Assay Detail
Binding
CHEMBL646437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.76 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL65271 | — | — | 1 | 9.55 |
| CHEMBL302765 | — | — | 1 | 9.54 |
| CHEMBL138332 | — | — | 1 | 9.31 |
| CHEMBL88147 | — | — | 1 | 9.19 |
| CHEMBL422820 | — | — | 1 | 8.83 |
| CHEMBL141154 | — | — | 1 | 8.68 |
| CHEMBL137950 | — | — | 1 | 7.88 |
| CHEMBL139182 | — | — | 1 | 7.70 |
| CHEMBL342906 | — | — | 1 | 7.37 |
| CHEMBL344706 | — | — | 1 | 6.21 |
| CHEMBL423542 | — | — | 1 | 5.57 |
| CHEMBL16867 | — | — | 1 | 5.55 |
| CHEMBL137879 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL65271 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL302765 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL138332 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL88147 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL422820 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL141154 | — | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL137950 | — | Ki | = | 13.28 | nM | 7.88 |
| CHEMBL139182 | — | Ki | = | 19.81 | nM | 7.70 |
| CHEMBL342906 | — | Ki | = | 42.65 | nM | 7.37 |
| CHEMBL344706 | — | Ki | = | 613.0 | nM | 6.21 |
| CHEMBL423542 | — | Ki | = | 2666.0 | nM | 5.57 |
| CHEMBL16867 | — | Ki | = | 2785.0 | nM | 5.55 |
| CHEMBL137879 | — | Ki | = | 3579.0 | nM | 5.45 |