Assay Detail
Binding
CHEMBL3887426
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biological Assay: Assay Method 1: T84 frozen pellets (contents of 1-4x15 cm culture dishes) were homogenized in 300 mL of FAAH assay buffer (125 mM Tris, 1 mM EDTA, 0.2% glycerol, 0.02% Triton X-100, 0.4 mM Hepes, pH 9). The assay mixture was prepared from 50 uL of the cell homogenate, 10 uL of the test compound, and 40 uL of anandamide [1-3H-ethanolamine] (3H-AEA; Perkin-Elmer, 10.3 Ci/mmol), which was added last, for a final tracer concentration of 200 nM. The reaction mixture was incubated at rt for 1 hour (h). During the incubation, 96-well Multiscreen filter plates (catalog number MAFCNOB50; Millipore, Bedford, Mass., USA) were loaded with 25 uL of activated charcoal (Multiscreen column loader, catalog number MACL09625, Millipore) and washed once with 100 uL of MeOH. Also during the incubation, 96-well DYNEX MicroLite plates (catalog number NL510410) were loaded with 100 uL of MicroScint40 (catalog number 6013641, Packard Bioscience, Meriden, Conn., USA).
135
Total Activities
131
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Piperazinyl and piperidinyl ureas as modulators of fatty acid amide hydrolase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 135 | 6.55 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164599 | — | — | 1 | 8.05 |
| CHEMBL2164596 | — | — | 1 | 8.05 |
| CHEMBL3949650 | — | — | 1 | 7.77 |
| CHEMBL2164598 | — | — | 1 | 7.75 |
| CHEMBL513789 | — | — | 2 | 7.72 |
| CHEMBL3958959 | — | — | 1 | 7.72 |
| CHEMBL3919995 | — | — | 1 | 7.72 |
| CHEMBL3939594 | — | — | 1 | 7.70 |
| CHEMBL3924088 | — | — | 1 | 7.68 |
| CHEMBL3944389 | — | — | 1 | 7.68 |
| CHEMBL3939432 | — | — | 1 | 7.66 |
| CHEMBL3934803 | — | — | 1 | 7.64 |
| CHEMBL3984894 | — | — | 1 | 7.62 |
| CHEMBL3950263 | — | — | 1 | 7.58 |
| CHEMBL3911047 | — | — | 1 | 7.57 |
| CHEMBL3961548 | — | — | 1 | 7.55 |
| CHEMBL3913379 | — | — | 1 | 7.54 |
| CHEMBL3927945 | — | — | 2 | 7.51 |
| CHEMBL3968643 | — | — | 1 | 7.50 |
| CHEMBL3982333 | — | — | 1 | 7.48 |
| CHEMBL3978604 | — | — | 1 | 7.32 |
| CHEMBL3983408 | — | — | 1 | 7.30 |
| CHEMBL3904461 | — | — | 1 | 7.28 |
| CHEMBL3981728 | — | — | 1 | 7.27 |
| CHEMBL3978478 | — | — | 1 | 7.24 |
| CHEMBL3935727 | — | — | 1 | 7.23 |
| CHEMBL3952197 | — | — | 1 | 7.21 |
| CHEMBL3913585 | — | — | 1 | 7.19 |
| CHEMBL3922585 | — | — | 1 | 7.17 |
| CHEMBL3966689 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164596 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2164599 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3949650 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2164598 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL513789 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3919995 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3958959 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3939594 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3944389 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3924088 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3939432 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL513789 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3934803 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3984894 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3950263 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3911047 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3961548 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3913379 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3927945 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3968643 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3982333 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3927945 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3978604 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3983408 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3904461 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3981728 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3978478 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3935727 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3952197 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3913585 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3922585 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3966689 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2164600 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3922544 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3968976 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2164605 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2164594 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3929968 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3891017 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3952351 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3958799 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3956448 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3951775 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3944835 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3976425 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3936942 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3910058 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3944804 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3905681 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3925659 | — | IC50 | = | 160.0 | nM | 6.80 |