Table 3.
Experimental activities of PTPN1 inhibitors across different classical PTPs.
Molecule | PTPN2 | PTPN1 | PTPRC | PTPRF | PTPN6 | PTPRB | PTPRE | PTPRA | |
---|---|---|---|---|---|---|---|---|---|
![]() |
a1 | 1.3 | 3.2 | 280 | >500 | - | - | - | - |
![]() |
a2 | 0.026 | 0.036 | 151 | >1000 | - | - | - | - |
![]() |
b1 | 1 | 1.6 | 64 | >1000 | - | - | - | - |
![]() |
b2 | 0.68 | 0.82 | 55 | 320 | - | - | - | - |
![]() |
b3 | 0.32 | 0.3 | 26 | >1000 | - | - | - | - |
![]() |
b4 | 0.18 | 0.14 | 33 | >1000 | - | - | - | - |
![]() |
c1 | 4.1 | 9.2 | >1250 | 1100 | - | - | - | - |
![]() |
d1 | - | 23 | 160 | >2000 | 510 | 33 | 130 | 870 |
![]() |
d2 | - | 9.9 | 37 | 68 | 94 | 14 | 45 | 190 |
![]() |
d3 | - | 14 | 56 | 550 | 16 | 6 | 66 | 800 |
![]() |
d4 | - | 8 | 20 | 450 | 28 | 3.6 | 33 | 180 |
![]() |
d5 | - | 14 | 49 | 420 | 84 | 17 | 33 | 89 |
![]() |
e1 | - | 58 | 260 | >2000 | >2000 | 160 | 360 | >2000 |
![]() |
e2 | - | 62 | 210 | >2000 | 60 | 18 | 740 | 1700 |
![]() |
e3 | - | 8.1 | 41 | 410 | 100 | 19 | 45 | 290 |
![]() |
e4 | - | 0.29 | 59 | >2000 | >2000 | 560 | 1100 | >2000 |
![]() |
e5 | - | 14 | 53 | 360 | 350 | 11 | 20 | 170 |
![]() |
f1 | 1.1 | 0.6 | 489 | 176 | 289 | 21 | >500 | >500 |
Activity given as inhibition constant Ki in µM.