Assay Detail
Binding
CHEMBL5055347
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Displacement of [3H]PI-2620 from Tau in human brain homogenate incubated for 60 mins by radioligand binding assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Microtubule-associated protein tau (CHEMBL1293224) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-activity relationship around PI-2620 highlights the importance of the nitrogen atom position in the tricyclic core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.24 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5084771 | — | — | 1 | 8.51 |
| CHEMBL5082735 | — | — | 1 | 8.46 |
| CHEMBL5088921 | — | — | 1 | 8.31 |
| CHEMBL5081662 | — | — | 1 | 7.81 |
| CHEMBL5091624 | — | — | 1 | 7.75 |
| CHEMBL5084917 | — | — | 1 | 7.44 |
| CHEMBL5083649 | — | — | 1 | 7.16 |
| CHEMBL5077904 | — | — | 1 | 7.09 |
| CHEMBL5090407 | — | — | 1 | 6.94 |
| CHEMBL5080178 | — | — | 1 | 6.58 |
| CHEMBL5081126 | — | — | 1 | 6.51 |
| CHEMBL5081957 | — | — | 1 | 6.46 |
| CHEMBL5094590 | — | — | 1 | 6.25 |
| CHEMBL5092563 | — | — | 1 | 6.13 |
| CHEMBL5091757 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5084771 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5082735 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5088921 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5081662 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5091624 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5084917 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5083649 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5077904 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL5090407 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL5080178 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5081126 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5081957 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL5094590 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL5092563 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL5091757 | — | IC50 | > | 1000.0 | nM | - |