Assay Detail
Binding
CHEMBL5732349
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biological Assay: The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR2 activity, may be demonstrated by methodology known in the art. Antagonist constants are determined as follows. The compounds of the present invention were tested in a fluorescence laser imaging plate reader based assay. This assay is a common functional assay to monitor Ca2+ mobilization in whole cells expressing recombinant receptor coupled with a promiscuous G-protein. CHO dhfr-cells stably expressing recombinant human mGluR2 and Gα16 loaded with Fluo-4 AM (Invitrogen, Carlsbad Calif.) are treated with various concentrations of antagonists of compounds and the Ca2+ response is monitored on a FLIPR384 (Molecular Devices, Sunnydale Calif.) for agonist activity. Then 2,500 nM glutamate is added and the antagonist response is monitored. The maximum calcium response at each concentration of compound for agonist or antagonist were plotted as dose responses and the curves were fitted with a four parameter logistic equation giving IC50 and Hill coefficient using the iterative non linear curve fitting software ADA (Merck & Co).
945
Total Activities
292
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 315 | 7.34 | 8.40 |
| kon | 315 | - | - |
| k_off | 315 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3945590 | — | — | 3 | 8.40 |
| CHEMBL3971388 | — | — | 3 | 8.30 |
| CHEMBL3964644 | — | — | 6 | 8.30 |
| CHEMBL3946016 | — | — | 6 | 8.30 |
| CHEMBL3923126 | — | — | 3 | 8.30 |
| CHEMBL3983863 | — | — | 3 | 8.22 |
| CHEMBL5958633 | — | — | 3 | 8.22 |
| CHEMBL3966866 | — | — | 9 | 8.22 |
| CHEMBL3955188 | — | — | 3 | 8.22 |
| CHEMBL3941863 | — | — | 3 | 8.22 |
| CHEMBL3925177 | — | — | 3 | 8.15 |
| CHEMBL3937970 | — | — | 3 | 8.15 |
| CHEMBL3950572 | — | — | 3 | 8.15 |
| CHEMBL3961599 | — | — | 3 | 8.15 |
| CHEMBL3958138 | — | — | 3 | 8.15 |
| CHEMBL5818443 | — | — | 3 | 8.15 |
| CHEMBL3937038 | — | — | 3 | 8.10 |
| CHEMBL3904730 | — | — | 6 | 8.10 |
| CHEMBL3939455 | — | — | 6 | 8.10 |
| CHEMBL3971450 | — | — | 3 | 8.10 |
| CHEMBL3959134 | — | — | 3 | 8.10 |
| CHEMBL4108673 | — | — | 3 | 8.10 |
| CHEMBL4106729 | — | — | 3 | 8.10 |
| CHEMBL3912615 | — | — | 3 | 8.10 |
| CHEMBL4110317 | — | — | 3 | 8.10 |
| CHEMBL3894283 | — | — | 3 | 8.10 |
| CHEMBL3892073 | — | — | 3 | 8.05 |
| CHEMBL6009139 | — | — | 3 | 8.05 |
| CHEMBL3985872 | — | — | 3 | 8.05 |
| CHEMBL4109555 | — | — | 3 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3945590 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3946016 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3971388 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3964644 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3964644 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3923126 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3941863 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3955188 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3966866 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3983863 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5958633 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3925177 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5818443 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3950572 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3958138 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3961599 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3937970 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3937038 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4108673 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3959134 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3904730 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3894283 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4110317 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3912615 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3971450 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4106729 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3939455 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL6009139 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3983820 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3892073 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3954035 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3936681 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3985872 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4109555 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4113710 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3925389 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3979547 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3946016 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4111267 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3953157 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3935153 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3936681 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3926942 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3904730 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4113710 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3939455 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3892899 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3966866 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3959588 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4109697 | — | IC50 | = | 11.0 | nM | 7.96 |