Assay Detail
Binding
CHEMBL642181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A2A receptor in rat striatal membranes using [3H]-CGS- 21680.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| 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 | 32 | 6.13 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 7.99 |
| CHEMBL2113550 | — | — | 1 | 7.78 |
| CHEMBL383548 | — | — | 1 | 7.58 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.25 |
| CHEMBL204820 | — | — | 1 | 7.23 |
| CHEMBL205058 | — | — | 1 | 6.62 |
| CHEMBL610394 | — | — | 1 | 6.59 |
| CHEMBL379472 | — | — | 1 | 6.58 |
| CHEMBL203933 | — | — | 1 | 6.55 |
| CHEMBL608327 | — | — | 1 | 6.33 |
| CHEMBL380914 | — | — | 1 | 6.25 |
| CHEMBL426669 | — | — | 1 | 6.17 |
| CHEMBL2113540 | — | — | 1 | 6.13 |
| CHEMBL202249 | — | — | 1 | 6.10 |
| CHEMBL202690 | — | — | 1 | 6.05 |
| CHEMBL437315 | — | — | 1 | 6.04 |
| CHEMBL610112 | — | — | 1 | 6.01 |
| CHEMBL203812 | — | — | 1 | 5.98 |
| CHEMBL265587 | — | — | 1 | 5.93 |
| CHEMBL204651 | — | — | 1 | 5.80 |
| CHEMBL203667 | — | — | 1 | 5.78 |
| CHEMBL426847 | — | — | 1 | 5.75 |
| CHEMBL377291 | — | — | 1 | 5.73 |
| CHEMBL437506 | — | — | 1 | 5.71 |
| CHEMBL413046 | — | — | 1 | 5.63 |
| CHEMBL203958 | — | — | 1 | 5.60 |
| CHEMBL383268 | — | — | 1 | 5.58 |
| CHEMBL437503 | — | — | 1 | 5.53 |
| CHEMBL202722 | — | — | 1 | 5.45 |
| CHEMBL206265 | — | — | 1 | 5.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL2113550 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL383548 | — | Ki | = | 26.6 | nM | 7.58 |
| CHEMBL119709 | IB-MECA | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL204820 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL205058 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL610394 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL379472 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL203933 | — | Ki | = | 279.0 | nM | 6.55 |
| CHEMBL608327 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL380914 | — | Ki | = | 557.0 | nM | 6.25 |
| CHEMBL426669 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL2113540 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL202249 | — | Ki | = | 799.0 | nM | 6.10 |
| CHEMBL202690 | — | Ki | = | 884.0 | nM | 6.05 |
| CHEMBL437315 | — | Ki | = | 917.0 | nM | 6.04 |
| CHEMBL610112 | — | Ki | = | 977.0 | nM | 6.01 |
| CHEMBL203812 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL265587 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL204651 | — | Ki | = | 1570.0 | nM | 5.80 |
| CHEMBL203667 | — | Ki | = | 1670.0 | nM | 5.78 |
| CHEMBL426847 | — | Ki | = | 1793.0 | nM | 5.75 |
| CHEMBL377291 | — | Ki | = | 1860.0 | nM | 5.73 |
| CHEMBL437506 | — | Ki | = | 1960.0 | nM | 5.71 |
| CHEMBL413046 | — | Ki | = | 2330.0 | nM | 5.63 |
| CHEMBL203958 | — | Ki | = | 2530.0 | nM | 5.60 |
| CHEMBL383268 | — | Ki | = | 2650.0 | nM | 5.58 |
| CHEMBL437503 | — | Ki | = | 2970.0 | nM | 5.53 |
| CHEMBL202722 | — | Ki | = | 3580.0 | nM | 5.45 |
| CHEMBL206265 | — | Ki | = | 7130.0 | nM | 5.15 |
| CHEMBL204246 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL381917 | — | Ki | = | 48700.0 | nM | 4.31 |