Assay Detail
Functional
CHEMBL1786743
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Antagonist activity at human mGluR1
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 7.72 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783874 | — | — | 1 | 9.05 |
| CHEMBL1783864 | — | — | 1 | 8.96 |
| CHEMBL1783875 | — | — | 1 | 8.82 |
| CHEMBL1784049 | — | — | 1 | 8.74 |
| CHEMBL1784053 | — | — | 1 | 8.72 |
| CHEMBL1783858 | — | — | 1 | 8.70 |
| CHEMBL1783876 | — | — | 1 | 8.68 |
| CHEMBL1784067 | — | — | 1 | 8.52 |
| CHEMBL1784051 | — | — | 1 | 8.42 |
| CHEMBL1784068 | — | — | 1 | 8.41 |
| CHEMBL1783863 | — | — | 1 | 8.36 |
| CHEMBL1784059 | — | — | 1 | 8.34 |
| CHEMBL1784070 | — | — | 1 | 8.17 |
| CHEMBL1783862 | — | — | 1 | 8.17 |
| CHEMBL1783865 | — | — | 1 | 8.16 |
| CHEMBL1784054 | — | — | 1 | 8.11 |
| CHEMBL1784072 | — | — | 1 | 8.09 |
| CHEMBL1784065 | — | — | 1 | 8.05 |
| CHEMBL428909 | — | — | 1 | 8.02 |
| CHEMBL1784056 | — | — | 1 | 8.02 |
| CHEMBL1783869 | — | — | 1 | 7.98 |
| CHEMBL1784052 | — | — | 1 | 7.97 |
| CHEMBL1784061 | — | — | 1 | 7.97 |
| CHEMBL1783867 | — | — | 1 | 7.97 |
| CHEMBL1783859 | — | — | 1 | 7.96 |
| CHEMBL1784055 | — | — | 1 | 7.91 |
| CHEMBL1783861 | — | — | 1 | 7.90 |
| CHEMBL1784050 | — | — | 1 | 7.90 |
| CHEMBL1784069 | — | — | 1 | 7.89 |
| CHEMBL1784057 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783874 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1783864 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1783875 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1784049 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1784053 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1783858 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1783876 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1784067 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1784051 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1784068 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1783863 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1784059 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1784070 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1783862 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1783865 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1784054 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL1784072 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL1784065 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL428909 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL1784056 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL1783869 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL1784052 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL1784061 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL1783867 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL1783859 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1784055 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL1784050 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL1783861 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL1784069 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1784057 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL1784063 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1783868 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL1784064 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1784077 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1784066 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1783870 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1784075 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1784062 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1783860 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1783866 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1784058 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1784073 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1783871 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL1784048 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL1784074 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL1784080 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL1783872 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL1784076 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL1784071 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL1784078 | — | IC50 | = | 219.0 | nM | 6.66 |