Assay Detail
Functional
CHEMBL3859969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human LPA1 receptor expressed in CHO cells assessed as reduction in LPA-induced intracellular Ca2+ concentration pretreated with compound followed by LPA addition by fluorescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.54 | 8.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3975893 | — | — | 1 | 8.46 |
| CHEMBL3976876 | — | — | 1 | 8.23 |
| CHEMBL3917128 | — | — | 1 | 7.82 |
| CHEMBL3947597 | — | — | 1 | 7.38 |
| CHEMBL3971582 | — | — | 1 | 7.15 |
| CHEMBL272087 | — | — | 1 | 7.05 |
| CHEMBL3956307 | — | — | 1 | 7.00 |
| CHEMBL3986868 | — | — | 1 | 7.00 |
| CHEMBL3932828 | — | — | 1 | 6.89 |
| CHEMBL3984953 | — | — | 1 | 6.85 |
| CHEMBL3956293 | — | — | 1 | 6.85 |
| CHEMBL3941037 | — | — | 1 | 6.80 |
| CHEMBL3901754 | — | — | 1 | 6.72 |
| CHEMBL3959223 | — | — | 1 | 6.68 |
| CHEMBL3944344 | — | — | 1 | 6.66 |
| CHEMBL3896148 | — | — | 1 | 6.64 |
| CHEMBL3890162 | — | — | 1 | 6.58 |
| CHEMBL3930834 | — | — | 1 | 6.58 |
| CHEMBL3950523 | — | — | 1 | 6.41 |
| CHEMBL3913038 | — | — | 1 | 6.17 |
| CHEMBL3915800 | — | — | 1 | 5.89 |
| CHEMBL3902849 | — | — | 1 | 5.77 |
| CHEMBL3912909 | — | — | 1 | 5.48 |
| CHEMBL3979511 | — | — | 1 | 5.43 |
| CHEMBL3903904 | — | — | 1 | 5.36 |
| CHEMBL3921894 | — | — | 1 | 5.26 |
| CHEMBL3953068 | — | — | 1 | 5.18 |
| CHEMBL3959003 | — | — | 1 | 4.92 |
| CHEMBL3973793 | — | — | 1 | - |
| CHEMBL3981813 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3975893 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3976876 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3917128 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3947597 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3971582 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL272087 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3956307 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3986868 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3932828 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3984953 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3956293 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3941037 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3901754 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3959223 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3944344 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3896148 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3890162 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3930834 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3950523 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3913038 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL3915800 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3902849 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3912909 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3979511 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3903904 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL3921894 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3953068 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3959003 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL3973793 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3981813 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3905099 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3972833 | — | IC50 | > | 1000.0 | nM | - |