Assay Detail
Binding
CHEMBL642858
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as a radioligand
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of pyrazolo[4,3-d]pyrimidin-7-ones as adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 6.72 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL268964 | — | — | 1 | 9.40 |
| CHEMBL268026 | — | — | 1 | 9.10 |
| CHEMBL269218 | — | — | 1 | 9.10 |
| CHEMBL276830 | — | — | 1 | 8.74 |
| CHEMBL11439 | — | — | 1 | 8.70 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 8.52 |
| CHEMBL175215 | — | — | 1 | 8.52 |
| CHEMBL11288 | — | — | 1 | 8.30 |
| CHEMBL11120 | — | — | 1 | 8.26 |
| CHEMBL416884 | — | — | 1 | 8.10 |
| CHEMBL11033 | — | — | 1 | 8.00 |
| CHEMBL8488 | — | — | 1 | 7.66 |
| CHEMBL11636 | — | — | 1 | 7.64 |
| CHEMBL10790 | — | — | 1 | 7.46 |
| CHEMBL368473 | — | — | 1 | 7.30 |
| CHEMBL11385 | — | — | 1 | 7.30 |
| CHEMBL175437 | — | — | 1 | 7.17 |
| CHEMBL274778 | — | — | 1 | 6.70 |
| CHEMBL175067 | — | — | 1 | 6.64 |
| CHEMBL366461 | — | — | 1 | 6.60 |
| CHEMBL301814 | — | — | 1 | 6.51 |
| CHEMBL429032 | — | — | 1 | 6.46 |
| CHEMBL367705 | — | — | 1 | 6.42 |
| CHEMBL176895 | — | — | 1 | 6.40 |
| CHEMBL174672 | — | — | 1 | 6.39 |
| CHEMBL366454 | — | — | 1 | 6.33 |
| CHEMBL273508 | — | — | 1 | 6.30 |
| CHEMBL172362 | — | — | 1 | 6.17 |
| CHEMBL367514 | — | — | 1 | 6.09 |
| CHEMBL176778 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL268964 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL268026 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL269218 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL276830 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL11439 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL175215 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL11288 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL11120 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL416884 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL11033 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL8488 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL11636 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL10790 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL11385 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL368473 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL175437 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL274778 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL175067 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL366461 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL301814 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL429032 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL367705 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL176895 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL174672 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL366454 | — | IC50 | = | 463.0 | nM | 6.33 |
| CHEMBL273508 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL172362 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL367514 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL176778 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL177113 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL176454 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL78636 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL177793 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL176743 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL174212 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL176375 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL105861 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL176670 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL368609 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL367499 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL425674 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL173794 | — | IC50 | = | 5430.0 | nM | 5.26 |
| CHEMBL366685 | — | IC50 | = | 7060.0 | nM | 5.15 |
| CHEMBL426407 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL170643 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL174958 | — | IC50 | = | 20100.0 | nM | 4.70 |