Assay Detail
Binding
CHEMBL5736378
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Direct Determination By Fluorescence: Table 6 & 7: Fresh solutions of each test compound (2.5 mM in DMSO) are diluted in PBS pH=7.4 at concentrations between 0.5 nM and 5 μM in the presence or absence of α-syn (200 nM), Aβ1-42 (500 nM) or Tau (200 nM) fibers in a final 2 mL volume. After 1 h of incubation at RT, the binding of each compound to α-syn, A131-42 or Tau fibers is measured by fluorescence using the spectral changes of the compounds during their binding to the fibers, using the appropriate excitation/emission wavelengths (those giving the highest fluorescence variation during binding to the fibres). For each concentration of compound added to the fibres, the bound and free fractions are measured by fluorescence according to the following equation:F m =F B B+F F×(T−B).
57
Total Activities
11
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Compounds for using in imaging and particularly for the diagnosis of neurodegenerative diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 19 | 8.69 | 9.31 |
| kon | 19 | - | - |
| k_off | 19 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5896450 | — | — | 6 | 9.31 |
| CHEMBL5771524 | — | — | 6 | 9.28 |
| CHEMBL5790440 | — | — | 3 | 9.14 |
| CHEMBL5843241 | — | — | 3 | 9.10 |
| CHEMBL5843281 | — | — | 6 | 9.00 |
| CHEMBL5759738 | — | — | 3 | 8.90 |
| CHEMBL6035240 | — | — | 6 | 8.85 |
| CHEMBL6034599 | — | — | 6 | 8.62 |
| CHEMBL6001659 | — | — | 6 | 8.49 |
| CHEMBL207649 | — | — | 6 | 7.79 |
| CHEMBL1908919 | FLORBETAPIR | 4.0 | 6 | 7.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5896450 | — | Kd | = | 0.49 | nM | 9.31 |
| CHEMBL5896450 | — | Kd | = | 0.49 | nM | 9.31 |
| CHEMBL5771524 | — | Kd | = | 0.53 | nM | 9.28 |
| CHEMBL5771524 | — | Kd | = | 0.53 | nM | 9.28 |
| CHEMBL5790440 | — | Kd | = | 0.73 | nM | 9.14 |
| CHEMBL5843241 | — | Kd | = | 0.79 | nM | 9.10 |
| CHEMBL5843281 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL5843281 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL5759738 | — | Kd | = | 1.27 | nM | 8.90 |
| CHEMBL6035240 | — | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL6035240 | — | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL6034599 | — | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL6034599 | — | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL6001659 | — | Kd | = | 3.25 | nM | 8.49 |
| CHEMBL6001659 | — | Kd | = | 3.25 | nM | 8.49 |
| CHEMBL207649 | — | Kd | = | 16.1 | nM | 7.79 |
| CHEMBL207649 | — | Kd | = | 16.1 | nM | 7.79 |
| CHEMBL1908919 | FLORBETAPIR | Kd | = | 24.3 | nM | 7.61 |
| CHEMBL1908919 | FLORBETAPIR | Kd | = | 24.3 | nM | 7.61 |
| CHEMBL5843241 | — | k_off | = | - | s-1 | - |
| CHEMBL5843241 | — | kon | = | - | — | - |
| CHEMBL5843281 | — | k_off | = | - | s-1 | - |
| CHEMBL1908919 | FLORBETAPIR | kon | = | - | — | - |
| CHEMBL6001659 | — | k_off | = | - | s-1 | - |
| CHEMBL6001659 | — | kon | = | - | — | - |
| CHEMBL6035240 | — | k_off | = | - | s-1 | - |
| CHEMBL6035240 | — | kon | = | - | — | - |
| CHEMBL5771524 | — | k_off | = | - | s-1 | - |
| CHEMBL5771524 | — | kon | = | - | — | - |
| CHEMBL207649 | — | k_off | = | - | s-1 | - |
| CHEMBL207649 | — | kon | = | - | — | - |
| CHEMBL1908919 | FLORBETAPIR | k_off | = | - | s-1 | - |
| CHEMBL1908919 | FLORBETAPIR | kon | = | - | — | - |
| CHEMBL5843281 | — | kon | = | - | — | - |
| CHEMBL6034599 | — | k_off | = | - | s-1 | - |
| CHEMBL6034599 | — | kon | = | - | — | - |
| CHEMBL5896450 | — | k_off | = | - | s-1 | - |
| CHEMBL5896450 | — | kon | = | - | — | - |
| CHEMBL5843281 | — | k_off | = | - | s-1 | - |
| CHEMBL5843281 | — | kon | = | - | — | - |
| CHEMBL6001659 | — | k_off | = | - | s-1 | - |
| CHEMBL6001659 | — | kon | = | - | — | - |
| CHEMBL6035240 | — | k_off | = | - | s-1 | - |
| CHEMBL6035240 | — | kon | = | - | — | - |
| CHEMBL5771524 | — | k_off | = | - | s-1 | - |
| CHEMBL5759738 | — | kon | = | - | — | - |
| CHEMBL5771524 | — | kon | = | - | — | - |
| CHEMBL207649 | — | kon | = | - | — | - |
| CHEMBL207649 | — | k_off | = | - | s-1 | - |
| CHEMBL1908919 | FLORBETAPIR | k_off | = | - | s-1 | - |