Assay Detail
Binding
CHEMBL4369167
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]I-AB-MECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes
26
Total Activities
26
Compounds Tested
1
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
Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A<sub>3</sub> adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 7.47 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3407784 | — | — | 1 | 9.15 |
| CHEMBL3612932 | — | — | 1 | 8.96 |
| CHEMBL1257013 | — | — | 1 | 8.68 |
| CHEMBL193385 | — | — | 1 | 8.36 |
| CHEMBL2012680 | — | — | 1 | 8.18 |
| CHEMBL4587951 | — | — | 1 | 7.93 |
| CHEMBL4546937 | — | — | 1 | 7.89 |
| CHEMBL4534460 | — | — | 1 | 7.79 |
| CHEMBL4455344 | — | — | 1 | 7.76 |
| CHEMBL4559342 | — | — | 1 | 7.70 |
| CHEMBL4439593 | — | — | 1 | 7.69 |
| CHEMBL4447908 | — | — | 1 | 7.50 |
| CHEMBL4593728 | — | — | 1 | 7.48 |
| CHEMBL4468583 | — | — | 1 | 7.43 |
| CHEMBL4560015 | — | — | 1 | 7.37 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 7.14 |
| CHEMBL4563323 | — | — | 1 | 7.10 |
| CHEMBL4527909 | — | — | 1 | 6.94 |
| CHEMBL3941980 | — | — | 1 | 6.92 |
| CHEMBL4530091 | — | — | 1 | 6.89 |
| CHEMBL2012672 | — | — | 1 | 6.80 |
| CHEMBL2012686 | — | — | 1 | 6.33 |
| CHEMBL1877326 | — | — | 1 | 6.04 |
| CHEMBL4526748 | — | — | 1 | 5.17 |
| CHEMBL392149 | TECADENOSON | 2.0 | 1 | - |
| CHEMBL2163568 | GR-79236 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3407784 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3612932 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1257013 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL193385 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2012680 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4587951 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL4546937 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4534460 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL4455344 | — | Ki | = | 17.4 | nM | 7.76 |
| CHEMBL4559342 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4439593 | — | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL4447908 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4593728 | — | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL4468583 | — | Ki | = | 37.1 | nM | 7.43 |
| CHEMBL4560015 | — | Ki | = | 43.2 | nM | 7.37 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL4563323 | — | Ki | = | 79.2 | nM | 7.10 |
| CHEMBL4527909 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL3941980 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4530091 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL2012672 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL2012686 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL1877326 | — | Ki | = | 915.0 | nM | 6.04 |
| CHEMBL4526748 | — | Ki | = | 6820.0 | nM | 5.17 |
| CHEMBL392149 | TECADENOSON | Ki | - | — | - | |
| CHEMBL2163568 | GR-79236 | Ki | - | — | - |