Assay Detail
Binding
CHEMBL2344997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human LPA1 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay
22
Total Activities
11
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
Phosphorothioate analogs of sn-2 radyl lysophosphatidic acid (LPA): metabolically stabilized LPA receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 7.74 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2335052 | — | — | 2 | 8.08 |
| CHEMBL2335047 | — | — | 2 | 8.00 |
| CHEMBL2335050 | — | — | 2 | 7.96 |
| CHEMBL2335051 | — | — | 2 | 7.91 |
| CHEMBL357053 | — | — | 2 | 7.83 |
| CHEMBL2017139 | — | — | 2 | 7.78 |
| CHEMBL117021 | LYSOPHOSPHATIDIC ACID | — | 2 | 7.75 |
| CHEMBL153043 | — | — | 2 | 7.62 |
| CHEMBL2335049 | — | — | 2 | 7.58 |
| CHEMBL2335048 | — | — | 2 | 7.51 |
| CHEMBL364797 | — | — | 2 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2335052 | — | EC50 | = | 8.318 | nM | 8.08 |
| CHEMBL2335052 | — | EC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2335047 | — | EC50 | = | 10.1 | nM | 8.00 |
| CHEMBL2335047 | — | EC50 | = | 10.23 | nM | 7.99 |
| CHEMBL2335050 | — | EC50 | = | 11.1 | nM | 7.96 |
| CHEMBL2335050 | — | EC50 | = | 11.22 | nM | 7.95 |
| CHEMBL2335051 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL2335051 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL357053 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL357053 | — | EC50 | = | 14.7 | nM | 7.83 |
| CHEMBL2017139 | — | EC50 | = | 16.5 | nM | 7.78 |
| CHEMBL2017139 | — | EC50 | = | 16.6 | nM | 7.78 |
| CHEMBL117021 | LYSOPHOSPHATIDIC ACID | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL117021 | LYSOPHOSPHATIDIC ACID | EC50 | = | 17.78 | nM | 7.75 |
| CHEMBL153043 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL153043 | — | EC50 | = | 23.99 | nM | 7.62 |
| CHEMBL2335049 | — | EC50 | = | 26.3 | nM | 7.58 |
| CHEMBL2335049 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2335048 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL2335048 | — | EC50 | = | 30.9 | nM | 7.51 |
| CHEMBL364797 | — | EC50 | = | 71.0 | nM | 7.15 |
| CHEMBL364797 | — | EC50 | = | 70.79 | nM | 7.15 |