Assay Detail
Binding
CHEMBL638561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
74
Total Activities
72
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 | 74 | 7.15 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260331 | — | — | 1 | 8.26 |
| CHEMBL32598 | — | — | 1 | 8.05 |
| CHEMBL33491 | — | — | 1 | 8.00 |
| CHEMBL289903 | — | — | 1 | 7.92 |
| CHEMBL33455 | — | — | 2 | 7.92 |
| CHEMBL33305 | — | — | 1 | 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 |
| CHEMBL32552 | — | — | 1 | 7.41 |
| CHEMBL286420 | — | — | 1 | 7.39 |
| CHEMBL32582 | — | — | 1 | 7.33 |
| CHEMBL32770 | — | — | 1 | 7.30 |
| CHEMBL289002 | — | — | 1 | 7.29 |
| CHEMBL32359 | — | — | 1 | 7.28 |
| CHEMBL33930 | — | — | 1 | 7.26 |
| CHEMBL285900 | — | — | 1 | 7.25 |
| CHEMBL33709 | — | — | 1 | 7.24 |
| CHEMBL32581 | — | — | 1 | 7.24 |
| CHEMBL32311 | — | — | 1 | 7.23 |
| CHEMBL33653 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260331 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL32598 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL33491 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL33305 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL33455 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL289903 | — | 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 |
| CHEMBL32552 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL286420 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL32582 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL32770 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL289002 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL32359 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL33930 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL285900 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL32581 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL33709 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL32311 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL33653 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL284789 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL32118 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL286838 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL32950 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL287493 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL286102 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL34281 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL32388 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL32288 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL32289 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL290105 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL286212 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL2112067 | — | Ki | = | 93.0 | nM | 7.03 |
| CHEMBL445056 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL432273 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL32150 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL32757 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL444787 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL34097 | — | Ki | = | 111.0 | nM | 6.96 |