| Assay Method Information | |
| | Inhibition of ATX by Benzene Sulfonamide Series |
| Description: | Compound 3b was found to be the most potent ATX inhibitor with an IC50 of about 9 nM. The mechanism of action was determined to be competitive; however the traditional measure of a competitive inhibitor may not be appropriately applied in this context. 3b inhibited hydrolysis of the lipid-like substrate FS-3 while sparing effects on hydrolysis of the nucleotide substrate pNP-TMP. As such and with the observed molecular modeling it is known that 3b does not bind at the active site, in which case both substrates would be affected. However, because the compound is targeted toward the hydrophobic pocket of ATX, it shares space with the binding site for the hydrophobic tail of lipid substrates like FS-3. As such, the mechanism of action presents itself as competitive in the FS-3 hydrolysis assay even though the binding site of the 3b exists outside the catalytic site of the enzyme. |
| Affinity data for this assay | |
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