Basic Information
ID: ALA3706001
Type: Binding
Description: Metabotropic Glutamate Receptor Activity Assay: The utility of the compounds in accordance with the present invention as negative allosteric modulators of metabotropic glutamate receptor activity, in particular mGluR5 activity, can be demonstrated by methodology known in the art. Human embryonic kidney (HEK) cells transfected with rat or human mGluR5 were plated in clear bottom assay plates for assay in a Functional Drug Screening System (FDSS). The cells were loaded with a Ca2+-sensitive fluorescent dye (e.g., Fluo-4), and the plates were washed and placed in the FDSS instrument. Test compound was applied to cells 3 seconds after baseline readings were taken. Cells were incubated with the test compounds for 140 seconds and then stimulated with an EC20 concentration of an mGluR5 agonist (e.g., glutamate, 3,5-dihydroxyphenylglycine, or quisqualate); 60-80 seconds later an EC80 concentration of agonist was added and readings taken for an additional 40 seconds. Data were collected at 1 Hz. Negative allosteric modulation of the agonist.
Format: BAO_0000019
Organism: Rattus norvegicus
Target: Metabotropic glutamate receptor 5(ALA2564)
Document: ALA3638661
BindingDB Source: 6426
Activity Charts
Bioactivity
Activity Types for Assay ALA3706001
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 384.31 | 4.14 | 4.14 |
| 344.73 | 3.71 | 3.71 |
| 378.29 | 4.07 | 4.07 |
| 344.73 | 3.71 | 3.71 |
| 344.73 | 3.71 | 3.71 |
| 361.19 | 4.22 | 4.22 |
| 356.77 | 3.58 | 3.58 |
| 330.34 | 3.43 | 3.43 |
| 346.80 | 3.94 | 3.94 |
| 344.73 | 3.71 | 3.71 |
| 343.39 | 3.40 | 3.40 |
| 357.78 | 3.68 | 3.68 |
| 357.78 | 3.68 | 3.68 |
| 325.30 | 2.76 | 2.76 |
| 409.24 | 4.19 | 4.19 |