Assay Detail
Functional
CHEMBL1771830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human adenosine A3 receptor
84
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 84 | 8.02 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1771603 | — | — | 1 | 11.00 |
| CHEMBL168018 | — | — | 1 | 9.82 |
| CHEMBL324735 | — | — | 1 | 9.80 |
| CHEMBL352796 | — | — | 1 | 9.74 |
| CHEMBL329791 | — | — | 1 | 9.70 |
| CHEMBL349240 | — | — | 1 | 9.68 |
| CHEMBL165224 | — | — | 1 | 9.62 |
| CHEMBL165083 | — | — | 1 | 9.57 |
| CHEMBL166301 | — | — | 1 | 9.52 |
| CHEMBL330286 | — | — | 1 | 9.49 |
| CHEMBL165600 | — | — | 1 | 9.43 |
| CHEMBL344501 | — | — | 1 | 9.40 |
| CHEMBL354161 | — | — | 1 | 9.37 |
| CHEMBL350205 | — | — | 1 | 9.35 |
| CHEMBL348925 | — | — | 1 | 9.34 |
| CHEMBL352192 | — | — | 1 | 9.30 |
| CHEMBL167915 | — | — | 1 | 9.26 |
| CHEMBL65271 | — | — | 1 | 9.22 |
| CHEMBL423934 | — | — | 1 | 9.22 |
| CHEMBL165910 | — | — | 1 | 9.19 |
| CHEMBL88147 | — | — | 1 | 9.19 |
| CHEMBL341376 | — | — | 1 | 9.09 |
| CHEMBL355415 | — | — | 1 | 9.09 |
| CHEMBL350830 | — | — | 1 | 9.04 |
| CHEMBL138332 | — | — | 1 | 9.04 |
| CHEMBL349464 | — | — | 1 | 9.00 |
| CHEMBL165073 | — | — | 1 | 8.99 |
| CHEMBL163968 | — | — | 1 | 8.96 |
| CHEMBL16488 | — | — | 1 | 8.83 |
| CHEMBL141154 | — | — | 1 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1771603 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL168018 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL324735 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL352796 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL329791 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL349240 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL165224 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL165083 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL166301 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL330286 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL165600 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL344501 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL354161 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL350205 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL348925 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL352192 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL167915 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL423934 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL65271 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL165910 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL88147 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL355415 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL341376 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL138332 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL350830 | — | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL349464 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL165073 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL163968 | — | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL16488 | — | Ki | = | 1.47 | nM | 8.83 |
| CHEMBL141154 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL322983 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL353299 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL209943 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL317382 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL390407 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL280080 | — | Ki | = | 3.75 | nM | 8.43 |
| CHEMBL352707 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL474016 | — | Ki | = | 4.54 | nM | 8.34 |
| CHEMBL175494 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL1770311 | — | Ki | = | 8.472 | nM | 8.07 |
| CHEMBL1770311 | — | Ki | = | 8.48 | nM | 8.07 |
| CHEMBL361412 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL16687 | CGS-15943 | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL274273 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL324512 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL276321 | — | Ki | = | 27.5 | nM | 7.56 |
| CHEMBL416537 | — | Ki | = | 28.5 | nM | 7.54 |
| CHEMBL397821 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL236958 | — | Ki | = | 34.6 | nM | 7.46 |
| CHEMBL164867 | — | Ki | = | 40.0 | nM | 7.40 |