Assay Detail
Binding
CHEMBL4430980
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]MSX from A2A receptor in rat brain striatum membranes measured after 30 mins by liquid scintillation counting method
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Subcellular | Membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 62 | 5.75 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4554778 | — | — | 1 | 7.21 |
| CHEMBL4540395 | — | — | 1 | 6.92 |
| CHEMBL4483392 | — | — | 1 | 6.80 |
| CHEMBL4582207 | — | — | 1 | 6.50 |
| CHEMBL4549506 | — | — | 1 | 6.45 |
| CHEMBL4567470 | — | — | 1 | 6.35 |
| CHEMBL4451303 | — | — | 1 | 6.29 |
| CHEMBL4442891 | — | — | 1 | 6.25 |
| CHEMBL4555393 | — | — | 1 | 6.00 |
| CHEMBL4469103 | — | — | 1 | 5.88 |
| CHEMBL4465423 | — | — | 1 | 5.82 |
| CHEMBL4534266 | — | — | 1 | 5.80 |
| CHEMBL4518442 | — | — | 1 | 5.74 |
| CHEMBL4450570 | — | — | 1 | 5.67 |
| CHEMBL4556251 | — | — | 1 | 5.67 |
| CHEMBL4474238 | — | — | 1 | 5.65 |
| CHEMBL4449715 | — | — | 1 | 5.62 |
| CHEMBL4515367 | — | — | 1 | 5.61 |
| CHEMBL4464931 | — | — | 1 | 5.59 |
| CHEMBL4469213 | — | — | 1 | 5.56 |
| CHEMBL4465460 | — | — | 1 | 5.54 |
| CHEMBL4556578 | — | — | 1 | 5.54 |
| CHEMBL4546301 | — | — | 1 | 5.54 |
| CHEMBL4462800 | — | — | 1 | 5.53 |
| CHEMBL4463864 | — | — | 1 | 5.52 |
| CHEMBL4444119 | — | — | 1 | 5.42 |
| CHEMBL4555770 | — | — | 1 | 5.41 |
| CHEMBL4574304 | — | — | 1 | 5.38 |
| CHEMBL4571914 | — | — | 1 | 5.34 |
| CHEMBL4465764 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4554778 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4540395 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL4483392 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4582207 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL4549506 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL4567470 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL4451303 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL4442891 | — | Ki | = | 557.0 | nM | 6.25 |
| CHEMBL4555393 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL4469103 | — | Ki | = | 1310.0 | nM | 5.88 |
| CHEMBL4465423 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL4534266 | — | Ki | = | 1590.0 | nM | 5.80 |
| CHEMBL4518442 | — | Ki | = | 1840.0 | nM | 5.74 |
| CHEMBL4556251 | — | Ki | = | 2130.0 | nM | 5.67 |
| CHEMBL4450570 | — | Ki | = | 2120.0 | nM | 5.67 |
| CHEMBL4474238 | — | Ki | = | 2250.0 | nM | 5.65 |
| CHEMBL4449715 | — | Ki | = | 2420.0 | nM | 5.62 |
| CHEMBL4515367 | — | Ki | = | 2480.0 | nM | 5.61 |
| CHEMBL4464931 | — | Ki | = | 2580.0 | nM | 5.59 |
| CHEMBL4469213 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL4465460 | — | Ki | = | 2850.0 | nM | 5.54 |
| CHEMBL4556578 | — | Ki | = | 2910.0 | nM | 5.54 |
| CHEMBL4546301 | — | Ki | = | 2920.0 | nM | 5.54 |
| CHEMBL4462800 | — | Ki | = | 2940.0 | nM | 5.53 |
| CHEMBL4463864 | — | Ki | = | 3050.0 | nM | 5.52 |
| CHEMBL4444119 | — | Ki | = | 3830.0 | nM | 5.42 |
| CHEMBL4555770 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL4574304 | — | Ki | = | 4210.0 | nM | 5.38 |
| CHEMBL4571914 | — | Ki | = | 4520.0 | nM | 5.34 |
| CHEMBL4465764 | — | Ki | = | 4960.0 | nM | 5.30 |
| CHEMBL4456327 | — | Ki | = | 5080.0 | nM | 5.29 |
| CHEMBL4461040 | — | Ki | = | 5630.0 | nM | 5.25 |
| CHEMBL3827973 | — | Ki | = | 6040.0 | nM | 5.22 |
| CHEMBL4444501 | — | Ki | = | 6170.0 | nM | 5.21 |
| CHEMBL4535141 | — | Ki | = | 7110.0 | nM | 5.15 |
| CHEMBL4446062 | — | Ki | = | 9610.0 | nM | 5.02 |
| CHEMBL4467813 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4457067 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4581583 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4449829 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4443627 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4564018 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4470777 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4470386 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4476672 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4450675 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4447494 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4463900 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4472428 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4471953 | — | Ki | > | 1000.0 | nM | - |