Assay Detail
Binding
CHEMBL640353
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A1 receptor using N6-[3H]cyclohexyladenosine as radioligand in guinea pig forebrain membranes
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Subcellular | Brain membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 7.53 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL489640 | — | — | 1 | 9.49 |
| CHEMBL604242 | — | — | 1 | 9.12 |
| CHEMBL605440 | — | — | 1 | 9.12 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 8.89 |
| CHEMBL260167 | — | — | 1 | 8.72 |
| CHEMBL84363 | — | — | 1 | 8.52 |
| CHEMBL604609 | — | — | 1 | 8.48 |
| CHEMBL366808 | — | — | 1 | 8.47 |
| CHEMBL172950 | — | — | 1 | 8.46 |
| CHEMBL407273 | — | — | 1 | 8.42 |
| CHEMBL438025 | — | — | 1 | 8.37 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.19 |
| CHEMBL104491 | — | — | 1 | 8.15 |
| CHEMBL320872 | — | — | 1 | 8.00 |
| CHEMBL264033 | — | — | 1 | 7.96 |
| CHEMBL369602 | — | — | 1 | 7.89 |
| CHEMBL605273 | — | — | 1 | 7.77 |
| CHEMBL143622 | — | — | 1 | 7.72 |
| CHEMBL605488 | — | — | 1 | 7.70 |
| CHEMBL106548 | — | — | 1 | 7.66 |
| CHEMBL173220 | — | — | 1 | 7.64 |
| CHEMBL347787 | — | — | 1 | 7.60 |
| CHEMBL424949 | — | — | 1 | 7.60 |
| CHEMBL368658 | — | — | 1 | 7.51 |
| CHEMBL316545 | — | — | 1 | 7.39 |
| CHEMBL369437 | — | — | 1 | 7.31 |
| CHEMBL142410 | — | — | 1 | 7.31 |
| CHEMBL603777 | — | — | 1 | 7.16 |
| CHEMBL606110 | — | — | 1 | 7.14 |
| CHEMBL356458 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL489640 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL604242 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL605440 | — | Ki | = | 0.75 | nM | 9.12 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL260167 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL84363 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL604609 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL366808 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL172950 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL407273 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL438025 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL104491 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL320872 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL264033 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL369602 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL605273 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL143622 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL605488 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL106548 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL173220 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL347787 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL424949 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL368658 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL316545 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL369437 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL142410 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL603777 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL606110 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL356458 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL2373406 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL176320 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL367884 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL367198 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL33722 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL132441 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL173657 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL174120 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL55839 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL367240 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL172008 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL113 | CAFFEINE | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL172007 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL354334 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL171237 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL170590 | — | Ki | > | 100000.0 | nM | - |