Assay Detail
Binding
CHEMBL649066
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Inhibition of adenosine binding to A1 receptor of rat brain homogenates
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.67 | 6.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL356323 | CIPAMFYLLINE | 2.0 | 1 | 6.77 |
| CHEMBL144196 | — | — | 1 | 6.21 |
| CHEMBL145159 | — | — | 1 | 6.00 |
| CHEMBL146165 | — | — | 1 | 5.82 |
| CHEMBL144374 | — | — | 1 | 5.66 |
| CHEMBL144545 | — | — | 1 | 5.62 |
| CHEMBL439809 | — | — | 1 | 5.57 |
| CHEMBL142782 | — | — | 1 | 5.55 |
| CHEMBL341866 | — | — | 1 | 5.54 |
| CHEMBL342998 | — | — | 1 | 5.46 |
| CHEMBL144341 | — | — | 1 | 5.42 |
| CHEMBL357921 | — | — | 1 | 5.39 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 4.72 |
| CHEMBL342727 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL356323 | CIPAMFYLLINE | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL144196 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL145159 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL146165 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL144374 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL144545 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL439809 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL142782 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL341866 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL342998 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL144341 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL357921 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL342727 | — | IC50 | > | 10000.0 | nM | - |