| Compound name | Brutto | MW | CAS | PubChem CID | Action | Reference | Reference |
|---|---|---|---|---|---|---|---|
| PCI-32765 (Ibrutinib) | C25H24N6O2 | 440.50 | 936563-96-1 | 24821094 | Btk | Honigberg L.A. (2010) Proc Natl Acad Sci 107 13075-13080 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| ABL | 87 | 13 |
| AMPK | 88 | 4 |
| ASK1 | 103 | 1 |
| Aurora A | 92 | 0 |
| Aurora B | 96 | 13 |
| BRK |
10
|
3 |
| BRSK1 | 81 | 23 |
| BRSK2 | 100 | 9 |
| BTK | 55 | 3 |
| CAMK1 | 80 | 13 |
| CAMKK beta | 86 | 5 |
| CDK2-Cyclin A | 89 | 5 |
| CHK1 | 76 | 9 |
| CHK2 | 92 | 8 |
| CK1 delta | 98 | 5 |
| CK2 | 104 | 15 |
| CLK2 | 96 | 15 |
| CSK | 25 | 6 |
| DAPK1 | 95 | 4 |
| DYRK1A | 112 | 8 |
| DYRK2 | 83 | 1 |
| DYRK3 | 93 | 8 |
| EF2K | 88 | 0 |
| EIF2AK3 | 110 | 13 |
| EPH-A2 | 91 | 10 |
| EPH-A4 | 97 | 20 |
| EPH-B1 | 72 | 4 |
| EPH-B2 | 102 | 10 |
| EPH-B3 | 99 | 3 |
| EPH-B4 | 83 | 9 |
| ERK1 | 83 | 8 |
| ERK2 | 94 | 7 |
| ERK8 | 85 | 3 |
| FGF-R1 | 52 | 8 |
| GCK | 98 | 5 |
| GSK3 beta | 104 | 17 |
| HER4 |
7
|
0 |
| HIPK1 | 75 | 4 |
| HIPK2 | 91 | 11 |
| HIPK3 | 100 | 12 |
| IGF-1R | 95 | 0 |
| IKK beta | 94 | 4 |
| IKK epsilon | 100 | 4 |
| IR | 77 | 3 |
| IRAK1 | 108 | 7 |
| IRAK4 | 103 | 12 |
| IRR | 94 | 3 |
| JAK2 | 90 | 2 |
| JNK1 | 98 | 6 |
| JNK2 | 89 | 9 |
| JNK3 | 84 | 7 |
| Lck | 22 | 1 |
| LKB1 | 106 | 5 |
| MAPKAP-K2 | 88 | 5 |
| MAPKAP-K3 | 109 | 5 |
| MARK1 | 101 | 14 |
| MARK2 | 88 | 11 |
| MARK3 | 98 | 11 |
| MARK4 | 111 | 1 |
| MEKK1 | 106 | 6 |
| MELK | 69 | 5 |
| MINK1 | 90 | 0 |
| MKK1 | 85 | 2 |
| MKK2 | 94 | 1 |
| MKK6 | 82 | 0 |
| MLK1 | 104 | 7 |
| MLK3 | 87 | 0 |
| MNK1 | 91 | 17 |
| MNK2 | 106 | 9 |
| MPSK1 | 99 | 2 |
| MSK1 | 94 | 6 |
| MST2 | 88 | 3 |
| MST4 | 100 | 10 |
| NEK2a | 93 | 6 |
| NEK6 | 76 | 11 |
| NUAK1 | 99 | 10 |
| OSR1 | 96 | 1 |
| p38 alpha MAPK | 99 | 1 |
| p38 beta MAPK | 94 | 20 |
| p38 delta MAPK | 88 | 9 |
| p38 gamma MAPK | 89 | 9 |
| PAK2 | 87 | 1 |
| PAK4 | 93 | 10 |
| PAK5 | 93 | 13 |
| PAK6 | 95 | 3 |
| PDK1 | 93 | 8 |
| PHK | 116 | 34 |
| PIM1 | 98 | 2 |
| PIM2 | 99 | 1 |
| PIM3 | 94 | 4 |
| PKA | 89 | 1 |
| PKB alpha | 79 | 10 |
| PKB beta | 80 | 4 |
| PKC alpha | 99 | 8 |
| PKC gamma | 85 | 0 |
| PKC zeta | 90 | 10 |
| PKD1 | 64 | 16 |
| PLK1 | 88 | 13 |
| PRAK | 101 | 8 |
| PRK2 | 109 | 9 |
| RIPK2 | 21 | 1 |
| ROCK 2 | 93 | 3 |
| RSK1 | 94 | 12 |
| RSK2 | 103 | 6 |
| S6K1 | 93 | 4 |
| SGK1 | 95 | 7 |
| SmMLCK | 79 | 1 |
| Src | 37 | 4 |
| SRPK1 | 100 | 9 |
| STK33 | 97 | 2 |
| SYK | 90 | 7 |
| TAK1 | 102 | 10 |
| TAO1 | 113 | 5 |
| TBK1 | 102 | 3 |
| TESK1 | 69 | 9 |
| TIE2 | 71 | 10 |
| TLK1 | 96 | 12 |
| TrkA | 64 | 9 |
| TSSK1 | 105 | 2 |
| TTBK1 | 78 | 5 |
| TTK | 95 | 1 |
| VEGFR1 | 40 | 3 |
| YES1 | 20 | 0 |
| ZAP70 | 93 | 16 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| ABL | 80 | 1 |
| AMPK | 101 | 7 |
| ASK1 | 128 | 1 |
| Aurora A | 57 | 2 |
| Aurora B | 61 | 7 |
| BRK |
4
|
1 |
| BRSK1 | 80 | 28 |
| BRSK2 | 91 | 2 |
| BTK | 55 | 1 |
| CAMK1 | 99 | 12 |
| CAMKK beta | 109 | 5 |
| CDK2-Cyclin A | 99 | 10 |
| CHK1 | 93 | 9 |
| CHK2 | 77 | 6 |
| CK1 delta | 111 | 8 |
| CK2 | 115 | 7 |
| CLK2 | 95 | 9 |
| CSK | 15 | 13 |
| DAPK1 | 95 | 15 |
| DYRK1A | 105 | 8 |
| DYRK2 | 105 | 9 |
| DYRK3 | 86 | 14 |
| EF2K | 102 | 21 |
| EIF2AK3 | 81 | 5 |
| EPH-A2 | 98 | 9 |
| EPH-A4 | 92 | 13 |
| EPH-B1 | 90 | 9 |
| EPH-B2 | 65 | 0 |
| EPH-B3 | 96 | 5 |
| EPH-B4 | 74 | 0 |
| ERK1 | 93 | 21 |
| ERK2 | 99 | 0 |
| ERK8 | 98 | 6 |
| FGF-R1 | 24 | 1 |
| GCK | 77 | 6 |
| GSK3 beta | 95 | 6 |
| HER4 |
8
|
1 |
| HIPK1 | 87 | 2 |
| HIPK2 | 91 | 14 |
| HIPK3 | 123 | 4 |
| IGF-1R | 93 | 1 |
| IKK beta | 107 | 6 |
| IKK epsilon | 95 | 19 |
| IR | 99 | 10 |
| IRAK1 | 115 | 3 |
| IRAK4 | 102 | 9 |
| IRR | 101 | 0 |
| JAK2 | 103 | 2 |
| JNK1 | 98 | 7 |
| JNK2 | 101 | 3 |
| JNK3 | 96 | 5 |
| Lck | 14 | 2 |
| LKB1 | 134 | 43 |
| MAPKAP-K2 | 95 | 9 |
| MAPKAP-K3 | 109 | 0 |
| MARK1 | 103 | 12 |
| MARK2 | 102 | 6 |
| MARK3 | 94 | 3 |
| MARK4 | 114 | 5 |
| MEKK1 | 103 | 17 |
| MELK | 105 | 37 |
| MINK1 | 91 | 4 |
| MKK1 | 76 | 3 |
| MKK2 | 94 | 6 |
| MKK6 | 97 | 1 |
| MLK1 | 89 | 5 |
| MLK3 | 65 | 5 |
| MNK1 | 115 | 14 |
| MNK2 | 82 | 21 |
| MPSK1 | 117 | 9 |
| MSK1 | 101 | 6 |
| MST2 | 65 | 2 |
| MST4 | 73 | 4 |
| NEK2a | 107 | 12 |
| NEK6 | 99 | 9 |
| NUAK1 | 82 | 8 |
| OSR1 | 96 | 4 |
| p38 alpha MAPK | 103 | 3 |
| p38 beta MAPK | 103 | 8 |
| p38 delta MAPK | 104 | 14 |
| p38 gamma MAPK | 112 | 1 |
| PAK2 | 72 | 4 |
| PAK4 | 85 | 9 |
| PAK5 | 97 | 2 |
| PAK6 | 97 | 3 |
| PDK1 | 124 | 14 |
| PHK | 104 | 10 |
| PIM1 | 95 | 1 |
| PIM2 | 100 | 17 |
| PIM3 | 96 | 12 |
| PKA | 101 | 0 |
| PKB alpha | 97 | 1 |
| PKB beta | 93 | 7 |
| PKC alpha | 106 | 21 |
| PKC gamma | 104 | 14 |
| PKC zeta | 98 | 1 |
| PKD1 | 69 | 7 |
| PLK1 | 95 | 3 |
| PRAK | 107 | 6 |
| PRK2 | 100 | 9 |
| RIPK2 |
5
|
0 |
| ROCK 2 | 111 | 3 |
| RSK1 | 101 | 6 |
| RSK2 | 106 | 19 |
| S6K1 | 86 | 8 |
| SGK1 | 107 | 0 |
| SmMLCK | 90 | 1 |
| Src | 13 | 1 |
| SRPK1 | 115 | 8 |
| STK33 | 84 | 10 |
| SYK | 100 | 4 |
| TAK1 | 106 | 13 |
| TAO1 | 119 | 1 |
| TBK1 | 113 | 4 |
| TESK1 | 71 | 14 |
| TIE2 | 34 | 4 |
| TLK1 | 99 | 2 |
| TrkA | 46 | 1 |
| TSSK1 | 108 | 4 |
| TTBK1 | 100 | 9 |
| TTK | 101 | 3 |
| VEGFR1 |
7
|
1 |
| YES1 | 16 | 0 |
| ZAP70 | 107 | 5 |
| Kinase | % Activity Remaining | Standard Deviation |
|---|---|---|
| ABL | 39 | 2 |
| AMPK | 78 | 1 |
| ASK1 | 111 | 6 |
| Aurora A |
10
|
1 |
| Aurora B | 13 | 1 |
| BRK |
8
|
5 |
| BRSK1 | 49 | 11 |
| BRSK2 | 61 | 12 |
| BTK | 42 | 4 |
| CAMK1 | 33 | 8 |
| CAMKK beta | 80 | 3 |
| CDK2-Cyclin A | 84 | 6 |
| CHK1 | 77 | 0 |
| CHK2 | 35 | 9 |
| CK1 delta | 115 | 15 |
| CK2 | 111 | 10 |
| CLK2 | 71 | 10 |
| CSK |
3
|
0 |
| DAPK1 | 84 | 5 |
| DYRK1A | 87 | 1 |
| DYRK2 | 79 | 2 |
| DYRK3 | 68 | 5 |
| EF2K | 90 | 6 |
| EIF2AK3 | 28 | 2 |
| EPH-A2 | 64 | 5 |
| EPH-A4 | 45 | 1 |
| EPH-B1 | 86 | 2 |
| EPH-B2 | 11 | 1 |
| EPH-B3 | 51 | 2 |
| EPH-B4 | 39 | 0 |
| ERK1 | 84 | 7 |
| ERK2 | 90 | 12 |
| ERK8 | 74 | 1 |
| FGF-R1 | 15 | 2 |
| GCK | 38 | 0 |
| GSK3 beta | 75 | 9 |
| HER4 |
5
|
1 |
| HIPK1 | 75 | 14 |
| HIPK2 | 66 | 2 |
| HIPK3 | 110 | 8 |
| IGF-1R | 63 | 19 |
| IKK beta | 90 | 12 |
| IKK epsilon | 66 | 15 |
| IR | 31 | 11 |
| IRAK1 | 98 | 32 |
| IRAK4 | 86 | 3 |
| IRR | 29 | 5 |
| JAK2 | 83 | 13 |
| JNK1 | 75 | 1 |
| JNK2 | 123 | 29 |
| JNK3 | 86 | 2 |
| Lck |
9
|
3 |
| LKB1 | 100 | 0 |
| MAPKAP-K2 | 90 | 1 |
| MAPKAP-K3 | 75 | 20 |
| MARK1 | 88 | 11 |
| MARK2 | 82 | 7 |
| MARK3 | 76 | 14 |
| MARK4 | 80 | 6 |
| MEKK1 | 56 | 4 |
| MELK | 56 | 18 |
| MINK1 | 57 | 3 |
| MKK1 | 56 | 3 |
| MKK2 | 63 | 2 |
| MKK6 | 61 | 12 |
| MLK1 | 27 | 18 |
| MLK3 | 28 | 5 |
| MNK1 | 84 | 6 |
| MNK2 | 67 | 4 |
| MPSK1 | 104 | 7 |
| MSK1 | 55 | 6 |
| MST2 | 41 | 9 |
| MST4 | 27 | 6 |
| NEK2a | 35 | 2 |
| NEK6 | 93 | 12 |
| NUAK1 | 26 | 13 |
| OSR1 | 82 | 9 |
| p38 alpha MAPK | 101 | 8 |
| p38 beta MAPK | 68 | 4 |
| p38 delta MAPK | 80 | 3 |
| p38 gamma MAPK | 88 | 10 |
| PAK2 | 55 | 4 |
| PAK4 | 42 | 6 |
| PAK5 | 50 | 3 |
| PAK6 | 82 | 3 |
| PDK1 | 102 | 14 |
| PHK | 92 | 7 |
| PIM1 | 81 | 3 |
| PIM2 | 97 | 15 |
| PIM3 | 88 | 4 |
| PKA | 97 | 11 |
| PKB alpha | 78 | 1 |
| PKB beta | 71 | 4 |
| PKC alpha | 100 | 12 |
| PKC gamma | 99 | 5 |
| PKC zeta | 81 | 3 |
| PKD1 | 30 | 6 |
| PLK1 | 76 | 3 |
| PRAK | 83 | 11 |
| PRK2 | 90 | 2 |
| RIPK2 |
2
|
0 |
| ROCK 2 | 69 | 6 |
| RSK1 | 46 | 5 |
| RSK2 | 68 | 7 |
| S6K1 | 66 | 1 |
| SGK1 | 84 | 1 |
| SmMLCK | 44 | 6 |
| Src |
6
|
4 |
| SRPK1 | 99 | 0 |
| STK33 | 113 | 101 |
| SYK | 52 | 6 |
| TAK1 | 66 | 4 |
| TAO1 | 84 | 1 |
| TBK1 | 90 | 7 |
| TESK1 | 38 | 8 |
| TIE2 |
9
|
1 |
| TLK1 | 96 | 6 |
| TrkA | 13 | 7 |
| TSSK1 | 68 | 5 |
| TTBK1 | 81 | 11 |
| TTK | 82 | 9 |
| VEGFR1 |
2
|
1 |
| YES1 | 13 | 0 |
| ZAP70 | 101 | 10 |