Assay Detail
Binding
CHEMBL3418219
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ERAP1 expressed in baculovirus infected Sf9 cells using L-leucine-7-amido-4-methyl coumarin as substrate after 5 to 10 mins by fluorescence assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Endoplasmic reticulum aminopeptidase 1 (CHEMBL5939) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
3,4-diaminobenzoic acid derivatives as inhibitors of the oxytocinase subfamily of M1 aminopeptidases with immune-regulating properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 5.22 | 7.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416733 | — | — | 1 | 7.48 |
| CHEMBL3416720 | — | — | 1 | 6.10 |
| CHEMBL3416692 | — | — | 1 | 6.04 |
| CHEMBL3416716 | — | — | 1 | 5.96 |
| CHEMBL3416697 | — | — | 1 | 5.92 |
| CHEMBL3416726 | — | — | 1 | 5.60 |
| CHEMBL3416729 | — | — | 1 | 5.58 |
| CHEMBL3416727 | — | — | 1 | 5.55 |
| CHEMBL3416693 | — | — | 1 | 5.44 |
| CHEMBL3416583 | — | — | 1 | 5.17 |
| CHEMBL3416721 | — | — | 1 | 5.05 |
| CHEMBL3416711 | — | — | 1 | 5.03 |
| CHEMBL3416696 | — | — | 1 | 5.02 |
| CHEMBL3416685 | — | — | 1 | 5.01 |
| CHEMBL3416694 | — | — | 1 | 4.97 |
| CHEMBL3416713 | — | — | 1 | 4.92 |
| CHEMBL3416686 | — | — | 1 | 4.92 |
| CHEMBL3416712 | — | — | 1 | 4.87 |
| CHEMBL3416715 | — | — | 1 | 4.78 |
| CHEMBL3416584 | — | — | 1 | 4.74 |
| CHEMBL3416717 | — | — | 1 | 4.71 |
| CHEMBL3416707 | — | — | 1 | 4.46 |
| CHEMBL3416688 | — | — | 1 | 4.42 |
| CHEMBL3416730 | — | — | 1 | 4.42 |
| CHEMBL3416585 | — | — | 1 | 4.38 |
| CHEMBL3416723 | — | — | 1 | - |
| CHEMBL3416725 | — | — | 1 | - |
| CHEMBL3416572 | — | — | 1 | - |
| CHEMBL3416718 | — | — | 1 | - |
| CHEMBL3416569 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416733 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3416720 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3416692 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3416716 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3416697 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3416726 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3416729 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3416727 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3416693 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL3416583 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3416721 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL3416711 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3416696 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3416685 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3416694 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL3416713 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3416686 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL3416712 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL3416715 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL3416584 | — | IC50 | = | 18300.0 | nM | 4.74 |
| CHEMBL3416717 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL3416707 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL3416688 | — | IC50 | = | 38400.0 | nM | 4.42 |
| CHEMBL3416730 | — | IC50 | = | 38200.0 | nM | 4.42 |
| CHEMBL3416585 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL3416588 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL3416589 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416687 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416689 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416691 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416580 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416567 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3414595 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416703 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416706 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416579 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416569 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416718 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416572 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416725 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416723 | — | IC50 | > | 100000.0 | nM | - |