Assay Detail
Binding
CHEMBL874546
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Inhibitory concentration against human metabotropic glutamate receptor
32
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.45 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL174588 | — | — | 2 | 9.26 |
| CHEMBL178690 | — | — | 1 | 9.25 |
| CHEMBL2112967 | — | — | 1 | 9.00 |
| CHEMBL175463 | — | — | 1 | 8.70 |
| CHEMBL176279 | — | — | 1 | 8.52 |
| CHEMBL178592 | — | — | 1 | 8.40 |
| CHEMBL360728 | — | — | 1 | 8.22 |
| CHEMBL177519 | — | — | 1 | 8.15 |
| CHEMBL175377 | — | — | 1 | 8.10 |
| CHEMBL2112964 | — | — | 1 | 8.05 |
| CHEMBL369459 | — | — | 1 | 7.85 |
| CHEMBL2112048 | — | — | 1 | 7.80 |
| CHEMBL178741 | — | — | 1 | 7.75 |
| CHEMBL174216 | — | — | 1 | 7.54 |
| CHEMBL177586 | — | — | 1 | 7.29 |
| CHEMBL177043 | — | — | 1 | 7.21 |
| CHEMBL178742 | — | — | 1 | 7.13 |
| CHEMBL177585 | — | — | 1 | 7.10 |
| CHEMBL441844 | — | — | 1 | 7.07 |
| CHEMBL175699 | — | — | 1 | 7.07 |
| CHEMBL175643 | — | — | 1 | 7.03 |
| CHEMBL367227 | — | — | 1 | 6.98 |
| CHEMBL353547 | — | — | 1 | 6.80 |
| CHEMBL2112963 | — | — | 1 | 6.76 |
| CHEMBL2112965 | — | — | 1 | 6.72 |
| CHEMBL176068 | — | — | 1 | 6.35 |
| CHEMBL366448 | — | — | 1 | 5.93 |
| CHEMBL177736 | — | — | 1 | 5.36 |
| CHEMBL2112966 | — | — | 1 | 5.20 |
| CHEMBL174382 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL174588 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL178690 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL2112967 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL175463 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL176279 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL178592 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL360728 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL177519 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL175377 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2112964 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL369459 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2112048 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL178741 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL174216 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL177586 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL177043 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL178742 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL177585 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL441844 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL175699 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL175643 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL367227 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL174588 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL353547 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2112963 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL2112965 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL176068 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL366448 | — | IC50 | = | 1175.0 | nM | 5.93 |
| CHEMBL177736 | — | IC50 | = | 4360.0 | nM | 5.36 |
| CHEMBL2112966 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL174382 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL174218 | — | IC50 | > | 10000.0 | nM | - |