Assay Detail
Binding
CHEMBL3756027
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Displacement of [125I]AB-MECA at human A3A receptor expressed in CHO cell membrane after 60 mins by scintillation counting method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structural refinement of pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective antagonists for the human A3 adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 7.64 | 10.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3754229 | — | — | 1 | 10.57 |
| CHEMBL3753642 | — | — | 1 | 9.39 |
| CHEMBL3753544 | — | — | 1 | 8.88 |
| CHEMBL3753976 | — | — | 1 | 8.74 |
| CHEMBL3752840 | — | — | 1 | 8.67 |
| CHEMBL3751978 | — | — | 1 | 8.63 |
| CHEMBL3752862 | — | — | 1 | 8.61 |
| CHEMBL3754475 | — | — | 1 | 8.45 |
| CHEMBL3754500 | — | — | 1 | 8.23 |
| CHEMBL3751909 | — | — | 1 | 8.19 |
| CHEMBL3753507 | — | — | 1 | 8.02 |
| CHEMBL3752438 | — | — | 1 | 8.01 |
| CHEMBL3754656 | — | — | 1 | 8.01 |
| CHEMBL582911 | — | — | 1 | 7.80 |
| CHEMBL3752622 | — | — | 1 | 7.77 |
| CHEMBL3752275 | — | — | 1 | 7.48 |
| CHEMBL3753937 | — | — | 1 | 7.27 |
| CHEMBL3753056 | — | — | 1 | 7.11 |
| CHEMBL3754432 | — | — | 1 | 6.89 |
| CHEMBL3753994 | — | — | 1 | 6.70 |
| CHEMBL3752647 | — | — | 1 | 6.65 |
| CHEMBL3752218 | — | — | 1 | 6.65 |
| CHEMBL3751940 | — | — | 1 | 6.61 |
| CHEMBL3753291 | — | — | 1 | 6.60 |
| CHEMBL3754773 | — | — | 1 | 6.49 |
| CHEMBL3753700 | — | — | 1 | 6.38 |
| CHEMBL3753895 | — | — | 1 | 6.37 |
| CHEMBL3754014 | — | — | 1 | 6.31 |
| CHEMBL3753543 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3754229 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3753642 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL3753544 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL3753976 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL3752840 | — | Ki | = | 2.12 | nM | 8.67 |
| CHEMBL3751978 | — | Ki | = | 2.34 | nM | 8.63 |
| CHEMBL3752862 | — | Ki | = | 2.43 | nM | 8.61 |
| CHEMBL3754475 | — | Ki | = | 3.53 | nM | 8.45 |
| CHEMBL3754500 | — | Ki | = | 5.87 | nM | 8.23 |
| CHEMBL3751909 | — | Ki | = | 6.42 | nM | 8.19 |
| CHEMBL3753507 | — | Ki | = | 9.54 | nM | 8.02 |
| CHEMBL3752438 | — | Ki | = | 9.83 | nM | 8.01 |
| CHEMBL3754656 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL582911 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3752622 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3752275 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3753937 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3753056 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL3754432 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL3753994 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL3752647 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL3752218 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL3751940 | — | Ki | = | 247.0 | nM | 6.61 |
| CHEMBL3753291 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL3754773 | — | Ki | = | 321.0 | nM | 6.49 |
| CHEMBL3753700 | — | Ki | = | 413.0 | nM | 6.38 |
| CHEMBL3753895 | — | Ki | = | 432.0 | nM | 6.37 |
| CHEMBL3754014 | — | Ki | = | 485.0 | nM | 6.31 |
| CHEMBL3753543 | — | Ki | = | 868.0 | nM | 6.06 |