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FR221647 is a small molecule, non-nucleoside inhibitor of human adenosine deaminase (ADA), with a Ki value of 5.9 μM. It was discovered through structure-based de novo design as a novel ADA inhibitor with moderate activity and favorable pharmacokinetics compared to known inhibitors such as pentostatin and EHNA. The compound is not cytotoxic at concentrations up to 100 μM. Its primary mechanism is the inhibition of adenosine deaminase, an enzyme involved in purine metabolism and immune regulation. FR221647 has been developed experimentally but has not advanced beyond preclinical or early clinical development[1][2][3].
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