Assay Detail
Binding
CHEMBL863396
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]CGS-21680 from human adenosine A2A receptor transfected in HEK293 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.20 | 6.83 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202189 | — | — | 1 | 6.83 |
| CHEMBL203357 | — | — | 1 | 6.80 |
| CHEMBL200072 | — | — | 1 | 6.70 |
| CHEMBL200732 | — | — | 1 | 6.65 |
| CHEMBL200854 | — | — | 1 | 6.54 |
| CHEMBL381868 | — | — | 1 | 6.49 |
| CHEMBL370446 | — | — | 1 | 6.49 |
| CHEMBL200099 | — | — | 1 | 6.37 |
| CHEMBL200407 | — | — | 1 | 6.26 |
| CHEMBL200705 | — | — | 1 | 6.22 |
| CHEMBL381408 | — | — | 1 | 6.04 |
| CHEMBL370187 | — | — | 1 | 5.88 |
| CHEMBL200279 | — | — | 1 | 5.65 |
| CHEMBL199877 | — | — | 1 | 5.56 |
| CHEMBL199541 | — | — | 1 | 5.41 |
| CHEMBL200184 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202189 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL203357 | — | Ki | = | 158.0 | nM | 6.80 |
| CHEMBL200072 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL200732 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL200854 | — | Ki | = | 292.0 | nM | 6.54 |
| CHEMBL381868 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL370446 | — | Ki | = | 326.0 | nM | 6.49 |
| CHEMBL200099 | — | Ki | = | 429.0 | nM | 6.37 |
| CHEMBL200407 | — | Ki | = | 549.0 | nM | 6.26 |
| CHEMBL200705 | — | Ki | = | 604.0 | nM | 6.22 |
| CHEMBL381408 | — | Ki | = | 921.0 | nM | 6.04 |
| CHEMBL370187 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL200279 | — | Ki | = | 2220.0 | nM | 5.65 |
| CHEMBL199877 | — | Ki | = | 2770.0 | nM | 5.56 |
| CHEMBL199541 | — | Ki | = | 3890.0 | nM | 5.41 |
| CHEMBL200184 | — | Ki | = | 4890.0 | nM | 5.31 |