Assay Detail
Binding
CHEMBL637899
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to A1 adenosine receptor from rat cortical membrane in presence of [3H]R-(phenylisopropyl)-adenosine
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of deazaxanthines: analogs of potent A1- and A2-adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 6.00 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL158507 | — | — | 1 | 8.00 |
| CHEMBL289413 | — | — | 1 | 7.89 |
| CHEMBL40386 | — | — | 1 | 7.58 |
| CHEMBL35415 | — | — | 1 | 7.41 |
| CHEMBL38528 | — | — | 1 | 7.33 |
| CHEMBL274855 | — | — | 1 | 7.17 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.05 |
| CHEMBL284991 | — | — | 1 | 7.01 |
| CHEMBL36683 | — | — | 1 | 6.96 |
| CHEMBL37247 | — | — | 1 | 6.89 |
| CHEMBL289474 | — | — | 1 | 6.78 |
| CHEMBL39932 | — | — | 1 | 6.66 |
| CHEMBL39646 | — | — | 1 | 6.57 |
| CHEMBL9069 | — | — | 1 | 6.52 |
| CHEMBL38505 | — | — | 1 | 6.36 |
| CHEMBL285294 | — | — | 1 | 6.25 |
| CHEMBL282993 | — | — | 1 | 6.19 |
| CHEMBL157655 | — | — | 1 | 6.16 |
| CHEMBL38755 | — | — | 1 | 5.77 |
| CHEMBL22178 | — | — | 1 | 5.64 |
| CHEMBL418243 | — | — | 1 | 5.64 |
| CHEMBL39898 | — | — | 1 | 5.58 |
| CHEMBL288574 | — | — | 1 | 5.54 |
| CHEMBL38301 | — | — | 1 | 5.51 |
| CHEMBL38297 | — | — | 1 | 5.44 |
| CHEMBL26897 | — | — | 1 | 5.41 |
| CHEMBL38370 | — | — | 1 | 5.27 |
| CHEMBL278332 | — | — | 1 | 5.16 |
| CHEMBL286070 | — | — | 1 | 5.04 |
| CHEMBL38811 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL158507 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL289413 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL40386 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL35415 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL38528 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL274855 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL284991 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL36683 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL37247 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL289474 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL39932 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL39646 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL9069 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL38505 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL285294 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL282993 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL157655 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL38755 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL22178 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL418243 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL39898 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL288574 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL38301 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL38297 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL26897 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL38370 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL278332 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL286070 | — | Ki | = | 9200.0 | nM | 5.04 |
| CHEMBL38811 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL39986 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL21053 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL284855 | — | Ki | = | 32000.0 | nM | 4.50 |
| CHEMBL1250 | 1-METHYLXANTHINE | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL113 | CAFFEINE | Ki | = | 41000.0 | nM | 4.39 |
| CHEMBL39852 | — | Ki | = | 43000.0 | nM | 4.37 |
| CHEMBL40120 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL37219 | — | Ki | > | 30000.0 | nM | - |