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PF-06840003, also known as EOS200271, is potent IDO-1 inhibitor (IC50 0.15 μM). PF-0684000 has moderate hIDO1 enzyme inhibition (IC50 0.41 μM). It is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms with hIDO-1 despite its small size. PF-0684000 shows good potency in an IDO-1 human whole blood assay and also shows a very favorable ADME profile leading to favorable predicted human pharmacokinetic properties, including a predicted half-life of 16−19 h.