Assay Detail
Functional
CHEMBL2184752
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Antagonist activity at LPA1 in human lung fibroblasts assessed as inhibition of LPA-induced contraction after 18 hrs by 3D collagen gel contraction assay
12
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of highly selective and orally active lysophosphatidic acid receptor-1 antagonists with potent activity on human lung fibroblasts.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.03 | 7.70 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2182044 | — | — | 1 | 7.70 |
| CHEMBL2182043 | — | — | 1 | 7.70 |
| CHEMBL2182063 | — | — | 1 | 7.70 |
| CHEMBL2182029 | — | — | 2 | 7.00 |
| CHEMBL2182052 | — | — | 1 | 6.82 |
| CHEMBL361501 | — | — | 1 | 6.80 |
| CHEMBL2182051 | — | — | 1 | 6.66 |
| CHEMBL2182046 | — | — | 1 | 6.47 |
| CHEMBL2182042 | — | — | 1 | 6.41 |
| CHEMBL2182050 | — | — | 1 | - |
| CHEMBL256470 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2182044 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2182043 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2182063 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2182029 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2182052 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL361501 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2182051 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2182046 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2182042 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL2182029 | — | Inhibition | - | % | - | |
| CHEMBL2182050 | — | Inhibition | - | % | - | |
| CHEMBL256470 | — | Inhibition | - | % | - |