Assay Detail
Binding
CHEMBL4427014
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Inhibition human DAGLalpha expressed in HEK293T cell membrane fractions using DAG as substrate preincubated for 30 mins followed by ABP HT01 probe addition measured after 30 mins in presence of probe by gel-based ABPP competition assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Inhibitors of diacylglycerol lipases in neurodegenerative and metabolic disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.46 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4581240 | — | — | 1 | 9.30 |
| CHEMBL3895863 | — | — | 1 | 8.90 |
| CHEMBL2136920 | — | — | 1 | 6.90 |
| CHEMBL4476210 | — | — | 1 | 6.60 |
| CHEMBL2144065 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4581240 | — | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL3895863 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL2136920 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4476210 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL2144065 | — | IC50 | = | 2511.89 | nM | 5.60 |