| Compound name | Brutto | MW | CAS | PubChem CID | Action | Reference | Reference |
|---|---|---|---|---|---|---|---|
| Novartis 12a (PKD1) | C23H29F3N6O3 | 494.51 | PKD1 | Meredith E.L. (2010) J.Med.Chem. 53 5422-5438 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| ABL | 102 | 11 |
| AMPK | 97 | 17 |
| ASK1 | 98 | 9 |
| Aurora A | 92 | 7 |
| Aurora B | 132 | 19 |
| BRK | 114 | 1 |
| BRSK1 | 96 | 15 |
| BRSK2 | 67 | 8 |
| BTK | 92 | 2 |
| CAMK1 | 81 | 3 |
| CAMKK beta | 85 | 17 |
| CDK2-Cyclin A | 66 | 7 |
| CHK1 | 115 | 34 |
| CHK2 | 102 | 1 |
| CK1 delta | 75 | 17 |
| CK2 | 107 | 2 |
| CLK2 | 78 | 8 |
| CSK | 113 | 11 |
| DAPK1 | 102 | 1 |
| DYRK1A | 97 | 1 |
| DYRK2 | 74 | 11 |
| DYRK3 | 39 | 4 |
| EF2K | 105 | 8 |
| EIF2AK3 | 108 | 12 |
| EPH-A2 | 78 | 13 |
| EPH-A4 | 90 | 12 |
| EPH-B1 | 96 | 8 |
| EPH-B2 | 105 | 10 |
| EPH-B3 | 105 | 3 |
| EPH-B4 | 103 | 6 |
| ERK1 | 78 | 10 |
| ERK2 | 36 | 19 |
| ERK8 | 63 | 7 |
| FGF-R1 | 110 | 7 |
| GCK | 41 | 4 |
| GSK3 beta | 86 | 3 |
| HER4 | 83 | 6 |
| HIPK1 | 99 | 10 |
| HIPK2 | 89 | 8 |
| HIPK3 | 95 | 5 |
| IGF-1R | 97 | 7 |
| IKK beta | 85 | 1 |
| IKK epsilon | 98 | 8 |
| IR | 89 | 5 |
| IRAK1 | 92 | 1 |
| IRAK4 | 96 | 7 |
| IRR | 100 | 13 |
| JAK2 | 82 | 7 |
| JNK1 | 109 | 15 |
| JNK2 | 91 | 1 |
| JNK3 | 88 | 13 |
| Lck | 84 | 8 |
| LKB1 | 77 | 2 |
| MAPKAP-K2 | 99 | 14 |
| MAPKAP-K3 | 92 | 1 |
| MARK1 | 51 | 13 |
| MARK2 | 97 | 11 |
| MARK3 | 92 | 17 |
| MARK4 | 87 | 4 |
| MEKK1 | 115 | 8 |
| MELK | 108 | 7 |
| MINK1 | 65 | 4 |
| MKK1 | 86 | 3 |
| MKK2 | 106 | 4 |
| MKK6 | 92 | 8 |
| MLK1 | 81 | 25 |
| MLK3 | 93 | 2 |
| MNK1 | 95 | 9 |
| MNK2 | 76 | 6 |
| MPSK1 | 100 | 4 |
| MSK1 | 97 | 11 |
| MST2 | 103 | 4 |
| MST4 | 117 | 2 |
| NEK2a | 111 | 6 |
| NEK6 | 86 | 10 |
| NUAK1 | 59 | 22 |
| OSR1 | 98 | 3 |
| p38 alpha MAPK | 104 | 0 |
| p38 beta MAPK | 99 | 0 |
| p38 delta MAPK | 89 | 2 |
| p38 gamma MAPK | 95 | 11 |
| PAK2 | 105 | 10 |
| PAK4 | 101 | 11 |
| PAK5 | 97 | 0 |
| PAK6 | 99 | 5 |
| PDK1 | 94 | 13 |
| PHK | 82 | 7 |
| PIM1 | 114 | 5 |
| PIM2 | 99 | 1 |
| PIM3 | 97 | 1 |
| PKA | 105 | 10 |
| PKB alpha | 109 | 2 |
| PKB beta | 97 | 14 |
| PKC alpha | 97 | 19 |
| PKC gamma | 106 | 2 |
| PKC zeta | 88 | 8 |
| PKD1 |
6
|
3 |
| PLK1 | 101 | 9 |
| PRAK | 109 | 3 |
| PRK2 | 96 | 6 |
| RIPK2 | 96 | 13 |
| ROCK 2 | 99 | 4 |
| RSK1 | 88 | 12 |
| RSK2 | 98 | 8 |
| S6K1 | 92 | 0 |
| SGK1 | 63 | 64 |
| SmMLCK | 85 | 14 |
| Src | 106 | 8 |
| SRPK1 | 105 | 10 |
| STK33 | 103 | 16 |
| SYK | 90 | 2 |
| TAK1 | 94 | 2 |
| TAO1 | 103 | 7 |
| TBK1 | 100 | 20 |
| TESK1 | 99 | 7 |
| TIE2 | 101 | 4 |
| TLK1 | 91 | 8 |
| TrkA | 72 | 1 |
| TSSK1 | 84 | 10 |
| TTBK1 | 93 | 8 |
| TTK | 111 | 14 |
| VEGFR1 | 95 | 12 |
| YES1 | 107 | 6 |
| ZAP70 | 108 | 14 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| ABL | 112 | 5 |
| AMPK | 61 | 9 |
| ASK1 | 84 | 3 |
| Aurora A | 88 | 7 |
| Aurora B | 117 | 0 |
| BRK | 124 | 15 |
| BRSK1 | 73 | 10 |
| BRSK2 | 26 | 4 |
| BTK | 120 | 4 |
| CAMK1 | 20 | 5 |
| CAMKK beta | 99 | 3 |
| CDK2-Cyclin A | 30 | 5 |
| CHK1 | 100 | 12 |
| CHK2 | 106 | 16 |
| CK1 delta | 42 | 6 |
| CK2 | 110 | 19 |
| CLK2 | 70 | 22 |
| CSK | 116 | 3 |
| DAPK1 | 93 | 16 |
| DYRK1A | 63 | 7 |
| DYRK2 | 29 | 2 |
| DYRK3 | 14 | 12 |
| EF2K | 111 | 11 |
| EIF2AK3 | 101 | 2 |
| EPH-A2 | 99 | 1 |
| EPH-A4 | 78 | 4 |
| EPH-B1 | 111 | 7 |
| EPH-B2 | 129 | 26 |
| EPH-B3 | 124 | 15 |
| EPH-B4 | 84 | 23 |
| ERK1 | 34 | 3 |
| ERK2 | 29 | 1 |
| ERK8 | 26 | 2 |
| FGF-R1 | 85 | 13 |
| GCK | 82 | 6 |
| GSK3 beta | 82 | 14 |
| HER4 | 99 | 23 |
| HIPK1 | 99 | 1 |
| HIPK2 | 125 | 1 |
| HIPK3 | 92 | 1 |
| IGF-1R | 102 | 12 |
| IKK beta | 50 | 1 |
| IKK epsilon | 87 | 13 |
| IR | 86 | 5 |
| IRAK1 | 102 | 21 |
| IRAK4 | 127 | 16 |
| IRR | 107 | 6 |
| JAK2 | 87 | 4 |
| JNK1 | 100 | 8 |
| JNK2 | 94 | 32 |
| JNK3 | 79 | 8 |
| Lck | 30 | 7 |
| LKB1 | 96 | 24 |
| MAPKAP-K2 | 72 | 12 |
| MAPKAP-K3 | 100 | 16 |
| MARK1 | 94 | 19 |
| MARK2 | 63 | 4 |
| MARK3 | 40 | 7 |
| MARK4 | 46 | 9 |
| MEKK1 | 114 | 27 |
| MELK | 78 | 17 |
| MINK1 | 13 | 1 |
| MKK1 | 77 | 18 |
| MKK2 | 123 | 2 |
| MKK6 | 29 | 6 |
| MLK1 | 69 | 3 |
| MLK3 | 86 | 10 |
| MNK1 | 38 | 3 |
| MNK2 | 31 | 2 |
| MPSK1 | 93 | 6 |
| MSK1 | 109 | 12 |
| MST2 | 110 | 1 |
| MST4 | 107 | 4 |
| NEK2a | 129 | 8 |
| NEK6 | 87 | 8 |
| NUAK1 | 17 | 5 |
| OSR1 | 104 | 6 |
| p38 alpha MAPK | 116 | 13 |
| p38 beta MAPK | 96 | 7 |
| p38 delta MAPK | 93 | 7 |
| p38 gamma MAPK | 96 | 5 |
| PAK2 | 93 | 1 |
| PAK4 | 93 | 6 |
| PAK5 | 90 | 1 |
| PAK6 | 99 | 7 |
| PDK1 | 114 | 28 |
| PHK | 29 | 1 |
| PIM1 | 98 | 14 |
| PIM2 | 102 | 5 |
| PIM3 | 58 | 1 |
| PKA | 109 | 8 |
| PKB alpha | 106 | 8 |
| PKB beta | 57 | 11 |
| PKC alpha | 95 | 15 |
| PKC gamma | 103 | 7 |
| PKC zeta | 109 | 3 |
| PKD1 |
5
|
2 |
| PLK1 | 117 | 3 |
| PRAK | 97 | 1 |
| PRK2 | 66 | 3 |
| RIPK2 | 96 | 3 |
| ROCK 2 | 108 | 26 |
| RSK1 | 53 | 9 |
| RSK2 | 110 | 22 |
| S6K1 | 96 | 1 |
| SGK1 | 104 | 25 |
| SmMLCK | 40 | 4 |
| Src | 90 | 7 |
| SRPK1 | 86 | 5 |
| STK33 | 83 | 22 |
| SYK | 104 | 6 |
| TAK1 | 100 | 5 |
| TAO1 | 113 | 22 |
| TBK1 | 88 | 9 |
| TESK1 | 102 | 3 |
| TIE2 | 111 | 9 |
| TLK1 | 107 | 9 |
| TrkA | 68 | 22 |
| TSSK1 | 56 | 1 |
| TTBK1 | 128 | 28 |
| TTK | 87 | 0 |
| VEGFR1 | 88 | 13 |
| YES1 | 94 | 6 |
| ZAP70 | 114 | 17 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| ABL | 100 | 5 |
| AMPK | 20 | 3 |
| ASK1 | 21 | 5 |
| Aurora A | 112 | 8 |
| Aurora B | 115 | 14 |
| BRK | 103 | 2 |
| BRSK1 | 26 | 1 |
| BRSK2 |
8
|
2 |
| BTK | 79 | 10 |
| CAMK1 |
1
|
0 |
| CAMKK beta | 62 | 17 |
| CDK2-Cyclin A | 11 | 2 |
| CHK1 | 70 | 1 |
| CHK2 | 88 | 10 |
| CK1 delta | 18 | 2 |
| CK2 | 65 | 1 |
| CLK2 | 51 | 8 |
| CSK | 90 | 11 |
| DAPK1 | 40 | 10 |
| DYRK1A | 21 | 2 |
| DYRK2 |
10
|
5 |
| DYRK3 |
7
|
5 |
| EF2K | 87 | 5 |
| EIF2AK3 | 97 | 1 |
| EPH-A2 | 82 | 10 |
| EPH-A4 | 48 | 9 |
| EPH-B1 | 99 | 1 |
| EPH-B2 | 113 | 29 |
| EPH-B3 | 94 | 5 |
| EPH-B4 | 91 | 3 |
| ERK1 |
10
|
2 |
| ERK2 |
6
|
2 |
| ERK8 |
4
|
2 |
| FGF-R1 | 82 | 1 |
| GCK | 44 | 1 |
| GSK3 beta | 51 | 7 |
| HER4 | 73 | 0 |
| HIPK1 | 106 | 2 |
| HIPK2 | 87 | 14 |
| HIPK3 | 101 | 11 |
| IGF-1R | 99 | 14 |
| IKK beta | 23 | 4 |
| IKK epsilon | 48 | 9 |
| IR | 93 | 11 |
| IRAK1 | 87 | 3 |
| IRAK4 | 92 | 4 |
| IRR | 97 | 9 |
| JAK2 | 89 | 6 |
| JNK1 | 38 | 18 |
| JNK2 | 35 | 4 |
| JNK3 | 31 | 4 |
| Lck |
9
|
1 |
| LKB1 | 71 | 6 |
| MAPKAP-K2 | 22 | 1 |
| MAPKAP-K3 | 92 | 12 |
| MARK1 | 76 | 9 |
| MARK2 | 31 | 4 |
| MARK3 | 15 | 4 |
| MARK4 |
10
|
4 |
| MEKK1 | 102 | 13 |
| MELK | 40 | 8 |
| MINK1 |
2
|
1 |
| MKK1 | 49 | 1 |
| MKK2 | 115 | 2 |
| MKK6 | 16 | 3 |
| MLK1 | 103 | 12 |
| MLK3 | 81 | 4 |
| MNK1 |
7
|
5 |
| MNK2 |
6
|
2 |
| MPSK1 | 84 | 12 |
| MSK1 | 79 | 3 |
| MST2 | 98 | 0 |
| MST4 | 95 | 1 |
| NEK2a | 113 | 1 |
| NEK6 | 42 | 5 |
| NUAK1 | 32 | 4 |
| OSR1 | 73 | 6 |
| p38 alpha MAPK | 103 | 3 |
| p38 beta MAPK | 62 | 9 |
| p38 delta MAPK | 50 | 1 |
| p38 gamma MAPK | 58 | 2 |
| PAK2 | 57 | 3 |
| PAK4 | 74 | 3 |
| PAK5 | 71 | 4 |
| PAK6 | 81 | 9 |
| PDK1 | 107 | 14 |
| PHK |
5
|
1 |
| PIM1 | 65 | 7 |
| PIM2 | 99 | 8 |
| PIM3 | 42 | 4 |
| PKA | 93 | 14 |
| PKB alpha | 94 | 11 |
| PKB beta |
3
|
1 |
| PKC alpha | 90 | 0 |
| PKC gamma | 115 | 10 |
| PKC zeta | 84 | 10 |
| PKD1 |
5
|
0 |
| PLK1 | 111 | 1 |
| PRAK | 65 | 11 |
| PRK2 | 19 | 1 |
| RIPK2 | 79 | 1 |
| ROCK 2 | 51 | 1 |
| RSK1 |
2
|
2 |
| RSK2 | 81 | 1 |
| S6K1 | 94 | 8 |
| SGK1 | 90 | 13 |
| SmMLCK |
10
|
5 |
| Src | 66 | 14 |
| SRPK1 | 46 | 5 |
| STK33 | 66 | 0 |
| SYK | 92 | 10 |
| TAK1 | 55 | 1 |
| TAO1 | 53 | 2 |
| TBK1 | 30 | 1 |
| TESK1 | 93 | 9 |
| TIE2 | 84 | 4 |
| TLK1 | 90 | 11 |
| TrkA | 71 | 4 |
| TSSK1 | 12 | 3 |
| TTBK1 | 93 | 5 |
| TTK | 79 | 7 |
| VEGFR1 | 68 | 1 |
| YES1 | 76 | 12 |
| ZAP70 | 109 | 1 |