Assay Detail
Functional
CHEMBL637241
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Antagonist activity against adenosine A1 receptor in human platelets
33
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.45 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.33 |
| CHEMBL160369 | — | — | 1 | 8.60 |
| CHEMBL300334 | — | — | 1 | 8.59 |
| CHEMBL134837 | — | — | 1 | 8.10 |
| CHEMBL53453 | — | — | 1 | 8.10 |
| CHEMBL57554 | — | — | 1 | 7.96 |
| CHEMBL56251 | — | — | 2 | 7.92 |
| CHEMBL59529 | — | — | 1 | 7.85 |
| CHEMBL294869 | — | — | 2 | 7.77 |
| CHEMBL56409 | — | — | 1 | 7.70 |
| CHEMBL55883 | — | — | 1 | 7.66 |
| CHEMBL300983 | — | — | 1 | 7.39 |
| CHEMBL53737 | — | — | 1 | 7.38 |
| CHEMBL56673 | — | — | 1 | 7.30 |
| CHEMBL57076 | — | — | 2 | 7.28 |
| CHEMBL57503 | — | — | 2 | 7.23 |
| CHEMBL157833 | — | — | 1 | 7.16 |
| CHEMBL417770 | — | — | 1 | 7.12 |
| CHEMBL418101 | — | — | 1 | 7.09 |
| CHEMBL292661 | — | — | 1 | 7.07 |
| CHEMBL58879 | — | — | 2 | 7.05 |
| CHEMBL292382 | — | — | 2 | 7.00 |
| CHEMBL299699 | — | — | 1 | 6.89 |
| CHEMBL58380 | — | — | 1 | 6.18 |
| CHEMBL54836 | — | — | 2 | - |
| CHEMBL301403 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL160369 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL300334 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL134837 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL53453 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL57554 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL56251 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL59529 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL294869 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL56409 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL55883 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL300983 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL53737 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL56673 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL57076 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL57503 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL56251 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL157833 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL417770 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL418101 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL294869 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL292661 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL58879 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL292382 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL299699 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL292382 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL58879 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL57503 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL58380 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL54836 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL57076 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL54836 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL301403 | — | Ki | > | 10000.0 | nM | - |