Assay Detail
Binding
CHEMBL640779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for adenosine A1 receptor using [3H]N6-(phenylisopropyl)adenosine (R)-[3H]-PIA as a radioligand in rat brain.
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 8.04 | 9.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL604356 | — | — | 1 | 9.33 |
| CHEMBL604152 | — | — | 1 | 9.06 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | — | 1 | 8.96 |
| CHEMBL604353 | — | — | 1 | 8.92 |
| CHEMBL1512545 | — | — | 1 | 8.89 |
| CHEMBL605179 | — | — | 1 | 8.71 |
| CHEMBL268364 | — | — | 1 | 8.62 |
| CHEMBL9180 | — | — | 1 | 8.60 |
| CHEMBL603937 | — | — | 1 | 8.43 |
| CHEMBL8969 | — | — | 1 | 8.43 |
| CHEMBL603400 | — | — | 1 | 8.35 |
| CHEMBL275635 | — | — | 1 | 8.18 |
| CHEMBL603938 | — | — | 1 | 8.17 |
| CHEMBL275232 | — | — | 1 | 8.16 |
| CHEMBL266522 | — | — | 1 | 8.14 |
| CHEMBL604357 | — | — | 1 | 8.08 |
| CHEMBL603923 | — | — | 1 | 8.08 |
| CHEMBL603931 | — | — | 1 | 8.06 |
| CHEMBL27081 | — | — | 1 | 8.05 |
| CHEMBL603929 | — | — | 1 | 8.02 |
| CHEMBL9725 | — | — | 1 | 7.94 |
| CHEMBL9289 | — | — | 1 | 7.81 |
| CHEMBL9095 | — | — | 1 | 7.80 |
| CHEMBL9574 | — | — | 1 | 7.80 |
| CHEMBL9717 | — | — | 1 | 7.78 |
| CHEMBL9542 | — | — | 1 | 7.75 |
| CHEMBL262060 | — | — | 1 | 7.70 |
| CHEMBL9239 | — | — | 1 | 7.62 |
| CHEMBL9201 | — | — | 1 | 7.60 |
| CHEMBL9695 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL604356 | — | Ki | = | 0.469 | nM | 9.33 |
| CHEMBL604152 | — | Ki | = | 0.867 | nM | 9.06 |
| CHEMBL273094 | XANTHINE AMINE CONGENER | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL604353 | — | Ki | = | 1.19 | nM | 8.92 |
| CHEMBL1512545 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL605179 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL268364 | — | Ki | = | 2.39 | nM | 8.62 |
| CHEMBL9180 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL603937 | — | Ki | = | 3.72 | nM | 8.43 |
| CHEMBL8969 | — | Ki | = | 3.69 | nM | 8.43 |
| CHEMBL603400 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL275635 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL603938 | — | Ki | = | 6.75 | nM | 8.17 |
| CHEMBL275232 | — | Ki | = | 6.85 | nM | 8.16 |
| CHEMBL266522 | — | Ki | = | 7.26 | nM | 8.14 |
| CHEMBL604357 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL603923 | — | Ki | = | 8.37 | nM | 8.08 |
| CHEMBL603931 | — | Ki | = | 8.71 | nM | 8.06 |
| CHEMBL27081 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL603929 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL9725 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL9289 | — | Ki | = | 15.5 | nM | 7.81 |
| CHEMBL9095 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL9574 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL9717 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL9542 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL262060 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL9239 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL9201 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL9695 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL269782 | — | Ki | = | 37.8 | nM | 7.42 |
| CHEMBL9335 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL9437 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL9723 | — | Ki | = | 54.9 | nM | 7.26 |
| CHEMBL416881 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL162392 | — | Ki | = | 367.0 | nM | 6.43 |