Assay Detail
Binding
CHEMBL636451
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Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
23
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.61 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260331 | — | — | 1 | 8.26 |
| CHEMBL33491 | — | — | 1 | 8.00 |
| CHEMBL289903 | — | — | 1 | 7.92 |
| CHEMBL33305 | — | — | 1 | 7.92 |
| CHEMBL33455 | — | — | 2 | 7.92 |
| CHEMBL32229 | — | — | 1 | 7.89 |
| CHEMBL32802 | — | — | 1 | 7.80 |
| CHEMBL32591 | — | — | 1 | 7.75 |
| CHEMBL33695 | — | — | 1 | 7.72 |
| CHEMBL287529 | — | — | 1 | 7.70 |
| CHEMBL2113342 | — | — | 1 | 7.62 |
| CHEMBL32225 | — | — | 1 | 7.55 |
| CHEMBL284615 | — | — | 1 | 7.50 |
| CHEMBL32281 | — | — | 1 | 7.47 |
| CHEMBL32481 | — | — | 1 | 7.46 |
| CHEMBL431703 | — | — | 1 | 7.44 |
| CHEMBL408186 | — | — | 1 | 7.42 |
| CHEMBL32582 | — | — | 1 | 7.33 |
| CHEMBL32770 | — | — | 1 | 7.30 |
| CHEMBL285900 | — | — | 1 | 7.25 |
| CHEMBL286838 | — | — | 1 | 7.12 |
| CHEMBL444787 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260331 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL33491 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL289903 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL33305 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL33455 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL32229 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL33455 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL32802 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL32591 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL33695 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL287529 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2113342 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL32225 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL284615 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL32281 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL32481 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL431703 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL408186 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL32582 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL32770 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL285900 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL286838 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL444787 | — | Ki | = | 108.0 | nM | 6.97 |