Assay Detail
Binding
CHEMBL644773
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Binding affinity for A2-adenosine receptor by the displacement of specific [3H]-CGS- binding in rat striatal membranes was determined
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 6.82 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL610426 | — | — | 1 | 8.21 |
| CHEMBL2113613 | — | — | 1 | 8.14 |
| CHEMBL464859 | NECA | — | 1 | 7.99 |
| CHEMBL261482 | — | — | 1 | 7.87 |
| CHEMBL2113567 | — | — | 1 | 7.75 |
| CHEMBL2113565 | — | — | 1 | 7.72 |
| CHEMBL2113612 | — | — | 1 | 7.68 |
| CHEMBL2113570 | — | — | 1 | 7.62 |
| CHEMBL2113569 | — | — | 1 | 7.50 |
| CHEMBL2113638 | — | — | 1 | 7.46 |
| CHEMBL2113611 | — | — | 1 | 7.42 |
| CHEMBL610710 | — | — | 1 | 7.26 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.25 |
| CHEMBL2113620 | — | — | 1 | 7.19 |
| CHEMBL519809 | — | — | 1 | 7.17 |
| CHEMBL3351031 | — | — | 1 | 7.08 |
| CHEMBL2113614 | — | — | 1 | 7.02 |
| CHEMBL608761 | — | — | 1 | 7.00 |
| CHEMBL605866 | — | — | 1 | 6.92 |
| CHEMBL3351032 | — | — | 1 | 6.72 |
| CHEMBL133566 | — | — | 1 | 6.71 |
| CHEMBL2113639 | — | — | 1 | 6.59 |
| CHEMBL1256785 | — | — | 1 | 6.38 |
| CHEMBL2113618 | — | — | 1 | 6.37 |
| CHEMBL610143 | — | — | 1 | 6.36 |
| CHEMBL2113617 | — | — | 1 | 6.25 |
| CHEMBL2113571 | — | — | 1 | 6.24 |
| CHEMBL608762 | — | — | 1 | 6.24 |
| CHEMBL49843 | — | — | 1 | 6.22 |
| CHEMBL2113610 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL610426 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL2113613 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL464859 | NECA | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL261482 | — | Ki | = | 13.4 | nM | 7.87 |
| CHEMBL2113567 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL2113565 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2113612 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2113570 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2113569 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2113638 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2113611 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL610710 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL119709 | IB-MECA | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2113620 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL519809 | — | Ki | = | 66.8 | nM | 7.17 |
| CHEMBL3351031 | — | Ki | = | 83.5 | nM | 7.08 |
| CHEMBL2113614 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL608761 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL605866 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3351032 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL133566 | — | Ki | = | 197.0 | nM | 6.71 |
| CHEMBL2113639 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL1256785 | — | Ki | = | 415.0 | nM | 6.38 |
| CHEMBL2113618 | — | Ki | = | 423.0 | nM | 6.37 |
| CHEMBL610143 | — | Ki | = | 441.0 | nM | 6.36 |
| CHEMBL2113617 | — | Ki | = | 559.0 | nM | 6.25 |
| CHEMBL2113571 | — | Ki | = | 574.0 | nM | 6.24 |
| CHEMBL608762 | — | Ki | = | 574.0 | nM | 6.24 |
| CHEMBL49843 | — | Ki | = | 597.0 | nM | 6.22 |
| CHEMBL2113610 | — | Ki | = | 609.0 | nM | 6.21 |
| CHEMBL609830 | — | Ki | = | 794.0 | nM | 6.10 |
| CHEMBL610996 | — | Ki | = | 988.0 | nM | 6.00 |
| CHEMBL609245 | — | Ki | = | 1590.0 | nM | 5.80 |
| CHEMBL608653 | — | Ki | = | 1650.0 | nM | 5.78 |
| CHEMBL609642 | — | Ki | = | 2460.0 | nM | 5.61 |
| CHEMBL609923 | — | Ki | = | 2730.0 | nM | 5.56 |
| CHEMBL610429 | — | Ki | = | 9070.0 | nM | 5.04 |