Assay Detail
Binding
CHEMBL4880929
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Inhibition of Transporter, Adenosine at 10 µM in the Eurofins-Panlabs radioligand binding assay (Eurofins_assay_202000)
21
Total Activities
11
Compounds Tested
3
Activity Types
14
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Profiling data from Eurofins-Panlabs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 17 | - | - |
| IC50 | 2 | 5.40 | 5.79 |
| Ki | 2 | 5.87 | 6.26 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Assay protocol publication | Assay protocol publication | - | — | PMID: 3965849 |
| Detection method | Detection method | - | — | Radioligand Binding |
| Incubation temperature | Incubation temperature | - | — | 25 °C |
| Incubation time | Incubation time | - | — | 30 min |
| Ligand | Ligand | - | — | [3H] Nitrobenzylthioinosine |
| Ligand Bmax | Ligand Bmax | 0.24 | pM/ mg protein | — |
| Ligand concentration | Ligand concentration | 0.5 | nM | — |
| Ligand Kd | Ligand Kd | 0.26 | nM | — |
| Ligand specific binding | Ligand specific binding | 90.0 | % | — |
| Non-specific ligand with concentration | Non-specific ligand with concentration | - | — | 5 µM Nitrobenzylthioinosine |
| Reference compound | Reference compound | - | — | Nitrobenzylthioinosine |
| reference compound IC50 | reference compound IC50 | 0.85 | nM | — |
| reference compound Ki | reference compound Ki | 0.29 | nM | — |
| Source of protein | Source of protein | - | — | Duncan Hartley derived Guinea pig cerebral cortex |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204538 | THPP-1 | — | 6 | 6.26 |
| CHEMBL4098877 | MLi-2 | — | 6 | 5.48 |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4535474 | BAY-293 | — | 1 | - |
| CHEMBL1800685 | PPTN | — | 1 | - |
| CHEMBL4643852 | BAY-6672 | — | 1 | - |
| CHEMBL4514203 | BAY-390 | — | 1 | - |
| CHEMBL1800285 | MSD-M1PAM | — | 1 | - |
| CHEMBL5084426 | — | — | 1 | - |
| CHEMBL5410211 | — | — | 1 | - |
| CHEMBL4594444 | PECAVAPTAN | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204538 | THPP-1 | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL2204538 | THPP-1 | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL4098877 | MLi-2 | Ki | = | 3320.0 | nM | 5.48 |
| CHEMBL4098877 | MLi-2 | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4535474 | BAY-293 | Inhibition | = | 62.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | 51.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | 11.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | -1.0 | % | - |
| CHEMBL4098877 | MLi-2 | Inhibition | = | 2.0 | % | - |
| CHEMBL1800685 | PPTN | Inhibition | = | 9.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | 75.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | 40.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | 21.0 | % | - |
| CHEMBL2204538 | THPP-1 | Inhibition | = | -6.0 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 10.0 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | -2.0 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 2.0 | % | - |
| CHEMBL5084426 | — | Inhibition | = | 71.0 | % | - |
| CHEMBL5410211 | — | Inhibition | = | -2.2 | % | - |
| CHEMBL4537788 | BAY-784 | Inhibition | = | 25.0 | % | - |
| CHEMBL4594444 | PECAVAPTAN | Inhibition | = | 21.0 | % | - |