Assay Detail
Binding
CHEMBL639433
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]R-PIA.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 6.62 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202722 | — | — | 1 | 8.23 |
| CHEMBL464859 | NECA | — | 1 | 8.20 |
| CHEMBL383548 | — | — | 1 | 7.80 |
| CHEMBL204820 | — | — | 1 | 7.66 |
| CHEMBL379472 | — | — | 1 | 7.53 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.27 |
| CHEMBL203812 | — | — | 1 | 7.14 |
| CHEMBL203960 | — | — | 1 | 7.12 |
| CHEMBL205058 | — | — | 1 | 7.06 |
| CHEMBL203958 | — | — | 1 | 7.05 |
| CHEMBL380914 | — | — | 1 | 7.05 |
| CHEMBL204246 | — | — | 1 | 6.99 |
| CHEMBL383268 | — | — | 1 | 6.89 |
| CHEMBL202690 | — | — | 1 | 6.84 |
| CHEMBL426847 | — | — | 1 | 6.77 |
| CHEMBL437315 | — | — | 1 | 6.68 |
| CHEMBL610394 | — | — | 1 | 6.61 |
| CHEMBL426669 | — | — | 1 | 6.60 |
| CHEMBL2113540 | — | — | 1 | 6.54 |
| CHEMBL377291 | — | — | 1 | 6.38 |
| CHEMBL413046 | — | — | 1 | 6.37 |
| CHEMBL203933 | — | — | 1 | 6.36 |
| CHEMBL265587 | — | — | 1 | 6.34 |
| CHEMBL437503 | — | — | 1 | 6.27 |
| CHEMBL2113550 | — | — | 1 | 6.14 |
| CHEMBL202249 | — | — | 1 | 6.12 |
| CHEMBL206116 | — | — | 1 | 6.09 |
| CHEMBL608327 | — | — | 1 | 6.09 |
| CHEMBL610112 | — | — | 1 | 6.04 |
| CHEMBL437506 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202722 | — | Ki | = | 5.92 | nM | 8.23 |
| CHEMBL464859 | NECA | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL383548 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL204820 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL379472 | — | Ki | = | 29.4 | nM | 7.53 |
| CHEMBL119709 | IB-MECA | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL203812 | — | Ki | = | 72.7 | nM | 7.14 |
| CHEMBL203960 | — | Ki | = | 75.1 | nM | 7.12 |
| CHEMBL205058 | — | Ki | = | 86.4 | nM | 7.06 |
| CHEMBL203958 | — | Ki | = | 89.1 | nM | 7.05 |
| CHEMBL380914 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL204246 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL383268 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL202690 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL426847 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL437315 | — | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL610394 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL426669 | — | Ki | = | 252.0 | nM | 6.60 |
| CHEMBL2113540 | — | Ki | = | 292.0 | nM | 6.54 |
| CHEMBL377291 | — | Ki | = | 419.0 | nM | 6.38 |
| CHEMBL413046 | — | Ki | = | 428.0 | nM | 6.37 |
| CHEMBL203933 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL265587 | — | Ki | = | 453.0 | nM | 6.34 |
| CHEMBL437503 | — | Ki | = | 537.0 | nM | 6.27 |
| CHEMBL2113550 | — | Ki | = | 725.0 | nM | 6.14 |
| CHEMBL202249 | — | Ki | = | 761.0 | nM | 6.12 |
| CHEMBL206116 | — | Ki | = | 814.0 | nM | 6.09 |
| CHEMBL608327 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL610112 | — | Ki | = | 901.0 | nM | 6.04 |
| CHEMBL437506 | — | Ki | = | 1170.0 | nM | 5.93 |
| CHEMBL381917 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL204651 | — | Ki | = | 1770.0 | nM | 5.75 |
| CHEMBL206265 | — | Ki | = | 2040.0 | nM | 5.69 |
| CHEMBL204190 | — | Ki | = | 4790.0 | nM | 5.32 |
| CHEMBL203667 | — | Ki | = | 14400.0 | nM | 4.84 |