| Assay Method Information | |
| | IDUA Inhibitory Assay |
| Description: | The compounds of Example 1 were evaluated on their inhibitory potential against rh-α-IDUA, and their apparent IC50 values were determined by using the fluorogenic substrates 4-methylumbelliferyl-α-iduronide (4-MU-IdoA) and results are shown in Table 1. CIdoA analogues 27a-c with IC50 values in low-micromolar range proved more potent than CIdoADNJ analogues 28a-c, most of which were inactive at 250 μM except 28c. Satisfyingly, a significant reduction of IC50 from 6.7 μM (12) to 1.0 μM (27c) indicated that the conjugation of negatively-charged phosphate group with certain orientation improved the inhibitory potency and then furnished 27c as the most potent IDUA inhibitors in the present disclosure. |
| Affinity data for this assay | |
|---|---|
| If you find an error in this entry please send us an E-mail | |