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212 In 2010, a high-throughput screening campaign followed by structure–activity relationship (SAR) investigation led to the development of 9 (GKT136901), a pyrazolopyridinedione compound claimed to be a preferential inhibitor of NOX1 and NOX4 isoforms ( K i of 160 and 165 nM, respectively) compared to NOX2 ( K i of 1530 nM)