Assay Detail
Binding
CHEMBL645451
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Binding affinity to A2 adenosine receptor from rat striatal membrane in presence of [3H]5'-(N-ethylcarboximido)-adenosine
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
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 | 5.37 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL26897 | — | — | 1 | 7.03 |
| CHEMBL158507 | — | — | 1 | 6.75 |
| CHEMBL39898 | — | — | 1 | 6.58 |
| CHEMBL282993 | — | — | 1 | 6.54 |
| CHEMBL289413 | — | — | 1 | 6.35 |
| CHEMBL38528 | — | — | 1 | 6.29 |
| CHEMBL289474 | — | — | 1 | 6.19 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.08 |
| CHEMBL39932 | — | — | 1 | 6.00 |
| CHEMBL39646 | — | — | 1 | 5.96 |
| CHEMBL35415 | — | — | 1 | 5.92 |
| CHEMBL285294 | — | — | 1 | 5.75 |
| CHEMBL274855 | — | — | 1 | 5.72 |
| CHEMBL284991 | — | — | 1 | 5.70 |
| CHEMBL9069 | — | — | 1 | 5.66 |
| CHEMBL38505 | — | — | 1 | 5.29 |
| CHEMBL36683 | — | — | 1 | 5.28 |
| CHEMBL157655 | — | — | 1 | 5.18 |
| CHEMBL278332 | — | — | 1 | 5.00 |
| CHEMBL38301 | — | — | 1 | 4.92 |
| CHEMBL38370 | — | — | 1 | 4.92 |
| CHEMBL418243 | — | — | 1 | 4.89 |
| CHEMBL38297 | — | — | 1 | 4.85 |
| CHEMBL22178 | — | — | 1 | 4.82 |
| CHEMBL37247 | — | — | 1 | 4.80 |
| CHEMBL38755 | — | — | 1 | 4.75 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.72 |
| CHEMBL21053 | — | — | 1 | 4.60 |
| CHEMBL39986 | — | — | 1 | 4.48 |
| CHEMBL288574 | — | — | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL26897 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL158507 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL39898 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL282993 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL289413 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL38528 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL289474 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL39932 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL39646 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL35415 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL285294 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL274855 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL284991 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL9069 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL38505 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL36683 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL157655 | — | Ki | = | 6600.0 | nM | 5.18 |
| CHEMBL278332 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL38301 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL38370 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL418243 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL38297 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL22178 | — | Ki | = | 15000.0 | nM | 4.82 |
| CHEMBL37247 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL38755 | — | Ki | = | 18000.0 | nM | 4.75 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL21053 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL39986 | — | Ki | = | 33000.0 | nM | 4.48 |
| CHEMBL288574 | — | Ki | = | 34000.0 | nM | 4.47 |
| CHEMBL38811 | — | Ki | = | 40000.0 | nM | 4.40 |
| CHEMBL113 | CAFFEINE | Ki | = | 43000.0 | nM | 4.37 |
| CHEMBL1250 | 1-METHYLXANTHINE | Ki | = | 47000.0 | nM | 4.33 |
| CHEMBL284855 | — | Ki | = | 72000.0 | nM | 4.14 |
| CHEMBL286070 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL40120 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL39852 | — | Ki | > | 250000.0 | nM | - |
| CHEMBL40386 | — | Ki | > | 500.0 | nM | - |
| CHEMBL37219 | — | Ki | > | 100000.0 | nM | - |