Assay Detail
Binding
CHEMBL2187072
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Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter
36
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Medicinal chemistry of A₃ adenosine receptor modulators: pharmacological activities and therapeutic implications.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 6.29 | 7.80 |
| IC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL186113 | GW-328267 | 1.0 | 2 | 7.80 |
| CHEMBL88147 | — | — | 1 | 7.60 |
| CHEMBL332091 | — | — | 1 | 7.00 |
| CHEMBL322250 | — | — | 1 | 6.92 |
| CHEMBL2181971 | — | — | 1 | 6.84 |
| CHEMBL122396 | — | — | 1 | 6.67 |
| CHEMBL2181965 | — | — | 1 | 6.33 |
| CHEMBL193692 | — | — | 1 | 6.29 |
| CHEMBL198779 | — | — | 1 | 6.08 |
| CHEMBL175543 | — | — | 1 | 5.64 |
| CHEMBL2181970 | — | — | 1 | 5.62 |
| CHEMBL193421 | — | — | 1 | 5.60 |
| CHEMBL2181977 | — | — | 1 | 5.09 |
| CHEMBL2181969 | — | — | 1 | 4.53 |
| CHEMBL113420 | — | — | 1 | - |
| CHEMBL123705 | — | — | 1 | - |
| CHEMBL99178 | — | — | 1 | - |
| CHEMBL211862 | — | — | 1 | - |
| CHEMBL363419 | — | — | 1 | - |
| CHEMBL589080 | — | — | 1 | - |
| CHEMBL2181975 | — | — | 1 | - |
| CHEMBL2181972 | — | — | 1 | - |
| CHEMBL339066 | — | — | 1 | - |
| CHEMBL398587 | — | — | 1 | - |
| CHEMBL1625681 | — | — | 1 | - |
| CHEMBL371404 | — | — | 1 | - |
| CHEMBL188035 | — | — | 1 | - |
| CHEMBL2181973 | — | — | 1 | - |
| CHEMBL2181976 | — | — | 1 | - |
| CHEMBL434534 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL186113 | GW-328267 | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL88147 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL332091 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL322250 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL2181971 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL122396 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL2181965 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL193692 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL198779 | — | Ki | = | 833.0 | nM | 6.08 |
| CHEMBL175543 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL2181970 | — | Ki | = | 2370.0 | nM | 5.62 |
| CHEMBL193421 | — | Ki | = | 2530.0 | nM | 5.60 |
| CHEMBL2181977 | — | Ki | = | 8050.0 | nM | 5.09 |
| CHEMBL2181969 | — | Ki | = | 29800.0 | nM | 4.53 |
| CHEMBL2181966 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL2177153 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2181968 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2181967 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2181964 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL113420 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL123705 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL99178 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL211862 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL363419 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL589080 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2181975 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2181972 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL339066 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL398587 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL1625681 | — | Ki | > | 1280.0 | nM | - |
| CHEMBL371404 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL188035 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2181973 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2181976 | — | Ki | > | 826.0 | nM | - |
| CHEMBL434534 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL186113 | GW-328267 | Ki | >= | 1000.0 | nM | - |