Table 3.
Selected small molecules with excellent kinase inhibition activity
Compounds | Chemical Structures | Targets | IC50 | References |
---|---|---|---|---|
1 | ![]() |
VEGFR-2 | 0.19 nM | 471 |
2 | ![]() |
VEGFR-2 | 2.6 nM | 472 |
3 | ![]() |
VEGFR-2 | 3.2 nM | 473 |
4 | ![]() |
VEGFR-2 | 3.2 nM | 474 |
5 | ![]() |
VEGFR-2 | 27 nM | 475 |
6 | ![]() |
VEGFR-2 | 66 nM | 476 |
7 | ![]() |
VEGFR-2 | 0.12 μM | 477 |
8 | ![]() |
VEGFR-2 | 0.12 μM | 478 |
9 | ![]() |
VEGFR-2 | 0.23 μM | 479 |
10 | ![]() |
VEGFR-2 | 0.29 μM | 480 |
11 | ![]() |
VEGFR-2 | 0.31 μM | 481 |
12 | ![]() |
VEGFR-2 PDGFR-β |
24.7 nM 16.1 nM |
481 |
13 | ![]() |
VEGFR-2 FGFR-1 PDGFR-β |
7 nM 69 nM 31 nM |
482 |
14 | ![]() |
VEGFR-2 FGFR-1 PDGFR-β |
0.18 μM 0.23 μM 0.1 μM |
481 |
15 | ![]() |
VEGFR-2 c-Met PDGFR-β |
435 nM 654 nM 371 nM |
481,483 |
16 | ![]() |
VEGFR-2 Tie-2 EphB4 |
1.05 nM 2.47 nM 0.27 nM |
484,485 |
17 | ![]() |
VEGFR-2 Tie-2 EphB4 |
1.85 nM 0.73 nM 2.99 nM |
486 |
18 | ![]() |
VEGFR-2 Tie-2 EphB4 |
2.35 nM 5.63 nM 3.87 nM |
487 |
19 | ![]() |
VEGFR-2 HDAC4 |
5 μM 0.36 μM |
488 |
20 | ![]() |
FGFR-4 | 5.4 nM | 489 |
21 | ![]() |
FGFR-1 FGFR-2 VEGFR-2 |
1.0 nM 4.5 nM 2.9 nM |
490 |
22 | ![]() |
FGFR-1 FGFR-2 FGFR-3 |
0.6 μM 1.3 μM 4.1 μM |
491 |
23 | ![]() |
HIF-1α | 0.6 μM | 492 |
24 | ![]() |
HIF-1α | 0.32 μM | 493 |
25 | ![]() |
HIF-1α | 0.6 μM | 494 |