Assay Detail
Binding
CHEMBL646483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A2 receptor in rat striatal membranes using N-[3H]-ethyladenosin-5''-uronamide as radioligand in the presence of 50 nM cyclopentyladenosine
44
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Striatum |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
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 | 6.18 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | — | 1 | 9.14 |
| CHEMBL303198 | — | — | 1 | 8.29 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.68 |
| CHEMBL308499 | — | — | 1 | 7.58 |
| CHEMBL318607 | — | — | 1 | 6.77 |
| CHEMBL321309 | — | — | 2 | 6.68 |
| CHEMBL415321 | — | — | 2 | 6.54 |
| CHEMBL84144 | — | — | 2 | 6.48 |
| CHEMBL52333 | ROLOFYLLINE | 3.0 | 1 | 6.42 |
| CHEMBL313780 | — | — | 1 | 6.39 |
| CHEMBL84363 | — | — | 1 | 6.37 |
| CHEMBL102859 | — | — | 1 | 6.36 |
| CHEMBL318537 | — | — | 1 | 6.36 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.23 |
| CHEMBL320668 | — | — | 1 | 6.16 |
| CHEMBL72669 | — | — | 1 | 6.15 |
| CHEMBL321507 | — | — | 1 | 6.07 |
| CHEMBL104189 | — | — | 1 | 6.06 |
| CHEMBL2373406 | — | — | 1 | 6.00 |
| CHEMBL320872 | — | — | 1 | 5.96 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | — | 1 | 5.92 |
| CHEMBL160704 | — | — | 1 | 5.92 |
| CHEMBL316545 | — | — | 1 | 5.92 |
| CHEMBL268071 | — | — | 1 | 5.89 |
| CHEMBL104491 | — | — | 1 | 5.80 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 5.64 |
| CHEMBL106937 | — | — | 1 | 5.57 |
| CHEMBL418101 | — | — | 1 | 5.29 |
| CHEMBL101800 | — | — | 1 | 5.20 |
| CHEMBL102371 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16687 | CGS-15943 | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL303198 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL308499 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL318607 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL321309 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL415321 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL84144 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL52333 | ROLOFYLLINE | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL313780 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL84363 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL318537 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL102859 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL415321 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL321309 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL84144 | — | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 590.0 | nM | 6.23 |
| CHEMBL320668 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL72669 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL321507 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL104189 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL2373406 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL320872 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL160704 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL316545 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL268071 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL104491 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL106937 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL418101 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL101800 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL102371 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL113 | CAFFEINE | Ki | = | 27000.0 | nM | 4.57 |
| CHEMBL102372 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL443274 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL35 | FUROSEMIDE | Ki | > | 100000.0 | nM | - |
| CHEMBL320147 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL105100 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL22099 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL415323 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL320661 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL106548 | — | Ki | > | 100000.0 | nM | - |