Assay Detail
Binding
CHEMBL643729
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Inhibition of binding of [3H]5'-(N-ethylcarbamoyl)-adenosine to adenosine A2 receptor in rat striatal membranes
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 6.44 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL59084 | — | — | 1 | 8.30 |
| CHEMBL52993 | — | — | 1 | 8.20 |
| CHEMBL293102 | — | — | 1 | 8.17 |
| CHEMBL56610 | — | — | 1 | 8.03 |
| CHEMBL56076 | — | — | 1 | 7.61 |
| CHEMBL294185 | — | — | 1 | 7.58 |
| CHEMBL408489 | — | — | 1 | 7.55 |
| CHEMBL552985 | — | — | 1 | 7.33 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 7.20 |
| CHEMBL34504 | — | — | 1 | 6.92 |
| CHEMBL56399 | — | — | 1 | 6.83 |
| CHEMBL553037 | — | — | 1 | 6.75 |
| CHEMBL158507 | — | — | 1 | 6.75 |
| CHEMBL8969 | — | — | 1 | 6.68 |
| CHEMBL292904 | — | — | 1 | 6.50 |
| CHEMBL294463 | — | — | 1 | 6.50 |
| CHEMBL33722 | — | — | 1 | 6.42 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.39 |
| CHEMBL59488 | — | — | 1 | 6.38 |
| CHEMBL55623 | 2-[4-(2,6-Dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-phenoxy]-N-[2-(2-thiophen-2-yl-acetylamino-5-yl-acetyloxymercury)-ethyl]-acetamide | — | 1 | 6.34 |
| CHEMBL55356 | — | — | 1 | 6.23 |
| CHEMBL55839 | — | — | 1 | 6.19 |
| CHEMBL439747 | — | — | 1 | 6.08 |
| CHEMBL11348 | — | — | 1 | 6.08 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 6.07 |
| CHEMBL444575 | — | — | 1 | 6.06 |
| CHEMBL417607 | — | — | 1 | 6.01 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | — | 1 | 5.84 |
| CHEMBL298625 | — | — | 1 | 5.79 |
| CHEMBL52067 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL59084 | — | Ki | = | 5.03 | nM | 8.30 |
| CHEMBL52993 | — | Ki | = | 6.26 | nM | 8.20 |
| CHEMBL293102 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL56610 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL56076 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL294185 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL408489 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL552985 | — | Ki | = | 46.8 | nM | 7.33 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL34504 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL56399 | — | Ki | = | 147.0 | nM | 6.83 |
| CHEMBL158507 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL553037 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL8969 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL294463 | — | Ki | = | 315.0 | nM | 6.50 |
| CHEMBL292904 | — | Ki | = | 314.0 | nM | 6.50 |
| CHEMBL33722 | — | Ki | = | 381.0 | nM | 6.42 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL59488 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL55623 | 2-[4-(2,6-Dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-phenoxy]-N-[2-(2-thiophen-2-yl-acetylamino-5-yl-acetyloxymercury)-ethyl]-acetamide | Ki | = | 458.0 | nM | 6.34 |
| CHEMBL55356 | — | Ki | = | 594.0 | nM | 6.23 |
| CHEMBL55839 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL11348 | — | Ki | = | 836.0 | nM | 6.08 |
| CHEMBL439747 | — | Ki | = | 841.0 | nM | 6.08 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 848.0 | nM | 6.07 |
| CHEMBL444575 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL417607 | — | Ki | = | 984.0 | nM | 6.01 |
| CHEMBL106265 | 8-CYCLOPENTYLTHEOPHYLLINE | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL298625 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL52067 | — | Ki | = | 1740.0 | nM | 5.76 |
| CHEMBL27041 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL293337 | — | Ki | = | 2780.0 | nM | 5.56 |
| CHEMBL56751 | — | Ki | = | 3360.0 | nM | 5.47 |
| CHEMBL56952 | — | Ki | = | 3510.0 | nM | 5.46 |
| CHEMBL59585 | — | Ki | = | 4450.0 | nM | 5.35 |
| CHEMBL157655 | — | Ki | = | 5160.0 | nM | 5.29 |
| CHEMBL292016 | — | Ki | = | 11300.0 | nM | 4.95 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 25300.0 | nM | 4.60 |
| CHEMBL56813 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL292157 | — | Ki | > | 7000.0 | nM | - |
| CHEMBL56018 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL27762 | — | Ki | > | 5000.0 | nM | - |