Assay Detail
Binding
CHEMBL4262256
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Inhibition of recombinant human DAGLalpha expressed in HEK293 cells using PNP-butyrate as substrate pretreated for 20 to 30 mins followed by substrate addition measured every 60 secs for 20 mins by colorimetric method
23
Total Activities
23
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 |
Publication
Chiral disubstituted piperidinyl ureas: a class of dual diacylglycerol lipase-α and ABHD6 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.59 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3906477 | — | — | 1 | 9.10 |
| CHEMBL4279328 | — | — | 1 | 9.10 |
| CHEMBL4294845 | — | — | 1 | 7.80 |
| CHEMBL4287766 | — | — | 1 | 7.80 |
| CHEMBL4281906 | — | — | 1 | 7.80 |
| CHEMBL4284689 | — | — | 1 | 7.60 |
| CHEMBL4281842 | — | — | 1 | 7.60 |
| CHEMBL4289572 | — | — | 1 | 7.60 |
| CHEMBL4277989 | — | — | 1 | 7.50 |
| CHEMBL3934441 | — | — | 1 | 7.40 |
| CHEMBL4279884 | — | — | 1 | 7.10 |
| CHEMBL4291201 | — | — | 1 | 7.10 |
| CHEMBL4288486 | — | — | 1 | 6.80 |
| CHEMBL4289712 | — | — | 1 | 5.90 |
| CHEMBL4283505 | — | — | 1 | - |
| CHEMBL4294085 | — | — | 1 | - |
| CHEMBL4290683 | — | — | 1 | - |
| CHEMBL4286853 | — | — | 1 | - |
| CHEMBL4278939 | — | — | 1 | - |
| CHEMBL4276750 | — | — | 1 | - |
| CHEMBL4277826 | — | — | 1 | - |
| CHEMBL4278232 | — | — | 1 | - |
| CHEMBL4290942 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3906477 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4279328 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4294845 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4287766 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4281906 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4284689 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4281842 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4289572 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4277989 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3934441 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4279884 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4291201 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4288486 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4289712 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4283505 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4294085 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4290683 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4286853 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4278939 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4276750 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4277826 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4278232 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4290942 | — | IC50 | > | 10000.0 | nM | - |