TABLE 1.
Modalities | ka | kd | KD | IC50 |
---|---|---|---|---|
m−1 s−1 | s−1 | nm | nm | |
IHVTIPADLWDWINK-NH2 (CVX5484) | 1.3 ± 0.2 × 105 | 1.32 ± 0.07 × 10−3 | 10 ± 2 | No activity |
PyrEIHVTIPADLWDWINK-NH2 | 1.7 ± 0.2 × 105 | 1.0 ± 0.2 × 10−3 | 6.0 ± 0.6 | 1.4 |
PyrEAIHVTIPADLWDWINK-NH2 | 1.3 ± 0.3 × 105 | 1.0 ± 0.2 × 10−3 | 8 ± 2 | 1.7 |
PyrEGIHVTIPADLWDWINK-NH2 | 1.5 ± 0.4 × 105 | 1.1 ± 0.2 × 10−3 | 7.2 ± 0.8 | 10 |
PyrEGGIHVTIPADLWDWINK-NH2 | 1.6 ± 0.3 × 105 | 1.1 ± 0.3 × 10−3 | 7 ± 2 | 2.4 |
Q-G6-HC | 2.5 ± 0.9 × 104 | 1.4 ± 0.2 × 10−3 | 60 ± 30 | 7.0 |
Q-GSE12-HC | 3.0 ± 1.0 × 104 | 1.9 ± 0.5 × 10− | 80 ± 70 | 12 |
Q-GSE21-HC | 1.84 ± 0.02 × 104 | 1.7 ± 0.3 × 10−3 | 100 ± 20 | >133 |
Q-GSE21-LC | 5.0 ± 3.0 × 103 | 1.9 ± 0.3 × 10−3 | 500 ± 300 | 18.4 |
Q-GSE21-LC-T5A | 2.2 ± 0.5 × 105 | 2.5 ± 0.5 × 10−4 | 1.2 ± 0.2 | 0.25 |