Assay Detail
Binding
CHEMBL640367
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Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 7.47 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL334776 | — | — | 1 | 9.64 |
| CHEMBL2112182 | — | — | 1 | 9.52 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.34 |
| CHEMBL604356 | — | — | 1 | 9.33 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | — | 1 | 9.23 |
| CHEMBL284969 | — | — | 1 | 9.22 |
| CHEMBL1512545 | — | — | 1 | 9.07 |
| CHEMBL139000 | (R)-PIA | — | 1 | 8.92 |
| CHEMBL45891 | — | — | 1 | 8.89 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 8.89 |
| CHEMBL268364 | — | — | 1 | 8.62 |
| CHEMBL273671 | — | — | 1 | 8.60 |
| CHEMBL135163 | — | — | 1 | 8.33 |
| CHEMBL2181971 | — | — | 1 | 8.28 |
| CHEMBL464859 | NECA | — | 1 | 8.20 |
| CHEMBL193692 | — | — | 1 | 8.17 |
| CHEMBL262984 | — | — | 1 | 8.16 |
| CHEMBL604202 | — | — | 1 | 8.08 |
| CHEMBL285819 | — | — | 1 | 8.03 |
| CHEMBL19768 | — | — | 1 | 8.00 |
| CHEMBL84545 | — | — | 1 | 7.98 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | — | 1 | 7.96 |
| CHEMBL16687 | CGS-15943 | — | 1 | 7.68 |
| CHEMBL435977 | — | — | 1 | 7.64 |
| CHEMBL72669 | — | — | 1 | 7.55 |
| CHEMBL605668 | — | — | 1 | 7.32 |
| CHEMBL27041 | — | — | 1 | 7.24 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.07 |
| CHEMBL2094089 | — | — | 1 | 6.85 |
| CHEMBL319387 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL334776 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL2112182 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL604356 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL68738 | N6-CYCLOPENTYLADENOSINE | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL284969 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1512545 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL139000 | (R)-PIA | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL45891 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL268364 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL273671 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL135163 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL2181971 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL464859 | NECA | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL193692 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL262984 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL604202 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL285819 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL19768 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL84545 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL16687 | CGS-15943 | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL435977 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL72669 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL605668 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL27041 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL2094089 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL319387 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL2113496 | — | Ki | = | 211.0 | nM | 6.68 |
| CHEMBL1950647 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL303198 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL608320 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL1256672 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL606093 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL8488 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL331372 | CGS-21680 | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL607498 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL72577 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL87459 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL282038 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL113 | CAFFEINE | Ki | = | 29000.0 | nM | 4.54 |