Assay Detail
Binding
CHEMBL2049774
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FAAH in rat brain membranes assessed as hydrolysis of [14C]-anandamide preincubated for 20 mins before [14C]-anandamide addition measured after 30 mins
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.65 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL184238 | URB-597 | 1.0 | 1 | 8.22 |
| CHEMBL2047530 | — | — | 1 | 7.40 |
| CHEMBL2047528 | — | — | 1 | 7.30 |
| CHEMBL336297 | — | — | 1 | 7.00 |
| CHEMBL2047527 | — | — | 1 | 6.96 |
| CHEMBL440526 | — | — | 1 | 6.77 |
| CHEMBL2047526 | — | — | 1 | 6.54 |
| CHEMBL128390 | — | — | 1 | 6.40 |
| CHEMBL128043 | — | — | 1 | 6.10 |
| CHEMBL130918 | — | — | 1 | 5.85 |
| CHEMBL2047529 | — | — | 1 | 5.74 |
| CHEMBL2047531 | — | — | 1 | 5.57 |
| CHEMBL2047525 | — | — | 1 | - |
| CHEMBL128551 | — | — | 1 | - |
| CHEMBL132110 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL184238 | URB-597 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2047530 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2047528 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL336297 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2047527 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL440526 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2047526 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL128390 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL128043 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL130918 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2047529 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL2047531 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL2047525 | — | IC50 | - | — | - | |
| CHEMBL128551 | — | IC50 | - | — | - | |
| CHEMBL132110 | — | IC50 | - | — | - |