Assay Detail
Binding
CHEMBL2379575
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FAAH in Sprague-Dawley rat brain microsomes assessed as N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide conversion to 4-pyren-1-ylbutanoic acid preincubated for 10 mins measured after 45 mins by HPLC analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.59 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL175854 | — | — | 1 | 8.40 |
| CHEMBL2376224 | — | — | 1 | 8.30 |
| CHEMBL509860 | — | — | 1 | 8.30 |
| CHEMBL2376208 | — | — | 1 | 8.22 |
| CHEMBL2376210 | — | — | 1 | 8.15 |
| CHEMBL2376226 | — | — | 1 | 8.10 |
| CHEMBL2376209 | — | — | 1 | 8.05 |
| CHEMBL2376199 | — | — | 1 | 8.05 |
| CHEMBL2376220 | — | — | 1 | 8.05 |
| CHEMBL2376225 | — | — | 1 | 8.05 |
| CHEMBL2376219 | — | — | 1 | 8.00 |
| CHEMBL2376223 | — | — | 1 | 7.96 |
| CHEMBL2376228 | — | — | 1 | 7.96 |
| CHEMBL2376202 | — | — | 1 | 7.96 |
| CHEMBL485841 | — | — | 1 | 7.92 |
| CHEMBL2376211 | — | — | 1 | 7.92 |
| CHEMBL2376227 | — | — | 1 | 7.92 |
| CHEMBL2376221 | — | — | 1 | 7.89 |
| CHEMBL2376218 | — | — | 1 | 7.89 |
| CHEMBL2376215 | — | — | 1 | 7.85 |
| CHEMBL2376222 | — | — | 1 | 7.82 |
| CHEMBL2376200 | — | — | 1 | 7.80 |
| CHEMBL2376216 | — | — | 1 | 7.80 |
| CHEMBL2376217 | — | — | 1 | 7.62 |
| CHEMBL2376201 | — | — | 1 | 7.54 |
| CHEMBL2376204 | — | — | 1 | 7.43 |
| CHEMBL2376203 | — | — | 1 | 7.40 |
| CHEMBL184238 | URB-597 | 1.0 | 1 | 7.21 |
| CHEMBL2376198 | — | — | 1 | 7.06 |
| CHEMBL2376229 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL175854 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2376224 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL509860 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2376208 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2376210 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2376226 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2376209 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2376199 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2376220 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2376225 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2376219 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2376223 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2376228 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2376202 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2376227 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL485841 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2376211 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2376218 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2376221 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2376215 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2376222 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2376200 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2376216 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2376217 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2376201 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2376204 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2376203 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL184238 | URB-597 | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2376198 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2376229 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2171700 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL570812 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2376206 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL2376207 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL561924 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2376205 | — | IC50 | > | 10000.0 | nM | - |