Assay Detail
Binding
CHEMBL1014571
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Displacement of [3H]MRE3008F20 from human cloned adenosine A3 receptor expressed in CHO cells
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship studies of a new series of imidazo[2,1-f]purinones as potent and selective A(3) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 7.35 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL434534 | — | — | 1 | 9.10 |
| CHEMBL371404 | — | — | 1 | 8.46 |
| CHEMBL464075 | — | — | 1 | 8.29 |
| CHEMBL189904 | — | — | 1 | 8.10 |
| CHEMBL506908 | — | — | 1 | 7.82 |
| CHEMBL372026 | — | — | 1 | 7.82 |
| CHEMBL465290 | — | — | 1 | 7.70 |
| CHEMBL426271 | — | — | 1 | 7.66 |
| CHEMBL364036 | — | — | 1 | 7.64 |
| CHEMBL188269 | — | — | 1 | 7.51 |
| CHEMBL465090 | — | — | 1 | 7.47 |
| CHEMBL188506 | — | — | 1 | 7.44 |
| CHEMBL464076 | — | — | 1 | 7.42 |
| CHEMBL189922 | — | — | 1 | 7.26 |
| CHEMBL465089 | — | — | 1 | 7.24 |
| CHEMBL373090 | — | — | 1 | 7.22 |
| CHEMBL193130 | — | — | 1 | 7.10 |
| CHEMBL464437 | — | — | 1 | 7.01 |
| CHEMBL191421 | — | — | 1 | 7.00 |
| CHEMBL526122 | — | — | 1 | 7.00 |
| CHEMBL465281 | — | — | 1 | 6.96 |
| CHEMBL435887 | — | — | 1 | 6.94 |
| CHEMBL454444 | — | — | 1 | 6.85 |
| CHEMBL520767 | — | — | 1 | 6.84 |
| CHEMBL518729 | — | — | 1 | 6.83 |
| CHEMBL465949 | — | — | 1 | 6.74 |
| CHEMBL193100 | — | — | 1 | 6.70 |
| CHEMBL481383 | — | — | 1 | 6.70 |
| CHEMBL191414 | — | — | 1 | 6.26 |
| CHEMBL190472 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL434534 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL371404 | — | Ki | = | 3.45 | nM | 8.46 |
| CHEMBL464075 | — | Ki | = | 5.13 | nM | 8.29 |
| CHEMBL189904 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL506908 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL372026 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL465290 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL426271 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL364036 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL188269 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL465090 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL188506 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL464076 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL189922 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL465089 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL373090 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL193130 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL464437 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL191421 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL526122 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL465281 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL435887 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL454444 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL520767 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL518729 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL465949 | — | Ki | = | 182.0 | nM | 6.74 |
| CHEMBL193100 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL481383 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL191414 | — | Ki | = | 555.0 | nM | 6.26 |
| CHEMBL190472 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL480599 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL480529 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL518703 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL464438 | — | Ki | > | 1000.0 | nM | - |