Assay Detail
Binding
CHEMBL1787847
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Inhibition of catalytic activity of recombinant human AP-N transfected in human HEK-293 cells assessed as cleavage of substrate L-leucine-p-nitroanilide to L-leucine and p-nitroaniline measured every 5 mins for 10 to 50 mins by spectrophotometric analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent macrocyclic inhibitors of insulin-regulated aminopeptidase (IRAP) by olefin ring-closing metathesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.58 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782887 | — | — | 1 | 6.62 |
| CHEMBL261120 | ANGIOTENSIN IV | — | 1 | 6.08 |
| CHEMBL1782885 | — | — | 1 | 5.97 |
| CHEMBL1782888 | — | — | 1 | 5.89 |
| CHEMBL1782889 | — | — | 1 | 5.80 |
| CHEMBL1782883 | — | — | 1 | 5.48 |
| CHEMBL1782881 | — | — | 1 | 5.30 |
| CHEMBL1782886 | — | — | 1 | 5.27 |
| CHEMBL1782884 | — | — | 1 | 5.08 |
| CHEMBL1782882 | — | — | 1 | 4.92 |
| CHEMBL1782890 | — | — | 1 | 4.92 |
| CHEMBL1782891 | — | — | 1 | - |
| CHEMBL1782869 | — | — | 1 | - |
| CHEMBL1782892 | — | — | 1 | - |
| CHEMBL1782893 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782887 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL261120 | ANGIOTENSIN IV | Ki | = | 841.0 | nM | 6.08 |
| CHEMBL1782885 | — | Ki | = | 1074.0 | nM | 5.97 |
| CHEMBL1782888 | — | Ki | = | 1299.0 | nM | 5.89 |
| CHEMBL1782889 | — | Ki | = | 1571.0 | nM | 5.80 |
| CHEMBL1782883 | — | Ki | = | 3283.0 | nM | 5.48 |
| CHEMBL1782881 | — | Ki | = | 4955.0 | nM | 5.30 |
| CHEMBL1782886 | — | Ki | = | 5413.0 | nM | 5.27 |
| CHEMBL1782884 | — | Ki | = | 8345.0 | nM | 5.08 |
| CHEMBL1782882 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL1782890 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL1782891 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1782869 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1782892 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1782893 | — | Ki | > | 100000.0 | nM | - |