TABLE 1.
Activities and categories of DDR inhibitors
| Target | Inhibitor | IC50 DDR1 | IC50 DDR2 | Category |
|---|---|---|---|---|
| Multi‐targeted kinase inhibitors | Imatinib 58 | 337 ± 56.0 nmol/L | 675.0 ± 127.0 nmol/L | Type‐II |
| Nilotinib 7 | 43.0 ± 3.0 nmol/L | 55.0 ± 9.0 nmol/L | Type‐II | |
| Dasatinib 56 | 0.5 ± 0.2 nmol/L | 1.4 ± 0.3 nmol/L | Type‐I | |
| ATP site kinase inhibitors | DDR1‐IN‐1 59 | 105.0 nmol/L | 413.0 nmol/L | Type‐II |
| DDR1‐IN‐259 | 47.0 nmol/L | 147.0 nmol/L | Type‐II | |
| Small molecular DDR inhibitors | 7rh 60 | 6.8 nmol/L | 101.4 nmol/L | Pyrazolopyrimidine derivatives |
| 7rj 60 | 7.0 nmol/L | 93.6 nmol/L | Pyrazolopyrimidine derivatives | |
| Compound 10 61 | 9.4 nmol/L | — | tetrahydroisoquinoline derivatives | |
| Compound 8v 14 | 23.8 nmol/L | — | 3′‐(imidazo[1,2‐a] pyrazin‐3‐yl)‐[1,1′‐biphenyl]‐3‐carboxamide | |
| Compound 23 63 | 97.0 nmol/L | — | Benzamide derivatives | |
| Compound 24 63 | 43.0 nmol/L | — | Benzamide derivatives | |
| DDR1 antibodies | 48B3 65 | 20 μg/mL | — | Monoclonal antibody |
| T4H11‐DM4 66 |
2.5 nM (HT‐29) 22.1 nmol/L (HCT116) >1 μmol/L (LoVo) |
— | Antibody‐drug conjugate | |
| AI‐designed DDR1 inhibitors | Compound 1 13 | 10.0 nmol/L | — | AI‐designed |
The bold types are inherent in the references.
Abbreviations: “‐”, not available; AI, artificial intelligence; ATP, adenosine triphosphate; DDR, discoidin domain receptor.