Assay Detail
Binding
CHEMBL1036747
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
33
Total Activities
33
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 | Autocuration |
Publication
1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.14 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL456125 | — | — | 1 | 9.00 |
| CHEMBL201145 | — | — | 1 | 8.66 |
| CHEMBL506179 | — | — | 1 | 8.59 |
| CHEMBL409514 | — | — | 1 | 8.21 |
| CHEMBL507754 | — | — | 1 | 8.19 |
| CHEMBL455986 | — | — | 1 | 8.05 |
| CHEMBL455999 | — | — | 1 | 7.96 |
| CHEMBL510409 | — | — | 1 | 7.72 |
| CHEMBL454700 | — | — | 1 | 7.64 |
| CHEMBL457418 | — | — | 1 | 7.62 |
| CHEMBL508090 | — | — | 1 | 7.46 |
| CHEMBL457881 | — | — | 1 | 7.36 |
| CHEMBL457014 | — | — | 1 | 7.30 |
| CHEMBL516154 | — | — | 1 | 7.27 |
| CHEMBL457015 | — | — | 1 | 7.19 |
| CHEMBL459553 | — | — | 1 | 7.17 |
| CHEMBL456816 | — | — | 1 | 7.15 |
| CHEMBL455985 | — | — | 1 | 7.05 |
| CHEMBL455998 | — | — | 1 | 6.94 |
| CHEMBL457880 | — | — | 1 | 6.81 |
| CHEMBL38528 | — | — | 1 | 6.74 |
| CHEMBL457442 | — | — | 1 | 6.70 |
| CHEMBL289413 | — | — | 1 | 6.64 |
| CHEMBL512216 | — | — | 1 | 6.54 |
| CHEMBL455315 | — | — | 1 | 6.47 |
| CHEMBL462095 | — | — | 1 | 6.34 |
| CHEMBL457209 | — | — | 1 | 6.32 |
| CHEMBL449133 | — | — | 1 | 6.31 |
| CHEMBL512388 | — | — | 1 | 6.29 |
| CHEMBL457659 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL456125 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL201145 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL506179 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL409514 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL507754 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL455986 | — | Ki | = | 8.9 | nM | 8.05 |
| CHEMBL455999 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL510409 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL454700 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL457418 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL508090 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL457881 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL457014 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL516154 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL457015 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL459553 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL456816 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL455985 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL455998 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL457880 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL38528 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL457442 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL289413 | — | Ki | = | 229.0 | nM | 6.64 |
| CHEMBL512216 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL455315 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL462095 | — | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL457209 | — | Ki | = | 479.0 | nM | 6.32 |
| CHEMBL449133 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL512388 | — | Ki | = | 513.0 | nM | 6.29 |
| CHEMBL457659 | — | Ki | = | 589.0 | nM | 6.23 |
| CHEMBL457441 | — | Ki | = | 676.0 | nM | 6.17 |
| CHEMBL452359 | — | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL460617 | — | Ki | = | 2239.0 | nM | 5.65 |