Table 3.
Summary of binding affinities and in vitro activity of cP4_4 and its variants where the fluoroacetimidoyl ornithine (FAO) warhead was replaced by arginine (Arg4), citrulline (Cit4), acetimidoyl ornithine (Me4) or chloroacetimidoyl ornithine (Cl4)
| SPR | COLDERS | |||||
|---|---|---|---|---|---|---|
| Ki (µM) | kinact (min-1) | kinact/Ki (M-1 min-1) | KD (µM) | IC50 (µM) T = 0 h | IC50 (µM) T = 1 h | |
| Arg4 | – | – | – | 2.0 ± 0.2 | >100 | |
| Cit4 | – | – | – | >10 | >100 | |
| Me4 | – | – | – | 1.7 ± 0.4 | >20 | |
| Cl4 | 4.0 ± 0.2 | 0.28 ± 0.02 | 70,000 | – | 8.2 ± 0.8 | 0.066 ± 0.009 |
| cP4_4 | 0.12 ± 0.01 | 0.11 ± 0.003 | 909,000 | – | 4.4 ± 0.07 | 0.070 ± 0.004 |
Surface plasmon resonance (SPR) data shows mean ± SEM of three independent replicates. COLDER data shows mean ± SEM of at least two independent replicates.