Alanine scan on peptide Ac-K(N3)-RR-cyclo(c(methylene)PLYISYDPVC)-RR-NH2 (MP-1687)a.
| Compound | Modification | KRASG12D GDP TR-FRET EC50 (nM) |
|---|---|---|
| MP-1687 | None | 60 |
| 5 | Pro6Ala | >48 080 |
| 6 | Leu7Ala | >48 080 |
| 7 | Tyr8Ala | 691 |
| 8 | Ile9Ala | >48 080 |
| 9 | Ser10Ala | 1072 |
| 10 | Tyr11Ala | 2430 |
| 11 | Asp12Ala | >48 080 |
| 12 | Pro13Ala | 427 |
| 13 | Val14Ala | 161 |
| ||
a
The d-Cys5 residue and thioacetal linker is highlighted in red in the structure. The N- and C-termini are shown. MP-1687 has the same macrocyclic core as MP-6483, with only two arginine residues at each terminus.