Assay Detail
Binding
CHEMBL4620114
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Negative allosteric modulation of human mGluR2 by FLIPR assay
34
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.19 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3892073 | — | — | 1 | 8.05 |
| CHEMBL4637618 | — | — | 1 | 8.00 |
| CHEMBL4642428 | — | — | 2 | 7.92 |
| CHEMBL4640203 | — | — | 1 | 7.89 |
| CHEMBL4642338 | — | — | 1 | 7.80 |
| CHEMBL4109248 | — | — | 1 | 7.80 |
| CHEMBL4644424 | — | — | 1 | 7.72 |
| CHEMBL3973949 | — | — | 1 | 7.68 |
| CHEMBL4647980 | — | — | 1 | 7.60 |
| CHEMBL4108213 | — | — | 1 | 7.44 |
| CHEMBL4640529 | — | — | 1 | 7.44 |
| CHEMBL3953417 | — | — | 1 | 7.24 |
| CHEMBL3919306 | — | — | 1 | 7.21 |
| CHEMBL3974648 | — | — | 1 | 7.17 |
| CHEMBL4638570 | — | — | 1 | 7.17 |
| CHEMBL4635528 | — | — | 1 | 7.04 |
| CHEMBL4643527 | — | — | 1 | 6.84 |
| CHEMBL3945170 | — | — | 1 | 6.83 |
| CHEMBL4634754 | — | — | 1 | 6.62 |
| CHEMBL4636186 | — | — | 1 | 6.43 |
| CHEMBL4642255 | — | — | 1 | 6.39 |
| CHEMBL4634600 | — | — | 1 | 6.39 |
| CHEMBL4634351 | — | — | 1 | 5.86 |
| CHEMBL4646222 | — | — | 1 | 5.57 |
| CHEMBL4645156 | — | — | 1 | - |
| CHEMBL4638395 | — | — | 1 | - |
| CHEMBL4632721 | — | — | 1 | - |
| CHEMBL4640683 | — | — | 1 | - |
| CHEMBL4649821 | — | — | 1 | - |
| CHEMBL4646658 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3892073 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4637618 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4642428 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4640203 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4642338 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4109248 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4644424 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4642428 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3973949 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4647980 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4108213 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4640529 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3953417 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3919306 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3974648 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4638570 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4635528 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4643527 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3945170 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4634754 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4636186 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL4642255 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL4634600 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL4634351 | — | IC50 | = | 1378.0 | nM | 5.86 |
| CHEMBL4646222 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4645156 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638395 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4632721 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4640683 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649821 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4646658 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638009 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4635360 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642363 | — | IC50 | > | 10000.0 | nM | - |