Assay Detail
Binding
CHEMBL901018
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Displacement of [3H]DPCPX from human adenosine A1 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 | 6.75 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL464859 | NECA | — | 1 | 7.85 |
| CHEMBL392136 | — | — | 1 | 7.72 |
| CHEMBL236958 | — | — | 1 | 7.36 |
| CHEMBL394063 | — | — | 1 | 7.34 |
| CHEMBL235071 | — | — | 1 | 7.19 |
| CHEMBL394064 | — | — | 1 | 7.10 |
| CHEMBL400812 | — | — | 1 | 7.09 |
| CHEMBL235075 | — | — | 1 | 7.05 |
| CHEMBL235718 | — | — | 1 | 7.04 |
| CHEMBL235295 | — | — | 1 | 7.00 |
| CHEMBL397821 | — | — | 1 | 6.98 |
| CHEMBL235076 | — | — | 1 | 6.97 |
| CHEMBL371834 | — | — | 1 | 6.96 |
| CHEMBL398787 | — | — | 1 | 6.93 |
| CHEMBL235294 | — | — | 1 | 6.69 |
| CHEMBL235512 | — | — | 1 | 6.59 |
| CHEMBL192555 | — | — | 1 | 6.47 |
| CHEMBL400811 | — | — | 1 | 6.41 |
| CHEMBL235719 | — | — | 1 | 6.33 |
| CHEMBL192198 | — | — | 1 | 6.23 |
| CHEMBL235935 | — | — | 1 | 6.12 |
| CHEMBL192615 | — | — | 1 | 6.05 |
| CHEMBL431733 | NAMODENOSON | 3.0 | 1 | 6.05 |
| CHEMBL401017 | — | — | 1 | 6.04 |
| CHEMBL372281 | — | — | 1 | 6.02 |
| CHEMBL192554 | — | — | 1 | 5.97 |
| CHEMBL235513 | — | — | 1 | 5.57 |
| CHEMBL190768 | — | — | 1 | 5.36 |
| CHEMBL235296 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL464859 | NECA | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL392136 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL236958 | — | Ki | = | 43.9 | nM | 7.36 |
| CHEMBL394063 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL235071 | — | Ki | = | 65.2 | nM | 7.19 |
| CHEMBL394064 | — | Ki | = | 80.2 | nM | 7.10 |
| CHEMBL400812 | — | Ki | = | 80.9 | nM | 7.09 |
| CHEMBL235075 | — | Ki | = | 89.5 | nM | 7.05 |
| CHEMBL235718 | — | Ki | = | 91.1 | nM | 7.04 |
| CHEMBL235295 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL397821 | — | Ki | = | 104.2 | nM | 6.98 |
| CHEMBL235076 | — | Ki | = | 106.7 | nM | 6.97 |
| CHEMBL371834 | — | Ki | = | 108.9 | nM | 6.96 |
| CHEMBL398787 | — | Ki | = | 116.5 | nM | 6.93 |
| CHEMBL235294 | — | Ki | = | 204.5 | nM | 6.69 |
| CHEMBL235512 | — | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL192555 | — | Ki | = | 339.5 | nM | 6.47 |
| CHEMBL400811 | — | Ki | = | 389.2 | nM | 6.41 |
| CHEMBL235719 | — | Ki | = | 462.2 | nM | 6.33 |
| CHEMBL192198 | — | Ki | = | 592.8 | nM | 6.23 |
| CHEMBL235935 | — | Ki | = | 764.0 | nM | 6.12 |
| CHEMBL192615 | — | Ki | = | 890.3 | nM | 6.05 |
| CHEMBL431733 | NAMODENOSON | Ki | = | 890.0 | nM | 6.05 |
| CHEMBL401017 | — | Ki | = | 916.0 | nM | 6.04 |
| CHEMBL372281 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL192554 | — | Ki | = | 1070.5 | nM | 5.97 |
| CHEMBL235513 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL190768 | — | Ki | = | 4400.5 | nM | 5.36 |
| CHEMBL235296 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL235717 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL193141 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL398788 | — | Ki | > | 10000.0 | nM | - |