Table 1.
Target Protein | Protein Class | Protein Mass (kDa) | Engineered/Native | Hit Rate (>3σ), % |
---|---|---|---|---|
ATG4B | Protease | 44.5 | Native | 0.1 |
Nativea | 1.4 | |||
Engineered | 1.5 | |||
Lfa1 | Integrin, I-domain | 21.0 | Engineeredb | 1.8 |
Engineeredb | 1.6 | |||
Mac1 | Integrin, I-domain | 22.8 | Engineeredb | 2.6 |
Engineeredb | 2.3 | |||
LRH-1c,d | Nuclear receptor | 28.3 | Native | 0.7 |
Target 1 | Ubiquitin ligase | 8.78 | Native | 1.4 |
Target 2 | Kinase | 19.3 | Native | 0.4 |
Target 3c | Kinase | 37.3 | Engineered | 0.6 |
14–3-3σ | Adapter protein | 26.5 | Native | 1.8 |
Engineeredb | 2.8 | |||
Engineeredb | 2.7 |
Screened in the presence of a protein partner.
Cys-mutants targeting the same pocket on a respective target.
Screened 1280 of 1600 compounds.
de Jesus Cortez et al.25