Assay Detail
Functional
CHEMBL864050
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 59 | 6.64 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL201943 | — | — | 1 | 9.03 |
| CHEMBL202307 | — | — | 1 | 8.70 |
| CHEMBL202003 | — | — | 1 | 7.99 |
| CHEMBL201068 | — | — | 1 | 7.72 |
| CHEMBL202323 | — | — | 1 | 7.64 |
| CHEMBL202436 | — | — | 1 | 7.60 |
| CHEMBL202002 | — | — | 1 | 7.44 |
| CHEMBL66654 | — | — | 1 | 7.41 |
| CHEMBL383771 | — | — | 1 | 7.34 |
| CHEMBL440220 | — | — | 1 | 7.31 |
| CHEMBL202116 | — | — | 1 | 7.22 |
| CHEMBL382658 | — | — | 1 | 7.16 |
| CHEMBL370559 | — | — | 1 | 7.11 |
| CHEMBL182950 | — | — | 1 | 7.08 |
| CHEMBL202124 | — | — | 1 | 6.89 |
| CHEMBL370453 | — | — | 1 | 6.85 |
| CHEMBL201787 | — | — | 1 | 6.79 |
| CHEMBL380710 | — | — | 1 | 6.72 |
| CHEMBL201771 | — | — | 1 | 6.65 |
| CHEMBL372511 | — | — | 1 | 6.64 |
| CHEMBL381483 | — | — | 1 | 6.58 |
| CHEMBL202610 | — | — | 1 | 6.47 |
| CHEMBL370142 | — | — | 1 | 6.38 |
| CHEMBL372532 | — | — | 1 | 6.37 |
| CHEMBL292065 | — | — | 1 | 6.33 |
| CHEMBL202331 | — | — | 1 | 6.32 |
| CHEMBL382491 | — | — | 1 | 6.28 |
| CHEMBL201974 | — | — | 1 | 6.18 |
| CHEMBL201857 | — | — | 1 | 6.16 |
| CHEMBL381031 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL201943 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL202307 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL202003 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL201068 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL202323 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL202436 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL202002 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL66654 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL383771 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL440220 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL202116 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL382658 | — | IC50 | = | 68.6 | nM | 7.16 |
| CHEMBL370559 | — | IC50 | = | 78.6 | nM | 7.11 |
| CHEMBL182950 | — | IC50 | = | 82.6 | nM | 7.08 |
| CHEMBL202124 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL370453 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL201787 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL380710 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL201771 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL372511 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL381483 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL202610 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL370142 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL372532 | — | IC50 | = | 426.0 | nM | 6.37 |
| CHEMBL292065 | — | IC50 | = | 462.0 | nM | 6.33 |
| CHEMBL202331 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL382491 | — | IC50 | = | 526.0 | nM | 6.28 |
| CHEMBL201974 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL201857 | — | IC50 | = | 698.0 | nM | 6.16 |
| CHEMBL381031 | — | IC50 | = | 789.0 | nM | 6.10 |
| CHEMBL201727 | — | IC50 | = | 833.0 | nM | 6.08 |
| CHEMBL202042 | — | IC50 | = | 946.0 | nM | 6.02 |
| CHEMBL414673 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL202203 | — | IC50 | = | 1093.0 | nM | 5.96 |
| CHEMBL202277 | — | IC50 | = | 1243.0 | nM | 5.91 |
| CHEMBL371884 | — | IC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL381482 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL202051 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL201774 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL201939 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL373017 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL202125 | — | IC50 | = | 2966.0 | nM | 5.53 |
| CHEMBL382527 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL202041 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL373060 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL202619 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL440218 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL371254 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL380881 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL434188 | — | IC50 | > | 10000.0 | nM | - |