Assay Detail
Binding
CHEMBL4040510
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-JNJ46281222 from human metabotropic glutamate receptor 2 expressed in CHOK1 cell membranes after 60 mins by microbeta counting analysis
41
Total Activities
41
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 and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 41 | 8.10 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4063313 | — | — | 1 | 9.05 |
| CHEMBL4101354 | — | — | 1 | 8.82 |
| CHEMBL4077609 | — | — | 1 | 8.72 |
| CHEMBL4075258 | — | — | 1 | 8.71 |
| CHEMBL4091370 | — | — | 1 | 8.69 |
| CHEMBL4104081 | — | — | 1 | 8.66 |
| CHEMBL4073628 | — | — | 1 | 8.65 |
| CHEMBL4080973 | — | — | 1 | 8.59 |
| CHEMBL4074421 | — | — | 1 | 8.52 |
| CHEMBL4093657 | — | — | 1 | 8.50 |
| CHEMBL4087196 | — | — | 1 | 8.44 |
| CHEMBL4072262 | — | — | 1 | 8.44 |
| CHEMBL4067421 | — | — | 1 | 8.41 |
| CHEMBL4064589 | — | — | 1 | 8.30 |
| CHEMBL4067290 | — | — | 1 | 8.28 |
| CHEMBL4074664 | — | — | 1 | 8.22 |
| CHEMBL4075762 | — | — | 1 | 8.22 |
| CHEMBL4089612 | — | — | 1 | 8.19 |
| CHEMBL4060306 | — | — | 1 | 8.17 |
| CHEMBL4103808 | — | — | 1 | 8.15 |
| CHEMBL4072134 | — | — | 1 | 8.13 |
| CHEMBL4093792 | — | — | 1 | 8.10 |
| CHEMBL4076786 | — | — | 1 | 8.06 |
| CHEMBL4088239 | — | — | 1 | 8.05 |
| CHEMBL4076639 | — | — | 1 | 8.03 |
| CHEMBL4089955 | — | — | 1 | 8.00 |
| CHEMBL4089416 | — | — | 1 | 7.99 |
| CHEMBL4081244 | — | — | 1 | 7.94 |
| CHEMBL4075537 | — | — | 1 | 7.93 |
| CHEMBL4067298 | — | — | 1 | 7.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4063313 | — | Ki | = | 0.8913 | nM | 9.05 |
| CHEMBL4101354 | — | Ki | = | 1.514 | nM | 8.82 |
| CHEMBL4077609 | — | Ki | = | 1.905 | nM | 8.72 |
| CHEMBL4075258 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL4091370 | — | Ki | = | 2.042 | nM | 8.69 |
| CHEMBL4104081 | — | Ki | = | 2.188 | nM | 8.66 |
| CHEMBL4073628 | — | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL4080973 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL4074421 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL4093657 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL4072262 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL4087196 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL4067421 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL4064589 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL4067290 | — | Ki | = | 5.248 | nM | 8.28 |
| CHEMBL4074664 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL4075762 | — | Ki | = | 6.026 | nM | 8.22 |
| CHEMBL4089612 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL4060306 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL4103808 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL4072134 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL4093792 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL4076786 | — | Ki | = | 8.71 | nM | 8.06 |
| CHEMBL4088239 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL4076639 | — | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL4089955 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4089416 | — | Ki | = | 10.23 | nM | 7.99 |
| CHEMBL4081244 | — | Ki | = | 11.48 | nM | 7.94 |
| CHEMBL4075537 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL4067298 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL4066051 | — | Ki | = | 14.79 | nM | 7.83 |
| CHEMBL4085882 | — | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL4075417 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL4088960 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL4075697 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL4100691 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL4092275 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL4075593 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL4076286 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL4062535 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL4093620 | — | Ki | = | 63.1 | nM | 7.20 |