Assay Detail
Binding
CHEMBL2344993
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Agonist activity at human LPA6 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425
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 | 6.94 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2335052 | — | — | 2 | 7.41 |
| CHEMBL153043 | — | — | 2 | 7.24 |
| CHEMBL2335049 | — | — | 2 | 7.18 |
| CHEMBL2335051 | — | — | 2 | 7.12 |
| CHEMBL2335050 | — | — | 2 | 7.11 |
| CHEMBL357053 | — | — | 2 | 7.10 |
| CHEMBL2017139 | — | — | 2 | 7.07 |
| CHEMBL2335047 | — | — | 2 | 7.05 |
| CHEMBL2335048 | — | — | 2 | 6.98 |
| CHEMBL364797 | — | — | 2 | 6.03 |
| CHEMBL117021 | LYSOPHOSPHATIDIC ACID | — | 2 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2335052 | — | EC50 | = | 38.9 | nM | 7.41 |
| CHEMBL2335052 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL153043 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL153043 | — | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL2335049 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2335049 | — | EC50 | = | 66.07 | nM | 7.18 |
| CHEMBL2335051 | — | EC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2335051 | — | EC50 | = | 75.86 | nM | 7.12 |
| CHEMBL2335050 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2335050 | — | EC50 | = | 77.62 | nM | 7.11 |
| CHEMBL357053 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL357053 | — | EC50 | = | 79.43 | nM | 7.10 |
| CHEMBL2017139 | — | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2017139 | — | EC50 | = | 85.11 | nM | 7.07 |
| CHEMBL2335047 | — | EC50 | = | 89.13 | nM | 7.05 |
| CHEMBL2335047 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2335048 | — | EC50 | = | 104.71 | nM | 6.98 |
| CHEMBL2335048 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL364797 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL364797 | — | EC50 | = | 933.25 | nM | 6.03 |
| CHEMBL117021 | LYSOPHOSPHATIDIC ACID | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL117021 | LYSOPHOSPHATIDIC ACID | EC50 | = | 977.24 | nM | 6.01 |