Assay Detail
Binding
CHEMBL3889073
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Competitive Binding Assay: For tau imaging probes other than THK-5105, binding to K18-ΔK280 aggregates was evaluated with a competitive binding test using [18F] THK-5105 as a radioactive competitor. In the binding test, [18F] THK-5105 (at a final concentration of 1.76 nM) and a tested compound (at final concentrations of from 0.1 to 1000 nM) coexisted in the reaction system, to which K18-ΔK280 aggregates (at a final concentration of 200 nM) was then added and the mixtures were incubated at room temperature for one hour. The radioactivity of [18F] THK-5105 binding to the aggregates was determined in a similar way as in the saturation binding test of THK-5105. The percentage of [18F] THK-5105 bonding in the absence of each tested compound was set to be 100%, and percentages of [18F] THK-5105 bonding at various concentrations of each of the tested compounds were determined.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Microtubule-associated protein tau (CHEMBL1293224) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tau imaging probe
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.48 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893272 | — | — | 1 | 8.04 |
| CHEMBL3985550 | — | — | 1 | 7.98 |
| CHEMBL3973145 | — | — | 1 | 7.67 |
| CHEMBL3939385 | — | — | 1 | 7.46 |
| CHEMBL3953540 | — | — | 1 | 7.44 |
| CHEMBL3947029 | — | — | 1 | 7.40 |
| CHEMBL2219511 | — | — | 1 | 7.23 |
| CHEMBL207649 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893272 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL3985550 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL3973145 | — | Ki | = | 21.4 | nM | 7.67 |
| CHEMBL3939385 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL3953540 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3947029 | — | Ki | = | 40.1 | nM | 7.40 |
| CHEMBL2219511 | — | Ki | = | 59.3 | nM | 7.23 |
| CHEMBL207649 | — | Ki | = | 256.0 | nM | 6.59 |