Assay Detail
Binding
CHEMBL1787846
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Inhibition of catalytic activity of recombinant human IRAP 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
16
Total Activities
16
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 | 16 | 6.81 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782887 | — | — | 1 | 8.74 |
| CHEMBL1782881 | — | — | 1 | 8.39 |
| CHEMBL1277437 | — | — | 1 | 7.70 |
| CHEMBL1782882 | — | — | 1 | 7.60 |
| CHEMBL1782888 | — | — | 1 | 7.52 |
| CHEMBL1782886 | — | — | 1 | 7.39 |
| CHEMBL1782885 | — | — | 1 | 7.30 |
| CHEMBL261120 | ANGIOTENSIN IV | — | 1 | 7.21 |
| CHEMBL1782883 | — | — | 1 | 7.19 |
| CHEMBL1782884 | — | — | 1 | 6.71 |
| CHEMBL1782890 | — | — | 1 | 6.46 |
| CHEMBL1782889 | — | — | 1 | 6.16 |
| CHEMBL1782869 | — | — | 1 | 5.40 |
| CHEMBL1782891 | — | — | 1 | 5.23 |
| CHEMBL1782893 | — | — | 1 | 4.97 |
| CHEMBL1782892 | — | — | 1 | 4.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782887 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1782881 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL1277437 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1782882 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL1782888 | — | Ki | = | 30.4 | nM | 7.52 |
| CHEMBL1782886 | — | Ki | = | 41.1 | nM | 7.39 |
| CHEMBL1782885 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL261120 | ANGIOTENSIN IV | Ki | = | 62.4 | nM | 7.21 |
| CHEMBL1782883 | — | Ki | = | 64.2 | nM | 7.19 |
| CHEMBL1782884 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL1782890 | — | Ki | = | 351.0 | nM | 6.46 |
| CHEMBL1782889 | — | Ki | = | 697.0 | nM | 6.16 |
| CHEMBL1782869 | — | Ki | = | 4011.0 | nM | 5.40 |
| CHEMBL1782891 | — | Ki | = | 5845.0 | nM | 5.23 |
| CHEMBL1782893 | — | Ki | = | 10800.0 | nM | 4.97 |
| CHEMBL1782892 | — | Ki | = | 12000.0 | nM | 4.92 |