Assay Detail
Binding
CHEMBL5735451
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Fluorescent Displacement Assay: A Nunc black plate was used as a 96-well plate for the purpose of measurement, and to each well was added 40 μL of sodium phosphate buffer and a sodium phosphate buffer solution of FABP3 (AVISCERA BIOSCIENCE) (250 nM, 25 μL), and for a blank, 25 μL of sodium phosphate buffer was added. To each well was added as a detection reagent, a 1,8-ANS (ALDRICH) solution (10 μM, ethanol/sodium phosphate buffer solution=1:4 v/v, 25 μL), and ethanol solutions of compounds diluted to different concentrations were added in an amount of 10 μL each (the final ethanol concentration was 15%). The plate was shaken for 10 sec. in the plate reader and incubated for 10 min. at room temperature. Then, it was subjected to fluorescent measurement at an excitation wavelength of 355 nm and a measurement wavelength of 460 nm. Used for measurement was ARVO X One by PerkinElmer Japan.
60
Total Activities
16
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Agent for treating synucleinopathy
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| kon | 20 | - | - |
| k_off | 20 | - | - |
| IC50 | 10 | 6.36 | 7.28 |
| Kd | 10 | 5.89 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5878164 | — | — | 3 | 7.28 |
| CHEMBL5555714 | — | — | 6 | 7.11 |
| CHEMBL5770423 | — | — | 6 | 6.55 |
| CHEMBL5976044 | — | — | 3 | 6.38 |
| CHEMBL6048509 | — | — | 3 | 6.29 |
| CHEMBL2334261 | — | — | 3 | 6.16 |
| CHEMBL2334255 | — | — | 6 | 6.14 |
| CHEMBL2334257 | — | — | 3 | 6.10 |
| CHEMBL5777988 | — | — | 3 | 6.10 |
| CHEMBL5757642 | — | — | 3 | 6.01 |
| CHEMBL5567823 | — | — | 3 | 5.95 |
| CHEMBL5801911 | — | — | 3 | 5.89 |
| CHEMBL5753881 | — | — | 3 | 5.89 |
| CHEMBL2334254 | — | — | 3 | 5.70 |
| CHEMBL5754165 | — | — | 3 | 5.55 |
| CHEMBL2334260 | — | — | 6 | 5.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5878164 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5555714 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5770423 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5555714 | — | Kd | = | 386.0 | nM | 6.41 |
| CHEMBL5976044 | — | Kd | = | 414.0 | nM | 6.38 |
| CHEMBL6048509 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2334261 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2334255 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL2334257 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL5777988 | — | Kd | = | 787.0 | nM | 6.10 |
| CHEMBL5757642 | — | Kd | = | 968.0 | nM | 6.01 |
| CHEMBL5567823 | — | Kd | = | 1128.0 | nM | 5.95 |
| CHEMBL2334255 | — | Kd | = | 1246.0 | nM | 5.90 |
| CHEMBL5753881 | — | Kd | = | 1293.0 | nM | 5.89 |
| CHEMBL5801911 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2334254 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5770423 | — | Kd | = | 2216.0 | nM | 5.65 |
| CHEMBL5754165 | — | Kd | = | 2846.0 | nM | 5.55 |
| CHEMBL2334260 | — | Kd | = | 9625.0 | nM | 5.02 |
| CHEMBL2334254 | — | k_off | = | - | s-1 | - |
| CHEMBL2334255 | — | k_off | = | - | s-1 | - |
| CHEMBL2334261 | — | k_off | = | - | s-1 | - |
| CHEMBL2334261 | — | kon | = | - | — | - |
| CHEMBL2334257 | — | k_off | = | - | s-1 | - |
| CHEMBL2334257 | — | kon | = | - | — | - |
| CHEMBL5878164 | — | k_off | = | - | s-1 | - |
| CHEMBL5878164 | — | kon | = | - | — | - |
| CHEMBL5770423 | — | k_off | = | - | s-1 | - |
| CHEMBL5770423 | — | kon | = | - | — | - |
| CHEMBL2334255 | — | k_off | = | - | s-1 | - |
| CHEMBL2334255 | — | kon | = | - | — | - |
| CHEMBL5555714 | — | k_off | = | - | s-1 | - |
| CHEMBL5555714 | — | kon | = | - | — | - |
| CHEMBL2334254 | — | kon | = | - | — | - |
| CHEMBL5976044 | — | kon | = | - | — | - |
| CHEMBL5567823 | — | k_off | = | - | s-1 | - |
| CHEMBL5567823 | — | kon | = | - | — | - |
| CHEMBL5976044 | — | k_off | = | - | s-1 | - |
| CHEMBL5777988 | — | kon | = | - | — | - |
| CHEMBL5757642 | — | k_off | = | - | s-1 | - |
| CHEMBL5777988 | — | k_off | = | - | s-1 | - |
| CHEMBL5757642 | — | kon | = | - | — | - |
| CHEMBL2334260 | — | k_off | = | - | s-1 | - |
| CHEMBL2334260 | — | kon | = | - | — | - |
| CHEMBL5753881 | — | kon | = | - | — | - |
| CHEMBL5770423 | — | k_off | = | - | s-1 | - |
| CHEMBL5770423 | — | kon | = | - | — | - |
| CHEMBL5754165 | — | kon | = | - | — | - |
| CHEMBL5753881 | — | k_off | = | - | s-1 | - |
| CHEMBL5754165 | — | k_off | = | - | s-1 | - |