Assay Detail
Binding
CHEMBL3599914
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometry
24
Total Activities
24
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
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 8.42 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3597596 | — | — | 1 | 9.52 |
| CHEMBL3597597 | — | — | 1 | 9.52 |
| CHEMBL3597600 | — | — | 1 | 9.52 |
| CHEMBL3597593 | — | — | 1 | 9.52 |
| CHEMBL3597585 | — | — | 1 | 9.40 |
| CHEMBL3597592 | — | — | 1 | 9.40 |
| CHEMBL3597602 | — | — | 1 | 9.30 |
| CHEMBL3597594 | — | — | 1 | 9.30 |
| CHEMBL3597598 | — | — | 1 | 9.30 |
| CHEMBL3597584 | — | — | 1 | 9.30 |
| CHEMBL369310 | — | — | 1 | 8.33 |
| CHEMBL66654 | — | — | 1 | 7.98 |
| CHEMBL3597595 | — | — | 1 | 7.54 |
| CHEMBL292065 | — | — | 1 | 7.49 |
| CHEMBL3597603 | — | — | 1 | 7.38 |
| CHEMBL3597591 | — | — | 1 | 7.22 |
| CHEMBL239800 | FENOBAM ANHYDROUS | 2.0 | 1 | 6.79 |
| CHEMBL3597604 | — | — | 1 | 6.58 |
| CHEMBL3597599 | — | — | 1 | 6.55 |
| CHEMBL3597590 | — | — | 1 | - |
| CHEMBL3597589 | — | — | 1 | - |
| CHEMBL3597588 | — | — | 1 | - |
| CHEMBL3597601 | — | — | 1 | - |
| CHEMBL3597587 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3597596 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3597597 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3597600 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3597593 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3597585 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3597592 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3597602 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3597594 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3597598 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3597584 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL369310 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL66654 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL3597595 | — | Ki | = | 29.2 | nM | 7.54 |
| CHEMBL292065 | — | Ki | = | 32.7 | nM | 7.49 |
| CHEMBL3597603 | — | Ki | = | 41.8 | nM | 7.38 |
| CHEMBL3597591 | — | Ki | = | 60.7 | nM | 7.22 |
| CHEMBL239800 | FENOBAM ANHYDROUS | Ki | = | 162.2 | nM | 6.79 |
| CHEMBL3597604 | — | Ki | = | 264.3 | nM | 6.58 |
| CHEMBL3597599 | — | Ki | = | 283.1 | nM | 6.55 |
| CHEMBL3597590 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3597589 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3597588 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3597601 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3597587 | — | Ki | > | 10000.0 | nM | - |