Assay Detail
Binding
CHEMBL4413470
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis
52
Total Activities
52
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
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 52 | 7.83 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3597594 | — | — | 1 | 9.30 |
| CHEMBL4472693 | — | — | 1 | 9.15 |
| CHEMBL4535926 | — | — | 1 | 9.15 |
| CHEMBL4439229 | — | — | 1 | 9.01 |
| CHEMBL4446275 | — | — | 1 | 8.70 |
| CHEMBL4441707 | — | — | 1 | 8.60 |
| CHEMBL4539036 | — | — | 1 | 8.60 |
| CHEMBL4472416 | — | — | 1 | 8.59 |
| CHEMBL4452522 | — | — | 1 | 8.57 |
| CHEMBL4592284 | — | — | 1 | 8.54 |
| CHEMBL4451661 | — | — | 1 | 8.54 |
| CHEMBL4455843 | — | — | 1 | 8.54 |
| CHEMBL4513498 | — | — | 1 | 8.48 |
| CHEMBL4551786 | — | — | 1 | 8.46 |
| CHEMBL4551238 | — | — | 1 | 8.44 |
| CHEMBL4448788 | — | — | 1 | 8.41 |
| CHEMBL4544729 | — | — | 1 | 8.40 |
| CHEMBL4475143 | — | — | 1 | 8.40 |
| CHEMBL4548820 | — | — | 1 | 8.37 |
| CHEMBL4548205 | — | — | 1 | 8.32 |
| CHEMBL4441964 | — | — | 1 | 8.24 |
| CHEMBL4542890 | — | — | 1 | 8.10 |
| CHEMBL4464022 | — | — | 1 | 8.07 |
| CHEMBL66654 | — | — | 1 | 7.98 |
| CHEMBL4460573 | — | — | 1 | 7.95 |
| CHEMBL4448804 | — | — | 1 | 7.92 |
| CHEMBL4456792 | — | — | 1 | 7.80 |
| CHEMBL4483689 | — | — | 1 | 7.74 |
| CHEMBL4520868 | — | — | 1 | 7.74 |
| CHEMBL4567923 | — | — | 1 | 7.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3597594 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4472693 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4535926 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4439229 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL4446275 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL4441707 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4539036 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4472416 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL4452522 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4592284 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4451661 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4455843 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4513498 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4551786 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL4551238 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4448788 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4544729 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4475143 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL4548820 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL4548205 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL4441964 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL4542890 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL4464022 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL66654 | — | Ki | = | 10.4 | nM | 7.98 |
| CHEMBL4460573 | — | Ki | = | 11.3 | nM | 7.95 |
| CHEMBL4448804 | — | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL4456792 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL4483689 | — | Ki | = | 18.4 | nM | 7.74 |
| CHEMBL4520868 | — | Ki | = | 18.2 | nM | 7.74 |
| CHEMBL4567923 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL4443478 | — | Ki | = | 20.4 | nM | 7.69 |
| CHEMBL4590911 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL292065 | — | Ki | = | 32.7 | nM | 7.49 |
| CHEMBL4464549 | — | Ki | = | 38.3 | nM | 7.42 |
| CHEMBL4568857 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4449412 | — | Ki | = | 48.2 | nM | 7.32 |
| CHEMBL4535967 | — | Ki | = | 64.2 | nM | 7.19 |
| CHEMBL4453683 | — | Ki | = | 67.3 | nM | 7.17 |
| CHEMBL4525950 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL4449729 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL4448304 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL239800 | FENOBAM ANHYDROUS | Ki | = | 162.2 | nM | 6.79 |
| CHEMBL4463438 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL4530045 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL4539998 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL4571404 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL4454630 | — | Ki | = | 276.0 | nM | 6.56 |
| CHEMBL4563328 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL4584639 | — | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL4474134 | — | Ki | = | 456.0 | nM | 6.34 |