Assay Detail
Binding
CHEMBL3418221
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant ERAP2 expressed in baculovirus infected cabbage looper ovary Hi5 cells using L-arginyl-7-amido-4-methyl coumarin as substrate after 5 to 10 mins by fluorescence assay
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Female gonad |
| Cell Type | BTI-TN-5B1-4 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Endoplasmic reticulum aminopeptidase 2 (CHEMBL5043) ↗| 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 | 60 | 5.24 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3416733 | — | — | 1 | 7.96 |
| CHEMBL3416727 | — | — | 1 | 6.62 |
| CHEMBL3416696 | — | — | 1 | 6.29 |
| CHEMBL3416697 | — | — | 1 | 6.23 |
| CHEMBL3416726 | — | — | 1 | 6.15 |
| CHEMBL3416725 | — | — | 1 | 6.12 |
| CHEMBL3416730 | — | — | 1 | 5.96 |
| CHEMBL3416701 | — | — | 1 | 5.96 |
| CHEMBL3416729 | — | — | 1 | 5.85 |
| CHEMBL3416692 | — | — | 1 | 5.80 |
| CHEMBL3416706 | — | — | 1 | 5.72 |
| CHEMBL3416583 | — | — | 1 | 5.68 |
| CHEMBL3416702 | — | — | 1 | 5.60 |
| CHEMBL3416694 | — | — | 1 | 5.60 |
| CHEMBL3416577 | — | — | 1 | 5.58 |
| CHEMBL3416567 | — | — | 1 | 5.50 |
| CHEMBL3416573 | — | — | 1 | 5.43 |
| CHEMBL3416693 | — | — | 1 | 5.42 |
| CHEMBL3416578 | — | — | 1 | 5.35 |
| CHEMBL3416717 | — | — | 1 | 5.32 |
| CHEMBL3416579 | — | — | 1 | 5.32 |
| CHEMBL3416695 | — | — | 1 | 5.30 |
| CHEMBL3416711 | — | — | 1 | 5.26 |
| CHEMBL3416723 | — | — | 1 | 5.21 |
| CHEMBL3416691 | — | — | 1 | 5.19 |
| CHEMBL3416584 | — | — | 1 | 5.08 |
| CHEMBL3416720 | — | — | 1 | 5.03 |
| CHEMBL3416572 | — | — | 1 | 5.01 |
| CHEMBL3416712 | — | — | 1 | 4.96 |
| CHEMBL3416731 | — | — | 1 | 4.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3416733 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3416727 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL3416696 | — | IC50 | = | 518.0 | nM | 6.29 |
| CHEMBL3416697 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL3416726 | — | IC50 | = | 709.0 | nM | 6.15 |
| CHEMBL3416725 | — | IC50 | = | 755.0 | nM | 6.12 |
| CHEMBL3416730 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3416701 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3416729 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3416692 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3416706 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3416583 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3416702 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3416694 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3416577 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3416567 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL3416573 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3416693 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3416578 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3416717 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3416579 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3416695 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3416711 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3416723 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3416691 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL3416584 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL3416720 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3416572 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL3416712 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3416731 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL3416713 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL3416580 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3416715 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL3416714 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3416585 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3416716 | — | IC50 | = | 20500.0 | nM | 4.69 |
| CHEMBL3416721 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3416728 | — | IC50 | = | 30600.0 | nM | 4.51 |
| CHEMBL3416588 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3416724 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL3416589 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3416685 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3416586 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3416582 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL3416699 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL3414595 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL3416719 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL3416574 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416566 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3416718 | — | IC50 | > | 100000.0 | nM | - |