Assay Detail
Binding
CHEMBL4385276
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Inhibition of recombinant human HL expressed in COS7 cells using PED-A1 containing DMPG vesicles as substrate pretreated for 20 mins followed by substrate addition and measured every 20 secs for 10 mins by fluorescence assay
16
Total Activities
15
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
Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.01 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL175247 | ORLISTAT | 4.0 | 1 | 8.52 |
| CHEMBL4440746 | — | — | 1 | 8.00 |
| CHEMBL4468090 | — | — | 1 | 7.68 |
| CHEMBL4536805 | — | — | 1 | 7.28 |
| CHEMBL4471545 | — | — | 1 | 7.28 |
| CHEMBL4473964 | — | — | 1 | 7.05 |
| CHEMBL4435864 | — | — | 1 | 6.92 |
| CHEMBL4577903 | — | — | 1 | 6.41 |
| CHEMBL4563513 | — | — | 1 | 6.35 |
| CHEMBL4516251 | — | — | 2 | 5.85 |
| CHEMBL4546575 | — | — | 1 | - |
| CHEMBL4567596 | — | — | 1 | - |
| CHEMBL4473238 | — | — | 1 | - |
| CHEMBL4589925 | — | — | 1 | - |
| CHEMBL4458141 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL175247 | ORLISTAT | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4440746 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4468090 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4536805 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4471545 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4473964 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4435864 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4577903 | — | IC50 | = | 391.0 | nM | 6.41 |
| CHEMBL4563513 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4516251 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4516251 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4546575 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4567596 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4473238 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4589925 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL4458141 | — | IC50 | < | 10.0 | nM | - |