Assay Detail
Binding
CHEMBL2421059
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Sprague Dawley rat lung native NAAA enzyme using heptadecenoylethanolamide as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by UPLC-MS analysis
30
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
N-acylethanolamine-hydrolyzing acid amidase (CHEMBL2034805) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and structure-activity relationship (SAR) of 2-methyl-4-oxo-3-oxetanylcarbamic acid esters, a class of potent N-acylethanolamine acid amidase (NAAA) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.72 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2419814 | — | — | 1 | 8.15 |
| CHEMBL2419830 | — | — | 1 | 7.89 |
| CHEMBL2419811 | — | — | 1 | 7.80 |
| CHEMBL2419808 | — | — | 3 | 7.75 |
| CHEMBL2419819 | — | — | 1 | 7.70 |
| CHEMBL2419827 | — | — | 1 | 7.52 |
| CHEMBL2419826 | — | — | 1 | 7.40 |
| CHEMBL2064166 | — | — | 1 | 7.30 |
| CHEMBL2419828 | — | — | 1 | 7.30 |
| CHEMBL2419810 | — | — | 1 | 7.22 |
| CHEMBL2419807 | — | — | 3 | 7.10 |
| CHEMBL2419821 | — | — | 1 | 7.05 |
| CHEMBL2419829 | — | — | 1 | 6.85 |
| CHEMBL2419825 | — | — | 1 | 6.57 |
| CHEMBL2419812 | — | — | 1 | 6.57 |
| CHEMBL2417575 | — | — | 1 | 6.54 |
| CHEMBL2419809 | — | — | 1 | 6.51 |
| CHEMBL2419815 | — | — | 1 | 6.51 |
| CHEMBL2419822 | — | — | 1 | 6.41 |
| CHEMBL2419818 | — | — | 1 | 6.32 |
| CHEMBL2419824 | — | — | 1 | 6.12 |
| CHEMBL2419823 | — | — | 1 | 5.93 |
| CHEMBL2419820 | — | — | 1 | 5.60 |
| CHEMBL2419817 | — | — | 1 | 5.45 |
| CHEMBL2419813 | — | — | 1 | 4.64 |
| CHEMBL2419816 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2419814 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2419830 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2419811 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2419808 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2419819 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2419808 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2419827 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2419826 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2064166 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2419828 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL2419810 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2419807 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2419821 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2419807 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2419829 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2419812 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2419825 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2417575 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL2419815 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2419809 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2419822 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2419818 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2419824 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2419823 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL2419820 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2419817 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL2419808 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2419807 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL2419813 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL2419816 | — | IC50 | - | — | - |