Assay Detail
Binding
CHEMBL901020
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Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells
33
Total Activities
33
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 | Intermediate |
Publication
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.42 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 9.66 |
| CHEMBL400812 | — | — | 1 | 8.96 |
| CHEMBL235513 | — | — | 1 | 8.80 |
| CHEMBL235295 | — | — | 1 | 8.37 |
| CHEMBL398787 | — | — | 1 | 8.04 |
| CHEMBL235717 | — | — | 1 | 7.91 |
| CHEMBL400811 | — | — | 1 | 7.82 |
| CHEMBL394063 | — | — | 1 | 7.54 |
| CHEMBL397821 | — | — | 1 | 7.48 |
| CHEMBL236958 | — | — | 1 | 7.46 |
| CHEMBL192615 | — | — | 1 | 7.40 |
| CHEMBL235512 | — | — | 1 | 7.38 |
| CHEMBL193141 | — | — | 1 | 7.38 |
| CHEMBL398788 | — | — | 1 | 7.36 |
| CHEMBL235719 | — | — | 1 | 7.31 |
| CHEMBL235935 | — | — | 1 | 7.31 |
| CHEMBL192554 | — | — | 1 | 7.30 |
| CHEMBL235075 | — | — | 1 | 7.29 |
| CHEMBL235296 | — | — | 1 | 7.25 |
| CHEMBL464859 | NECA | — | 1 | 7.14 |
| CHEMBL190768 | — | — | 1 | 7.06 |
| CHEMBL192555 | — | — | 1 | 7.04 |
| CHEMBL371834 | — | — | 1 | 7.02 |
| CHEMBL235718 | — | — | 1 | 7.01 |
| CHEMBL192198 | — | — | 1 | 7.01 |
| CHEMBL235294 | — | — | 1 | 7.00 |
| CHEMBL392136 | — | — | 1 | 6.99 |
| CHEMBL394064 | — | — | 1 | 6.53 |
| CHEMBL235071 | — | — | 1 | 6.43 |
| CHEMBL372281 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL431733 | NAMODENOSON | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL400812 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL235513 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL235295 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL398787 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL235717 | — | Ki | = | 12.3 | nM | 7.91 |
| CHEMBL400811 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL394063 | — | Ki | = | 29.2 | nM | 7.54 |
| CHEMBL397821 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL236958 | — | Ki | = | 34.6 | nM | 7.46 |
| CHEMBL192615 | — | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL235512 | — | Ki | = | 41.5 | nM | 7.38 |
| CHEMBL193141 | — | Ki | = | 41.9 | nM | 7.38 |
| CHEMBL398788 | — | Ki | = | 43.4 | nM | 7.36 |
| CHEMBL235935 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL235719 | — | Ki | = | 49.1 | nM | 7.31 |
| CHEMBL192554 | — | Ki | = | 49.8 | nM | 7.30 |
| CHEMBL235075 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL235296 | — | Ki | = | 55.7 | nM | 7.25 |
| CHEMBL464859 | NECA | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL190768 | — | Ki | = | 86.5 | nM | 7.06 |
| CHEMBL192555 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL371834 | — | Ki | = | 96.2 | nM | 7.02 |
| CHEMBL235718 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL192198 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL235294 | — | Ki | = | 101.2 | nM | 7.00 |
| CHEMBL392136 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL394064 | — | Ki | = | 295.2 | nM | 6.53 |
| CHEMBL235071 | — | Ki | = | 368.5 | nM | 6.43 |
| CHEMBL372281 | — | Ki | = | 382.5 | nM | 6.42 |
| CHEMBL235076 | — | Ki | = | 557.3 | nM | 6.25 |
| CHEMBL401017 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | > | 1000.0 | nM | - |