| Assay Method Information | |
| | Biochemical Evaluation |
| Description: | Table 1 and 2: The compounds were biochemically evaluated against a panel consisting of all enzymatically active DASH enzymes (DPP4, DPP8, DPP9, DPP2, FAP) and PREP. Potencies of the 2-cyanopyrrolidine-based compounds (5a-o) are shown in Table 1. The unsubstituted cyanopyrrolidine subset 5a-c comprises the closest analogues of vildagliptin that were synthesized. Compared to parent compound vildagliptin/4, the affinities of 5a-c are typically slightly increased across the full evaluation panel. Because of its generality, this trend can tentatively be attributed to the increased lipophilicity of the ether derivatives, compared to vildagliptin. This also indicates that the benzyl or butyl groups in these molecules are tolerated, but do not provide additional specific affinity-conferring interactions with the enzymes. |
| Affinity data for this assay | |
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