Assay Detail
Binding
CHEMBL639739
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Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes.
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
C2,N6-disubstituted adenosines: synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 49 | 6.97 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489640 | — | — | 1 | 9.38 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.93 |
| CHEMBL45891 | — | — | 1 | 8.85 |
| CHEMBL2113423 | — | — | 1 | 8.49 |
| CHEMBL603785 | — | — | 1 | 8.30 |
| CHEMBL2181971 | — | — | 1 | 8.28 |
| CHEMBL193692 | — | — | 1 | 8.17 |
| CHEMBL603995 | — | — | 1 | 8.11 |
| CHEMBL604202 | — | — | 1 | 8.08 |
| CHEMBL285819 | — | — | 1 | 8.03 |
| CHEMBL605035 | — | — | 1 | 7.91 |
| CHEMBL477 | ADENOSINE | 4.0 | 1 | 7.89 |
| CHEMBL605859 | — | — | 1 | 7.74 |
| CHEMBL604830 | — | — | 1 | 7.73 |
| CHEMBL603991 | — | — | 1 | 7.72 |
| CHEMBL606496 | — | — | 1 | 7.71 |
| CHEMBL132960 | — | — | 1 | 7.62 |
| CHEMBL606507 | — | — | 1 | 7.52 |
| CHEMBL605235 | — | — | 1 | 7.43 |
| CHEMBL604619 | — | — | 1 | 7.30 |
| CHEMBL606071 | — | — | 1 | 7.27 |
| CHEMBL604861 | — | — | 1 | 7.21 |
| CHEMBL603786 | — | — | 1 | 7.17 |
| CHEMBL1688963 | ISOGUANOSINE | — | 1 | 7.03 |
| CHEMBL605068 | — | — | 1 | 7.02 |
| CHEMBL388757 | N6-BENZYLADENOSINE | — | 1 | 6.92 |
| CHEMBL2094089 | — | — | 1 | 6.85 |
| CHEMBL603568 | — | — | 1 | 6.82 |
| CHEMBL605450 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489640 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL139000 | (R)-PIA | Ki | = | 1.17 | nM | 8.93 |
| CHEMBL45891 | — | Ki | = | 1.42 | nM | 8.85 |
| CHEMBL2113423 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL603785 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2181971 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL193692 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL603995 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL604202 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL285819 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL605035 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL477 | ADENOSINE | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL605859 | — | Ki | = | 18.1 | nM | 7.74 |
| CHEMBL604830 | — | Ki | = | 18.5 | nM | 7.73 |
| CHEMBL603991 | — | Ki | = | 19.2 | nM | 7.72 |
| CHEMBL606496 | — | Ki | = | 19.3 | nM | 7.71 |
| CHEMBL132960 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL606507 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL605235 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL604619 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL606071 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL604861 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL603786 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1688963 | ISOGUANOSINE | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL605068 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL388757 | N6-BENZYLADENOSINE | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2094089 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL603568 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL605450 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL603992 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL605661 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL606494 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL603353 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL1256672 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL603787 | — | Ki | = | 840.0 | nM | 6.08 |
| CHEMBL605025 | — | Ki | = | 1320.0 | nM | 5.88 |
| CHEMBL604206 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL605451 | — | Ki | = | 1620.0 | nM | 5.79 |
| CHEMBL604616 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL604621 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL605024 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL603994 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL603352 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL604409 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL603572 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL604825 | — | Ki | = | 10300.0 | nM | 4.99 |
| CHEMBL605238 | — | Ki | = | 18400.0 | nM | 4.74 |
| CHEMBL341031 | — | Ki | = | 45000.0 | nM | 4.35 |