Table 2. CPL302-253 interactions with human kinome.
CPL302-253 binding to a human kinome was assessed in KINOMEScan assay at 1 μM. The numbers represent % of the remaining binding of specific ligand to kinase in competitive binding assay with CPL302-253. The table includes targets with remaining binding lower than 40% and PI3K isoforms.
| Gene symbol | Remaining binding (%) |
|---|---|
| PIK3CA(H1047Y) | 0 |
| PIK3CD | 1.1 |
| PIK3CA(C420R) | 12 |
| ULK2 | 33 |
| MEK5 | 35 |
| ABL1-nonphosphorylated | 36 |
| PIK3CB | 42 |
| PIK3CA(I800L) | 44 |
| PIK3CA(E545A) | 45 |
| PIK3CA(E545K) | 54 |
| PIK3CA(E542K) | 82 |
| PIK3CA(H1047L) | 92 |
| PIK3CG | 94 |
| PIK3CA | 96 |
| PIK3CA(Q546K) | 99 |
| PIK3CA(M1043I) | 100 |