Assay Detail
Binding
CHEMBL1036748
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Displacement of [3H]ZM241385 from human cloned adenosine A2A receptor expressed in human HeLa cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| 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 | 30 | 6.66 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL507754 | — | — | 1 | 7.55 |
| CHEMBL201145 | — | — | 1 | 7.51 |
| CHEMBL457881 | — | — | 1 | 7.32 |
| CHEMBL516154 | — | — | 1 | 7.30 |
| CHEMBL455985 | — | — | 1 | 7.05 |
| CHEMBL506179 | — | — | 1 | 7.04 |
| CHEMBL456125 | — | — | 1 | 7.00 |
| CHEMBL455998 | — | — | 1 | 6.99 |
| CHEMBL454700 | — | — | 1 | 6.98 |
| CHEMBL455999 | — | — | 1 | 6.93 |
| CHEMBL462095 | — | — | 1 | 6.90 |
| CHEMBL457014 | — | — | 1 | 6.84 |
| CHEMBL457418 | — | — | 1 | 6.83 |
| CHEMBL455986 | — | — | 1 | 6.79 |
| CHEMBL510409 | — | — | 1 | 6.78 |
| CHEMBL449133 | — | — | 1 | 6.70 |
| CHEMBL457880 | — | — | 1 | 6.62 |
| CHEMBL409514 | — | — | 1 | 6.59 |
| CHEMBL456816 | — | — | 1 | 6.49 |
| CHEMBL457659 | — | — | 1 | 6.40 |
| CHEMBL508090 | — | — | 1 | 6.39 |
| CHEMBL457015 | — | — | 1 | 6.33 |
| CHEMBL38528 | — | — | 1 | 6.32 |
| CHEMBL457209 | — | — | 1 | 6.20 |
| CHEMBL457442 | — | — | 1 | 6.20 |
| CHEMBL289413 | — | — | 1 | 6.19 |
| CHEMBL459553 | — | — | 1 | 6.16 |
| CHEMBL455315 | — | — | 1 | 6.03 |
| CHEMBL512216 | — | — | 1 | 5.83 |
| CHEMBL512388 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL507754 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL201145 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL457881 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL516154 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL455985 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL506179 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL456125 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL455998 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL454700 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL455999 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL462095 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL457014 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL457418 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL455986 | — | Ki | = | 162.0 | nM | 6.79 |
| CHEMBL510409 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL449133 | — | Ki | = | 199.0 | nM | 6.70 |
| CHEMBL457880 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL409514 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL456816 | — | Ki | = | 324.0 | nM | 6.49 |
| CHEMBL457659 | — | Ki | = | 398.0 | nM | 6.40 |
| CHEMBL508090 | — | Ki | = | 408.0 | nM | 6.39 |
| CHEMBL457015 | — | Ki | = | 468.0 | nM | 6.33 |
| CHEMBL38528 | — | Ki | = | 479.0 | nM | 6.32 |
| CHEMBL457209 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL457442 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL289413 | — | Ki | = | 646.0 | nM | 6.19 |
| CHEMBL459553 | — | Ki | = | 692.0 | nM | 6.16 |
| CHEMBL455315 | — | Ki | = | 933.0 | nM | 6.03 |
| CHEMBL512216 | — | Ki | = | 1470.0 | nM | 5.83 |
| CHEMBL512388 | — | Ki | = | 2450.0 | nM | 5.61 |