Assay Detail
Binding
CHEMBL1102043
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Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 90 mins by filtration binding assay
19
Total Activities
19
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
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.61 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076587 | — | — | 1 | 7.85 |
| CHEMBL1082005 | — | — | 1 | 7.60 |
| CHEMBL1081038 | — | — | 1 | 7.46 |
| CHEMBL1082208 | — | — | 1 | 7.24 |
| CHEMBL1081812 | — | — | 1 | 7.09 |
| CHEMBL1082028 | — | — | 1 | 6.91 |
| CHEMBL1079803 | — | — | 1 | 6.60 |
| CHEMBL1076562 | — | — | 1 | 6.54 |
| CHEMBL1079801 | — | — | 1 | 6.54 |
| CHEMBL1082171 | — | — | 1 | 6.50 |
| CHEMBL1081041 | — | — | 1 | 6.47 |
| CHEMBL1081811 | — | — | 1 | 6.45 |
| CHEMBL1079804 | — | — | 1 | 6.43 |
| CHEMBL1080676 | — | — | 1 | 6.20 |
| CHEMBL1080500 | — | — | 1 | 6.15 |
| CHEMBL1082006 | — | — | 1 | 6.04 |
| CHEMBL1081971 | — | — | 1 | 6.03 |
| CHEMBL1081039 | — | — | 1 | 6.03 |
| CHEMBL375293 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076587 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1082005 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL1081038 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1082208 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL1081812 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL1082028 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL1079803 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL1076562 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL1079801 | — | Ki | = | 289.0 | nM | 6.54 |
| CHEMBL1082171 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL1081041 | — | Ki | = | 338.0 | nM | 6.47 |
| CHEMBL1081811 | — | Ki | = | 358.0 | nM | 6.45 |
| CHEMBL1079804 | — | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL1080676 | — | Ki | = | 635.0 | nM | 6.20 |
| CHEMBL1080500 | — | Ki | = | 702.0 | nM | 6.15 |
| CHEMBL1082006 | — | Ki | = | 914.0 | nM | 6.04 |
| CHEMBL1081971 | — | Ki | = | 931.0 | nM | 6.03 |
| CHEMBL1081039 | — | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL375293 | — | Ki | = | 2821.0 | nM | 5.55 |