Assay Detail
Binding
CHEMBL646320
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Binding affinity against adenosine A2 receptor using N-[3H]-ethyladenosin-5''-uronamide as radioligand in rat striatal membranes.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 37 | 5.84 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL366808 | — | — | 1 | 6.68 |
| CHEMBL172950 | — | — | 1 | 6.48 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 6.42 |
| CHEMBL84363 | — | — | 1 | 6.37 |
| CHEMBL407273 | — | — | 1 | 6.36 |
| CHEMBL438025 | — | — | 1 | 6.32 |
| CHEMBL55839 | — | — | 1 | 6.28 |
| CHEMBL143622 | — | — | 1 | 6.24 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.23 |
| CHEMBL356458 | — | — | 1 | 6.23 |
| CHEMBL173220 | — | — | 1 | 6.00 |
| CHEMBL2373406 | — | — | 1 | 6.00 |
| CHEMBL320872 | — | — | 1 | 5.96 |
| CHEMBL264033 | — | — | 1 | 5.92 |
| CHEMBL316545 | — | — | 1 | 5.92 |
| CHEMBL176320 | — | — | 1 | 5.92 |
| CHEMBL347787 | — | — | 1 | 5.92 |
| CHEMBL171237 | — | — | 1 | 5.92 |
| CHEMBL142410 | — | — | 1 | 5.82 |
| CHEMBL104491 | — | — | 1 | 5.80 |
| CHEMBL132441 | — | — | 1 | 5.77 |
| CHEMBL33722 | — | — | 1 | 5.72 |
| CHEMBL424949 | — | — | 1 | 5.66 |
| CHEMBL174120 | — | — | 1 | 5.64 |
| CHEMBL368658 | — | — | 1 | 5.64 |
| CHEMBL369602 | — | — | 1 | 5.29 |
| CHEMBL369437 | — | — | 1 | 5.22 |
| CHEMBL367884 | — | — | 1 | 5.22 |
| CHEMBL367198 | — | — | 1 | 4.92 |
| CHEMBL173657 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL366808 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL172950 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL84363 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL407273 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL438025 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL55839 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL143622 | — | Ki | = | 570.0 | nM | 6.24 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL356458 | — | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL173220 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL2373406 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL320872 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL171237 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL347787 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL264033 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL176320 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL316545 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL142410 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL104491 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL132441 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL33722 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL424949 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL174120 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL368658 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL369602 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL369437 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL367884 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL367198 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL173657 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL113 | CAFFEINE | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL172007 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL367240 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL106548 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL172008 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL170590 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL354334 | — | Ki | > | 100000.0 | nM | - |