Assay Detail
Functional
CHEMBL903635
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human recombinant LPA1 receptor expressed in CHOK1 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 | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.63 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL246942 | — | — | 1 | 6.89 |
| CHEMBL247959 | — | — | 1 | 6.89 |
| CHEMBL246735 | — | — | 1 | 6.85 |
| CHEMBL246943 | — | — | 1 | 6.77 |
| CHEMBL246527 | — | — | 1 | 6.70 |
| CHEMBL246929 | — | — | 1 | 6.66 |
| CHEMBL246928 | — | — | 1 | 6.58 |
| CHEMBL394038 | — | — | 1 | 6.55 |
| CHEMBL246734 | — | — | 1 | 6.43 |
| CHEMBL245295 | — | — | 1 | 6.37 |
| CHEMBL361501 | — | — | 1 | 6.29 |
| CHEMBL245895 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL246942 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL247959 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL246735 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL246943 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL246527 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL246929 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL246928 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL394038 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL246734 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL245295 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL361501 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL245895 | — | IC50 | > | 40000.0 | nM | - |