Assay Detail
Functional
CHEMBL5362071
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Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay
22
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293-A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Probable G-protein coupled receptor 34 (CHEMBL1075291) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Exploration of LPS<sub>2</sub> agonist binding modes using the combination of a new hydrophobic scaffold and homology modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 6.35 | 6.75 |
| pEC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5410755 | — | — | 2 | 6.75 |
| CHEMBL4072692 | — | — | 2 | 6.66 |
| CHEMBL1742484 | — | — | 2 | 6.54 |
| CHEMBL5398282 | — | — | 2 | 6.02 |
| CHEMBL5393782 | — | — | 2 | 5.80 |
| CHEMBL5404040 | — | — | 2 | - |
| CHEMBL5394475 | — | — | 2 | - |
| CHEMBL4099594 | — | — | 2 | - |
| CHEMBL5432264 | — | — | 2 | - |
| CHEMBL5398524 | — | — | 2 | - |
| CHEMBL5428143 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5410755 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5410755 | — | EC50 | = | 177.83 | nM | 6.75 |
| CHEMBL4072692 | — | EC50 | = | 218.78 | nM | 6.66 |
| CHEMBL4072692 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1742484 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1742484 | — | EC50 | = | 295.12 | nM | 6.53 |
| CHEMBL5398282 | — | EC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5398282 | — | EC50 | = | 954.99 | nM | 6.02 |
| CHEMBL5393782 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5393782 | — | EC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL5404040 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL5428143 | — | pEC50 | - | — | - | |
| CHEMBL5398524 | — | EC50 | < | 3162.28 | nM | - |
| CHEMBL5432264 | — | EC50 | < | 3162.28 | nM | - |
| CHEMBL4099594 | — | EC50 | < | 3162.28 | nM | - |
| CHEMBL5394475 | — | EC50 | < | 3162.28 | nM | - |
| CHEMBL5404040 | — | EC50 | < | 3162.28 | nM | - |
| CHEMBL5394475 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL4099594 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL5428143 | — | EC50 | - | — | - | |
| CHEMBL5398524 | — | EC50 | > | 3000.0 | nM | - |
| CHEMBL5432264 | — | EC50 | > | 3000.0 | nM | - |