Assay Detail
Binding
CHEMBL876574
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Ability to displace [125I]- AB-MECA from HEK 293 cell membrane expressing the human Adenosine A3 receptor
20
Total Activities
20
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
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.18 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL322250 | — | — | 1 | 8.40 |
| CHEMBL112923 | — | — | 1 | 8.38 |
| CHEMBL114832 | — | — | 1 | 8.30 |
| CHEMBL323717 | — | — | 1 | 8.20 |
| CHEMBL326757 | — | — | 1 | 8.08 |
| CHEMBL113634 | — | — | 1 | 8.00 |
| CHEMBL326319 | — | — | 1 | 7.85 |
| CHEMBL113420 | — | — | 1 | 7.46 |
| CHEMBL113512 | — | — | 1 | 7.44 |
| CHEMBL320751 | — | — | 1 | 7.17 |
| CHEMBL419394 | — | — | 1 | 7.11 |
| CHEMBL325010 | — | — | 1 | 6.94 |
| CHEMBL114304 | — | — | 1 | 6.70 |
| CHEMBL322968 | — | — | 1 | 6.68 |
| CHEMBL114127 | — | — | 1 | 6.67 |
| CHEMBL112256 | — | — | 1 | 6.43 |
| CHEMBL112536 | — | — | 1 | 6.26 |
| CHEMBL112098 | — | — | 1 | 6.02 |
| CHEMBL324428 | — | — | 1 | 5.95 |
| CHEMBL112194 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL322250 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL112923 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL114832 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL323717 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL326757 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL113634 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL326319 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL113420 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL113512 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL320751 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL419394 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL325010 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL114304 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL322968 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL114127 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL112256 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL112536 | — | Ki | = | 555.0 | nM | 6.26 |
| CHEMBL112098 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL324428 | — | Ki | = | 1125.0 | nM | 5.95 |
| CHEMBL112194 | — | Ki | = | 3020.0 | nM | 5.52 |