Table 3. Inhibitors of Preferred Human Kinase Purchased and Tested against Protozoan Pathogens and Host Cells.
| T. brucei |
Leishmania |
T. cruzi |
P. falciparum |
host
cell tox |
||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| no. | compd | compd name | human kinase (pIC50) | pEC50 (within 46%) | Promast pEC50 | Amast pEC50 | pEC50 (μM) (within 21%) | D6 pEC50 | W2 pEC50 | C235 pEC50 | 3T3 pTC50 | HepG2 pTC50 |
| 1 | NEU-838 | crizotinib | ALK (7.6) |
6.4 | 6.2 | 5.8 | 5.1 | 6.1 | 7.4 | 7.0 | 4.8 | 5.4 |
| 2 | NEU-844 | TAE684 | ALK (8.5) |
7.0 | 6.5 | 5.9 | 5.3 | 6.3 | 6.4 | 6.3 | 4.6 | 5.3 |
| 3 | NEU-893 | GSK1838705A | ALK (9.3) |
5.7 | <4.6 | <4.8 | 5.0 | 5.6 | 5.8 | 5.8 | 4.8 | 5.1 |
| 4 | NEU-967 | NVP-AEW5414 | IGF-1R (6.8) |
5.7 | 7.0 | 5.4 | 5.4 | 5.9 | 6.0 | 5.9 | 4.8 | 5.5 |
| 5 | NEU-968 | BMS-2652465 | CDK1-cyclinB (8.2) | 6.3 | 6.6 | <4.8 | <4.3 | 4.8 | 5.0 | 4.9 | <4 | <4.4 |
| 6 | NEU-969 | PHA-8481256 | CDK2-cyclinA (7.3) | 7.6 | 6.5 | 5.3 | 7.4 | 5.2 | 5.1 | 5.2 | <4 | 5.0 |
| 7 | NEU-970 | GSK1904529A7 | IGF-1R (7.6) |
5.9 | <4.9 | 5.5 | <4.3 | 6.8 | 7.0 | 6.9 | <4 | <4.4 |
| 8 | NEU-971 | JNJ-77066218 | CDK2-cyclinE (8.5) | 6.5 | <4.6 | <4.8 | <4.3 | 5.7 | 6.0 | 5.9 | <4 | 5.2 |
| 9 | NEU-973 | ON-019109 | PLK1 (8.0) |
<5.5 | <4.6 | <4.8 | <4.3 | <4.7 | <4.7 | <4.7 | <4 | <4.4 |
| 10 | NEU-974 | CH542480210 | ALK (8.7) |
<5.5 | 6.9 | <4.8 | <4.3 | 5.4 | <4.7 | <4.7 | <4 | <4.4 |
| 11 | NEU-975 | dinaciclib | CDK2 (9.0) |
7.4 | 5.8 | 5.6 | 7.0 | 5.9 | 6.1 | 6.5 | <4 | <4.4 |
| P35/CDK5 (9.0) | ||||||||||||
| 12 | NEU-976 | linsitinib | IGF1R (7.5) |
<5.5 | 5.1 | <4.8 | 5.0 | 6.3 | 5.7 | 6.3 | <4 | 4.5 |
| 13 | NEU-977 | roscovitine 13 | P35/CDK5 (9.0) |
<5.5 | 5.2 | <4.8 | <4.3 | 6.1 | 5.7 | 5.7 | <4 | 4.5 |
| 14 | NEU-978 | CHIR-9801414 | GSK3α/β (9.2) |
<5.5 | 5.2 | <4.8 | <4.3 | <4.7 | <4.7 | <4.7 | <4 | 4.8 |
| 15 | NEU-979 | volasertib | PLK1 (9.1) |
<5.5 | 5.8 | 5.1 | 4.9 | 6.8 | 6.8 | 6.8 | 4.6 | 5.5 |
| 16 | NEU-980 | BI 253616 | PLK1 (9.1) |
6.2 | 5.4 | 5.1 | 4.7 | 7.7 | 8.0 | 7.9 | 4.5 | 5.6 |
| 17 | NEU-982 | AT751918 | p35/CDK5 (7.9) |
6.5 | <4.6 | <4.8 | 5.9 | 5.9 | 6.1 | 6.5 | <4 | <4.4 |
| 18 | NEU-984 | SNS-03219, 20 | CDK9/cyclinT (8.4) |
6.9 | <4.6 | <4.8 | < 4.3 | 5.3 | 5.5 | 5.7 | <4 | <4.4 |
| 19 | NEU-985 | AZD543821 | CDK2/cyclinE (8.2) |
7.5 | 6.4 | 5.6 | 5.8 | 5.9 | 6.0 | 5.9 | <4 | 4.9 |
| 20 | NEU-986 | SB 41528622 | GSK-3α (7.1) |
6.1 | <4.6 | <4.8 | <4.3 | 4.8 | 4.6 | 4.6 | 4.2 | <4.4 |
| 21 | NEU-987 | flavopiridol | CDK1/2/4/6 (7.4) |
6.8 | 6.4 | 5.5 | 4.9 | 5.7 | 5.7 | 5.8 | < 4 | < 4.4 |
| 22 | NEU-989 | TWS11925 | GSK-3β (7.5) |
6.0 | 4.7 | <4.8 | <4.3 | 5.0 | 4.7 | 5.1 | 4.4 | <4.4 |
| 23 | NEU-990 | SB 21676322 | GSK-3α (7.5) |
<5.5 | 5.6 | <4.8 | <4.3 | <4.7 | <4.7 | <4.7 | <4 | <4.4 |
| 24 | NEU-991 | tideglusib | GSK-3β (7.2) |
<5.5 | 6.5 | <4.8 | 4.7 | 4.6 | 4.6 | 4.7 | 4.1 | <4.4 |
| 25 | NEU-1007 | PHA-79388727 | p25/CDK5 (8.3) |
5.7 | <4.6 | <4.8 | <4.3 | 5.7 | 5.6 | 5.6 | <4 | <4.4 |
| 26 | NEU-1049 | harmine | DYRK1B (7.6) |
<5.5 | 5.9 | 5.9 | 4.8 | <4.7 | <4.7 | <4.7 | <4 | <5.1 |