Assay Detail
Binding
CHEMBL649108
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Ability to inhibit binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptor in rat cerebral cortical membranes
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 5.03 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26350 | — | — | 1 | 6.30 |
| CHEMBL25223 | — | — | 1 | 6.22 |
| CHEMBL157655 | — | — | 1 | 6.16 |
| CHEMBL418193 | — | — | 1 | 6.00 |
| CHEMBL284860 | — | — | 1 | 5.72 |
| CHEMBL24774 | — | — | 1 | 5.70 |
| CHEMBL417834 | — | — | 1 | 5.58 |
| CHEMBL24444 | — | — | 1 | 5.51 |
| CHEMBL416013 | — | — | 1 | 5.48 |
| CHEMBL24759 | — | — | 1 | 5.22 |
| CHEMBL278332 | — | — | 1 | 5.16 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | — | 1 | 5.16 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | — | 1 | 5.10 |
| CHEMBL26606 | — | — | 1 | 5.05 |
| CHEMBL286785 | — | — | 1 | 5.00 |
| CHEMBL24049 | — | — | 1 | 4.92 |
| CHEMBL26119 | — | — | 1 | 4.92 |
| CHEMBL26176 | — | — | 1 | 4.89 |
| CHEMBL24445 | — | — | 1 | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.85 |
| CHEMBL24107 | — | — | 1 | 4.82 |
| CHEMBL26406 | — | — | 1 | 4.75 |
| CHEMBL25096 | — | — | 1 | 4.72 |
| CHEMBL26455 | — | — | 1 | 4.68 |
| CHEMBL417654 | — | — | 1 | 4.62 |
| CHEMBL24289 | — | — | 1 | 4.48 |
| CHEMBL286680 | — | — | 1 | 4.42 |
| CHEMBL25373 | — | — | 1 | 4.40 |
| CHEMBL282038 | — | — | 1 | 4.35 |
| CHEMBL25427 | — | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26350 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL25223 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL157655 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL418193 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL284860 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL24774 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL417834 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL24444 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL416013 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL24759 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL278332 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL23903 | 7-CHLOROETHYLTHEOPHYLLINE | Ki | = | 8000.0 | nM | 5.10 |
| CHEMBL26606 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL286785 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL24049 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL26119 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL26176 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL24445 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL24107 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL26406 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL25096 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL26455 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL417654 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL24289 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL286680 | — | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL25373 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL282038 | — | Ki | = | 45000.0 | nM | 4.35 |
| CHEMBL25427 | — | Ki | = | 47000.0 | nM | 4.33 |
| CHEMBL113 | CAFFEINE | Ki | = | 55000.0 | nM | 4.26 |
| CHEMBL26061 | — | Ki | = | 60000.0 | nM | 4.22 |
| CHEMBL25303 | — | Ki | = | 85000.0 | nM | 4.07 |
| CHEMBL699 | ETOFYLLINE | Ki | = | 105000.0 | nM | - |