Assay Detail
Binding
CHEMBL1913590
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Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat brain homogenates after 90 mins by liquid scintillation spectrometry
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationship studies in translocator protein ligands based on a pyrazolo[3,4-b]quinoline scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.56 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1911623 | — | — | 1 | 9.89 |
| CHEMBL1911624 | — | — | 1 | 9.89 |
| CHEMBL1911620 | — | — | 1 | 9.85 |
| CHEMBL1911625 | — | — | 1 | 9.55 |
| CHEMBL1911622 | — | — | 1 | 9.47 |
| CHEMBL1911621 | — | — | 1 | 9.08 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.89 |
| CHEMBL1911606 | — | — | 1 | 8.74 |
| CHEMBL1911616 | — | — | 1 | 8.17 |
| CHEMBL1911619 | — | — | 1 | 7.80 |
| CHEMBL1911607 | — | — | 1 | 7.77 |
| CHEMBL1911600 | — | — | 1 | 7.19 |
| CHEMBL1911615 | — | — | 1 | 7.06 |
| CHEMBL1911603 | — | — | 1 | 7.05 |
| CHEMBL1911618 | — | — | 1 | 7.05 |
| CHEMBL1911613 | — | — | 1 | 6.96 |
| CHEMBL1911605 | — | — | 1 | 6.93 |
| CHEMBL1911617 | — | — | 1 | 6.84 |
| CHEMBL1911604 | — | — | 1 | 6.82 |
| CHEMBL1911601 | — | — | 1 | 6.75 |
| CHEMBL1911609 | — | — | 1 | 6.66 |
| CHEMBL1911610 | — | — | 1 | 6.52 |
| CHEMBL1911611 | — | — | 1 | 6.16 |
| CHEMBL1911608 | — | — | 1 | 6.05 |
| CHEMBL1911602 | — | — | 1 | 5.86 |
| CHEMBL1911614 | — | — | 1 | 5.64 |
| CHEMBL1911612 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1911623 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL1911624 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL1911620 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL1911625 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL1911622 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL1911621 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL481537 | PK-11195 | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1911606 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1911616 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1911619 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1911607 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1911600 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1911615 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1911603 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1911618 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1911613 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1911605 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL1911617 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL1911604 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL1911601 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1911609 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1911610 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL1911611 | — | IC50 | = | 697.0 | nM | 6.16 |
| CHEMBL1911608 | — | IC50 | = | 881.0 | nM | 6.05 |
| CHEMBL1911602 | — | IC50 | = | 1392.0 | nM | 5.86 |
| CHEMBL1911614 | — | IC50 | = | 2271.0 | nM | 5.64 |
| CHEMBL1911612 | — | IC50 | = | 3464.0 | nM | 5.46 |