87 | 1 |
| p38 delta MAPK | 97 | 4 |
| p38 gamma MAPK | 77 | 2 |
| PAK2 | 44 | 6 |
| PAK4 | 69 | 5 |
| PAK5 | 62 | 3 |
| PAK6 | 71 | 12 |
| PDK1 | 105 | 0 |
| PHK | 43 | 0 |
| PIM1 | 54 | 7 |
| PIM2 | 94 | 1 |
| PIM3 | 53 | 13 |
| PKA | 98 | 7 |
| PKB alpha | 105 | 3 |
| PKB beta | 80 | 8 |
| PKC alpha | 41 | 1 |
| PKC zeta | 104 | 4 |
| PKD1 | 89 | 3 |
| PLK1 | 97 | 2 |
| PRAK | 96 | 3 |
| PRK2 | 80 | 13 |
| RIPK2 | 20 | 0 |
| ROCK 2 | 90 | 0 |
| RSK1 | 31 | 1 |
| RSK2 | 67 | 1 |
| S6K1 | 95 | 6 |
| SGK1 | 89 | 4 |
| SmMLCK | 51 | 6 |
| Src | 22 | 3 |
| SRPK1 | 71 | 12 |
| SYK | 82 | 14 |
| TAK1 | 107 | 3 |
| TAO1 | 42 | 5 |
| TBK1 | 87 | 3 |
| TrkA | 14 | 1 |
| TTK | 75 | 2 |
| VEGFR1 | 56 | 15 |
| YES1 | 11 | 2 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK | 47 | 2 |
| ASK1 | 101 | 12 |
| Aurora A |
3
|
0 |
| Aurora B | 42 | 7 |
| BRSK1 | 81 | 9 |
| BRSK2 | 80 | 3 |
| BTK | 53 | 3 |
| CAMK1 | 59 | 9 |
| CAMKK beta | 19 | 2 |
| CDK2-Cyclin A | 15 | 4 |
| CHK1 | 53 | 10 |
| CHK2 | 18 | 1 |
| CK1 delta | 87 | 2 |
| CK2 | 104 | 7 |
| CLK2 |
3
|
0 |
| CSK | 88 | 12 |
| DAPK1 | 96 | 8 |
| DYRK1A | 101 | 5 |
| DYRK2 | 87 | 7 |
| DYRK3 | 78 | 4 |
| EF2K | 96 | 10 |
| EPH-A2 | 36 | 7 |
| EPH-A4 | 29 | 13 |
| EPH-B1 | 36 | 5 |
| EPH-B2 |
4
|
7 |
| EPH-B3 | 20 | 4 |
| EPH-B4 | 13 | 0 |
| ERK1 | 78 | 6 |
| ERK2 | 103 | 9 |
| ERK8 |
1
|
1 |
| FGF-R1 | 43 | 3 |
| GCK | 93 | 2 |
| GSK3 beta | 41 | 3 |
| HER4 | 64 | 15 |
| HIPK1 | 42 | 2 |
| HIPK2 | 13 | 0 |
| HIPK3 | 31 | 3 |
| IGF-1R |
2
|
0 |
| IKK beta | 92 | 3 |
| IKK epsilon | 80 | 8 |
| IR | 14 | 3 |
| IRAK4 |
3
|
0 |
| IRR | 80 | 15 |
| JAK2 | 80 | 8 |
| JNK1 | 99 | 4 |
| JNK2 | 94 | 5 |
| JNK3 | 107 | 0 |
| Lck | 13 | 1 |
| LKB1 | 62 | 4 |
| MAPKAP-K2 | 86 | 2 |
| MAPKAP-K3 | 77 | 2 |
| MARK1 | 78 | 9 |
| MARK2 | 87 | 5 |
| MARK3 | 89 | 1 |
| MARK4 | 118 | 13 |
| MEKK1 | 35 | 0 |
| MELK | 15 | 5 |
| MINK1 | 64 | 4 |
| MKK1 | 85 | 1 |
| MKK2 | 77 | 7 |
| MKK6 | 95 | 2 |
| MLK1 | 69 | 4 |
| MLK3 | 77 | 12 |
| MNK1 | 103 | 13 |
| MNK2 | 92 | 11 |
| MSK1 | 51 | 1 |
| MST2 | 19 | 0 |
| MST4 | 50 | 1 |
| NEK2a | 87 | 1 |
| NEK6 | 101 | 3 |
| NUAK1 | 37 | 5 |
| p38 alpha MAPK | 89 | 0 |
| p38 beta MAPK | 76 | 5 |
| p38 delta MAPK | 24 | 2 |
| p38 gamma MAPK | 80 | 6 |
| PAK2 | 44 | 1 |
| PAK4 | 67 | 5 |
| PAK5 | 58 | 3 |
| PAK6 | 72 | 5 |
| PDK1 | 98 | 5 |
| PHK | 15 | 2 |
| PIM1 | 49 | 1 |
| PIM2 | 92 | 1 |
| PIM3 | 72 | 4 |
| PKA | 88 | 0 |
| PKB alpha | 86 | 10 |
| PKB beta | 94 | 2 |
| PKC alpha | 45 | 7 |
| PKC zeta | 98 | 9 |
| PKD1 | 85 | 1 |
| PLK1 | 85 | 1 |
| PRAK | 94 | 1 |
| PRK2 | 78 | 2 |
| RIPK2 | 17 | 0 |
| ROCK 2 | 82 | 3 |
| RSK1 | 29 | 1 |
| RSK2 | 64 | 7 |
| S6K1 | 92 | 2 |
| SGK1 | 90 | 1 |
| SmMLCK | 43 | 5 |
| Src | 20 | 3 |
| SRPK1 | 59 | 6 |
| SYK | 64 | 2 |
| TAK1 | 84 | 7 |
| TAO1 | 33 | 1 |
| TBK1 | 78 | 4 |
| TrkA | 19 | 8 |
| TTK | 73 | 9 |
| VEGFR1 | 52 | 11 |
| YES1 | 11 | 1 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| AMPK |
3
|
1 |
| Aurora A |
0
|
0 |
| Aurora B |
7
|
1 |
| BRSK1 | 41 | 11 |
| BRSK2 | 40 | 1 |
| BTK |
8
|
0 |
| CAMK1 | 11 | 0 |
| CAMKK beta | 19 | 2 |
| CDK2-Cyclin A |
3
|
1 |
| CHK1 | 52 | 6 |
| CHK2 |
4
|
1 |
| CK1 delta | 68 | 8 |
| CK2 | 85 | 1 |
| CLK2 |
1
|
0 |
| CSK |
9
|
1 |
| DAPK1 | 63 | 5 |
| DYRK1A | 61 | 3 |
| DYRK2 | 80 | 3 |
| DYRK3 | 43 | 1 |
| EF2K | 92 | 10 |
| EPH-A2 | 13 | 2 |
| EPH-A4 |
0
|
5 |
| EPH-B2 |
4
|
0 |
| EPH-B3 |
6
|
4 |
| EPH-B4 |
4
|
1 |
| ERK1 | 99 | 1 |
| ERK2 | 85 | 8 |
| ERK8 |
1
|
0 |
| FGF-R1 | 11 | 0 |
| GCK | 33 | 5 |
| GSK3 beta | 37 | 3 |
| HER4 | 51 | 0 |
| HIPK1 |
5
|
1 |
| HIPK2 |
5
|
0 |
| HIPK3 | 17 | 1 |
| IGF-1R |
2
|
1 |
| IKK beta | 84 | 7 |
| IKK epsilon | 76 | 9 |
| IR |
1
|
0 |
| IRAK4 |
2
|
1 |
| IRR | 52 | 0 |
| JAK2 | 30 | 0 |
| JNK1 | 53 | 9 |
| JNK2 | 54 | 5 |
| JNK3 | 54 | 3 |
| Lck |
5
|
3 |
| LKB1 |
8
|
1 |
| MAPKAP-K2 | 80 | 0 |
| MAPKAP-K3 | 85 | 7 |
| MARK1 | 58 | 1 |
| MARK2 | 44 | 3 |
| MARK3 | 57 | 2 |
| MARK4 | 43 | 3 |
| MEKK1 |
5
|
1 |
| MELK |
5
|
2 |
| MINK1 |
8
|
1 |
| MKK1 | 40 | 2 |
| MLK1 | 17 | 2 |
| MLK3 | 51 | 0 |
| MNK1 | 77 | 13 |
| MNK2 | 73 | 3 |
| MSK1 | 22 | 5 |
| MST2 |
3
|
0 |
| MST4 | 17 | 0 |
| NEK2a | 71 | 4 |
| NEK6 | 85 | 10 |
| NUAK1 |
7
|
0 |
| p38 alpha MAPK | 47 | 5 |
| p38 beta MAPK | 48 | 7 |
| p38 delta MAPK |
5
|
1 |
| p38 gamma MAPK | 45 | 5 |
| PAK2 | 16 | 2 |
| PAK4 | 20 | 6 |
| PAK5 | 22 | 0 |
| PAK6 | 27 | 1 |
| PDK1 | 106 | 8 |
| PHK |
2
|
0 |
| PIM1 | 11 | 1 |
| PIM2 | 77 | 11 |
| PIM3 | 21 | 1 |
| PKA | 54 | 2 |
| PKB alpha | 53 | 1 |
| PKB beta | 46 | 1 |
| PKC alpha | 11 | 2 |
| PKC zeta | 58 | 4 |
| PKD1 | 45 | 5 |
| PLK1 | 114 | 3 |
| PRAK | 96 | 9 |
| PRK2 | 32 | 2 |
| RIPK2 |
8
|
2 |
| ROCK 2 | 63 | 5 |
| RSK1 |
6
|
0 |
| RSK2 | 18 | 7 |
| S6K1 | 11 | 6 |
| SGK1 | 41 | 8 |
| SmMLCK |
5
|
0 |
| Src |
2
|
0 |
| SRPK1 | 11 | 3 |
| SYK | 28 | 7 |
| TAK1 | 27 | 0 |
| TBK1 | 93 | 1 |
| TrkA |
4
|
1 |
| TTK | 42 | 4 |
| VEGFR1 | 19 | 1 |
| YES1 |
6
|
0 |