Table 1 Inhibition constants (Ki) of RYM and GM 6001.
From: Novel Arginine-containing Macrocyclic MMP Inhibitors: Synthesis, 99mTc-labeling, and Evaluation
Ki* (nM) | rhMMP-2 | rhMMP-7 | rhMMP-9 | rhMMP-12 | rhMMP-13 | TACE |
---|---|---|---|---|---|---|
RYM | 5.8 ± 0.4 | 17.2 ± 0.1 | 20.4 ± 2.0 | 1.0 ± 0.5 | 15.3 ± 5.4 | 4.9 ± 1.3 |
GM-6001 | 0.5 ± 0.1 | 0.4 ± 0.0 | 1.2 ± 0.0 | 0.6 ± 0.0 | 0.3 ± 0.0 | 113.1 ± 4.1 |