| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3239893 | B | Inhibition of IDE in mouse Min6 cells assessed as effect on 2.8 mM of glucose-induced insulin secretion at 10 uM after 24 hrs by ELISA | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 2. | ALA3239894 | B | Inhibition of IDE in mouse Min6 cells assessed as effect on 11 mM of glucose-induced insulin secretion at 10 uM after 24 hrs by ELISA | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 3. | ALA3239895 | B | Inhibition of IDE in mouse Min6 cells assessed as effect on 20 mM of glucose-induced insulin secretion at 10 uM after 24 hrs by ELISA | Mus musculus | 1 | cell-based format | Scientific Literature | ||
| 4. | ALA3888053 | B | IDE Activity Assay: Macrocycles were assayed for IDE inhibition by monitoring cleavage of a substrate peptide containing a fluorophore-quencher pair such that cleavage of the model substrate results in increased fluorescence. Although our selection did not explicitly select for inhibition (only binding is required for enrichment), all four strongly enriched macrocycles inhibited IDE activity with IC50<10uM or equal to 10uM. The most potent macrocycle, trans-A12-B8-C6-D5 (6b), inhibited IDE with an IC50 of 140 nM. The three-dimensional conformation adopted by these compounds appears to be important to their inhibitory activity, as the trans-olefin isomers of macrocycles 3, 5, and 6 exhibit >10-fold stronger potency than the corresponding cis-olefin macrocycle isomers (Table 1). Compounds 1 and 4, which contained glycine (A2) instead of D-benzoylphenylalanine (A12) at the A position were inactive against IDE. | 2 | single protein format | BindingDB Database | |||
| 5. | ALA4200947 | B | Inhibition of mouse His-tagged IDE (42 to 1019 residues) using fluorophore/quencher-tagged RPPGFSAFK(Dnp)-OH peptide as substrate preincubated for 10 mins followed by substrate addition measured over 5 mins by TR-FRET assay | Mus musculus | 14 | single protein format | Scientific Literature | ||
| 6. | ALA4399075 | B | Inhibition of N-terminal His6-tagged mouse recombinant IDE Escherichia coli BL21 (DE3) cells using fluorogenic peptide Mca-RPPGFSAFK(Dnp)-OH as substrate by FRET assay | Mus musculus | 1 | assay format | Scientific Literature |
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