Assay Detail
Binding
CHEMBL645212
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand
44
Total Activities
41
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
Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 7.15 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 8.89 |
| CHEMBL84363 | — | — | 1 | 8.52 |
| CHEMBL321309 | — | — | 2 | 8.47 |
| CHEMBL84144 | — | — | 2 | 8.46 |
| CHEMBL415321 | — | — | 2 | 8.42 |
| CHEMBL318607 | — | — | 1 | 8.38 |
| CHEMBL318537 | — | — | 1 | 8.26 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 8.19 |
| CHEMBL104491 | — | — | 1 | 8.15 |
| CHEMBL16687 | CGS-15943 | — | 1 | 8.00 |
| CHEMBL320872 | — | — | 1 | 8.00 |
| CHEMBL160704 | — | — | 1 | 7.96 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.96 |
| CHEMBL313780 | — | — | 1 | 7.92 |
| CHEMBL418101 | — | — | 1 | 7.89 |
| CHEMBL320668 | — | — | 1 | 7.89 |
| CHEMBL321507 | — | — | 1 | 7.82 |
| CHEMBL102859 | — | — | 1 | 7.72 |
| CHEMBL106548 | — | — | 1 | 7.66 |
| CHEMBL104189 | — | — | 1 | 7.48 |
| CHEMBL72669 | — | — | 1 | 7.44 |
| CHEMBL316545 | — | — | 1 | 7.39 |
| CHEMBL268071 | — | — | 1 | 7.12 |
| CHEMBL2373406 | — | — | 1 | 7.10 |
| CHEMBL106937 | — | — | 1 | 7.09 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | — | 1 | 7.02 |
| CHEMBL308499 | — | — | 1 | 6.85 |
| CHEMBL320147 | — | — | 1 | 6.43 |
| CHEMBL415323 | — | — | 1 | 6.06 |
| CHEMBL443274 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL84363 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL321309 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL84144 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL415321 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL318607 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL321309 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL415321 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL318537 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL84144 | — | Ki | = | 5.6 | nM | 8.25 |
| 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 |
| CHEMBL16687 | CGS-15943 | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL160704 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL313780 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL320668 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL418101 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL321507 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL102859 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL106548 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL104189 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL72669 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL316545 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL268071 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL2373406 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL106937 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL308499 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL320147 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL415323 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL443274 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL105100 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL102371 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL22099 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL303198 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL320661 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL102372 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL101800 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL113 | CAFFEINE | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL35 | FUROSEMIDE | Ki | > | 100000.0 | nM | - |