Assay Detail
Binding
CHEMBL637553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.62 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.52 |
| CHEMBL284969 | — | — | 1 | 9.46 |
| CHEMBL139000 | (R)-PIA | — | 1 | 9.22 |
| CHEMBL251997 | — | — | 1 | 8.74 |
| CHEMBL2113388 | — | — | 1 | 8.33 |
| CHEMBL400189 | — | — | 1 | 8.02 |
| CHEMBL420705 | (S)-PIA | — | 1 | 7.93 |
| CHEMBL464859 | NECA | — | 1 | 7.85 |
| CHEMBL66393 | — | — | 1 | 7.73 |
| CHEMBL285819 | — | — | 1 | 7.70 |
| CHEMBL444550 | — | — | 1 | 7.70 |
| CHEMBL119709 | IB-MECA | — | 1 | 7.48 |
| CHEMBL603977 | — | — | 1 | 7.30 |
| CHEMBL2113418 | — | — | 1 | 6.85 |
| CHEMBL605034 | — | — | 1 | 6.59 |
| CHEMBL606495 | — | — | 1 | 6.27 |
| CHEMBL73809 | — | — | 1 | 6.13 |
| CHEMBL480143 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL284969 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL139000 | (R)-PIA | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL251997 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2113388 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL400189 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL420705 | (S)-PIA | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL464859 | NECA | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL66393 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL285819 | — | Ki | = | 20.2 | nM | 7.70 |
| CHEMBL444550 | — | Ki | = | 20.1 | nM | 7.70 |
| CHEMBL119709 | IB-MECA | Ki | = | 33.1 | nM | 7.48 |
| CHEMBL603977 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2113418 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL605034 | — | Ki | = | 254.0 | nM | 6.59 |
| CHEMBL606495 | — | Ki | = | 533.0 | nM | 6.27 |
| CHEMBL73809 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL480143 | — | Ki | = | 49500.0 | nM | 4.30 |