Assay Detail
Functional
CHEMBL5628569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human LPA1 receptor stably expressed in rat RH7777 cells assessed as reduction in LPA-induced intracellular Ca2+ concentration preincubated for 30 mins followed by LPA addition measured by Fluo-4 probe based fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RH7777 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lead generation from N-[benzyl(4-phenylbutyl)carbamoyl]amino acid as a novel LPA<sub>1</sub> antagonist for the treatment of systemic sclerosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.13 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5633614 | — | — | 1 | 8.80 |
| CHEMBL5632303 | — | — | 1 | 7.52 |
| CHEMBL5632315 | — | — | 1 | 7.29 |
| CHEMBL5632273 | — | — | 1 | 6.96 |
| CHEMBL5633770 | — | — | 1 | 6.33 |
| CHEMBL5633672 | — | — | 1 | 6.28 |
| CHEMBL5631989 | — | — | 1 | 6.23 |
| CHEMBL5633208 | — | — | 1 | 5.75 |
| CHEMBL5633075 | — | — | 1 | 5.67 |
| CHEMBL5632224 | — | — | 1 | 5.67 |
| CHEMBL5631605 | — | — | 1 | 5.56 |
| CHEMBL5634050 | — | — | 1 | 5.56 |
| CHEMBL5633162 | — | — | 1 | 5.46 |
| CHEMBL5633792 | — | — | 1 | 5.44 |
| CHEMBL5631516 | — | — | 1 | 5.31 |
| CHEMBL5633356 | — | — | 1 | 5.30 |
| CHEMBL5632524 | — | — | 1 | 5.06 |
| CHEMBL5633769 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5633614 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5632303 | — | IC50 | = | 30.1 | nM | 7.52 |
| CHEMBL5632315 | — | IC50 | = | 51.4 | nM | 7.29 |
| CHEMBL5632273 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5633770 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5633672 | — | IC50 | = | 521.0 | nM | 6.28 |
| CHEMBL5631989 | — | IC50 | = | 586.0 | nM | 6.23 |
| CHEMBL5633208 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL5633075 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL5632224 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL5631605 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL5634050 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL5633162 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL5633792 | — | IC50 | = | 3660.0 | nM | 5.44 |
| CHEMBL5631516 | — | IC50 | = | 4890.0 | nM | 5.31 |
| CHEMBL5633356 | — | IC50 | = | 5040.0 | nM | 5.30 |
| CHEMBL5632524 | — | IC50 | = | 8770.0 | nM | 5.06 |
| CHEMBL5633769 | — | IC50 | > | 10000.0 | nM | - |