Assay Detail
Binding
CHEMBL3772811
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NAAA expressed in HEK293 cells preincubated for 10 mins followed by N-(4-methyl-2-oxo-chromen-7-yl)-hexadecanamide substrate addition for 50 mins by fluorescence assay
46
Total Activities
46
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 |
Target
N-acylethanolamine-hydrolyzing acid amidase (CHEMBL4349) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 6.20 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770896 | — | — | 1 | 7.64 |
| CHEMBL3769844 | — | — | 1 | 7.48 |
| CHEMBL3770558 | — | — | 1 | 7.43 |
| CHEMBL3770525 | — | — | 1 | 7.39 |
| CHEMBL3769455 | — | — | 1 | 7.36 |
| CHEMBL3770490 | — | — | 1 | 7.31 |
| CHEMBL3770240 | — | — | 1 | 7.28 |
| CHEMBL3770567 | — | — | 1 | 7.15 |
| CHEMBL3769639 | — | — | 1 | 7.14 |
| CHEMBL3770726 | — | — | 1 | 7.14 |
| CHEMBL3771111 | — | — | 1 | 7.07 |
| CHEMBL3770640 | — | — | 1 | 6.91 |
| CHEMBL3771169 | — | — | 1 | 6.89 |
| CHEMBL3771196 | — | — | 1 | 6.85 |
| CHEMBL3769452 | — | — | 1 | 6.80 |
| CHEMBL3770354 | — | — | 1 | 6.64 |
| CHEMBL3770695 | — | — | 1 | 6.62 |
| CHEMBL3769689 | — | — | 1 | 6.60 |
| CHEMBL3770549 | — | — | 1 | 6.53 |
| CHEMBL3769597 | — | — | 1 | 6.51 |
| CHEMBL3770519 | — | — | 1 | 6.49 |
| CHEMBL3769678 | — | — | 1 | 6.48 |
| CHEMBL3770031 | — | — | 1 | 6.29 |
| CHEMBL3770722 | — | — | 1 | 6.28 |
| CHEMBL3770915 | — | — | 1 | 5.98 |
| CHEMBL3769700 | — | — | 1 | 5.96 |
| CHEMBL3770450 | — | — | 1 | 5.89 |
| CHEMBL3770901 | — | — | 1 | 5.86 |
| CHEMBL3771259 | — | — | 1 | 5.82 |
| CHEMBL3771368 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770896 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3769844 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3770558 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3770525 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3769455 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3770490 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3770240 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3770567 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3769639 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3770726 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3771111 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3770640 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3771169 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3771196 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3769452 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3770354 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3770695 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3769689 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3770549 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL3769597 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3770519 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL3769678 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3770031 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL3770722 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3770915 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3769700 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL3770450 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL3770901 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL3771259 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL3771368 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL3769409 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL3769503 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL3770849 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL3770547 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL3770146 | — | IC50 | = | 2890.0 | nM | 5.54 |
| CHEMBL3770250 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL3770090 | — | IC50 | = | 4470.0 | nM | 5.35 |
| CHEMBL3769770 | — | IC50 | = | 8110.0 | nM | 5.09 |
| CHEMBL3769763 | — | IC50 | = | 9510.0 | nM | 5.02 |
| CHEMBL3771160 | — | IC50 | = | 12910.0 | nM | 4.89 |
| CHEMBL3769976 | — | IC50 | = | 12830.0 | nM | 4.89 |
| CHEMBL3769863 | — | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL3771292 | — | IC50 | = | 25420.0 | nM | 4.59 |
| CHEMBL3771358 | — | IC50 | = | 29360.0 | nM | 4.53 |
| CHEMBL3771150 | — | IC50 | = | 30650.0 | nM | 4.51 |
| CHEMBL3770388 | — | IC50 | > | 50000.0 | nM | - |