Assay Detail
Functional
CHEMBL903636
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at LPA1 receptor in rat hepatic stellate cells assessed as inhibition of lysophosphatidic acid-induced intracellular calcium influx
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Lysophosphatidic acid receptor 1 (CHEMBL4595) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.12 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247959 | — | — | 1 | 7.54 |
| CHEMBL246929 | — | — | 1 | 7.32 |
| CHEMBL246943 | — | — | 1 | 7.25 |
| CHEMBL246735 | — | — | 1 | 7.14 |
| CHEMBL246527 | — | — | 1 | 7.14 |
| CHEMBL245295 | — | — | 1 | 7.13 |
| CHEMBL246928 | — | — | 1 | 7.09 |
| CHEMBL246942 | — | — | 1 | 7.00 |
| CHEMBL394038 | — | — | 1 | 6.96 |
| CHEMBL246734 | — | — | 1 | 6.92 |
| CHEMBL361501 | — | — | 1 | 6.80 |
| CHEMBL245895 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247959 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL246929 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL246943 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL246735 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL246527 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL245295 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL246928 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL246942 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL394038 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL246734 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL361501 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL245895 | — | IC50 | > | 20000.0 | nM | - |