| Compound ID |
Cluster
|
Compound Type
|
Target/Cell | Structure | Activity | Assay Description | Source | ||||
|---|---|---|---|---|---|---|---|---|---|---|---|
|
Type
|
Relation
|
Value
|
Unit
|
||||||||
| NAs.000009 | 8 | ribose-match | Adenosine A1 receptor |  |
Other | = | 15.0 | % | Inhibition of [3H]NECA binding to human recombinant adenosine A1 receptor expressed in CHO cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.000009 | 8 | ribose-match | Adenosine A3 receptor | |
Ki | = | 404.0 | nM | Displacement of [3H]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | CHEMBL2086387 | |
| NAs.000009 | 8 | ribose-match | Adenosine A2a receptor | |
Other | = | 35.0 | % | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293 cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL2086387 | |
| NAs.000009 | 8 | ribose-match | Adenosine A1 receptor | |
Other | = | 15.0 | % | Displacement of [3H]PIA from human recombinant adenosine A1 receptor expressed in CHO cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL2086387 | |
| NAs.000009 | 8 | ribose-match | Unchecked | |
Other | > | 20.0 | None | Selectivity for human recombinant adenosine A3 receptor over human recombinant adenosine A2A receptor | CHEMBL1154768 | |
| NAs.000009 | 8 | ribose-match | Adenosine A3 receptor | |
Other | = | 0.9 | % | Activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM incubated for 45 mins prior to forskolin-stimulation measured after 15 mins by enzyme immunoassay relative to 10 uM NECA | CHEMBL2086387 | |
| NAs.000009 | 8 | ribose-match | Adenosine A3 receptor | |
Other | = | 0.9 | % | Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA | CHEMBL1154768 | |
| NAs.000009 | 8 | ribose-match | Adenosine A3 receptor | |
Ki | = | 404.0 | nM | Displacement of [125I]AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.000009 | 8 | ribose-match | Adenosine A2a receptor | |
Other | = | 35.0 | % | Inhibition of [3H]CGS21680 binding to human adenosine A2A receptor expressed in HEK293 cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.000009 | 8 | ribose-match | Adenosine receptors; A1 & A3 | |
Other | > | 20.0 | None | Selectivity for human recombinant adenosine A3 receptor over human recombinant adenosine A1 receptor | CHEMBL1154768 | |
| NAs.002780 | 8 | ribose-match | Adenosine A3 receptor |  |
Other | = | 96.9 | % | Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA | CHEMBL1154768 | |
| NAs.002780 | 8 | ribose-match | Adenosine A1 receptor | |
Ki | = | 2320.0 | nM | Displacement of [3H]NECA from human recombinant adenosine A1 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.002780 | 8 | ribose-match | Adenosine A2a receptor | |
Ki | = | 550.0 | nM | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.002780 | 8 | ribose-match | Adenosine A3 receptor | |
Ki | = | 2.5 | nM | Displacement of [125I]AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.002780 | 8 | ribose-match | Unchecked | |
Other | = | 160.0 | None | Selectivity ratio of Ki for human recombinant adenosine A2A receptor to Ki for human recombinant adenosine A3 receptor | CHEMBL1154768 | |
| NAs.002907 | 8 | ribose-match | Adenosine A3 receptor |  |
Other | = | 25.6 | % | Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM treated 45 mins before forskolin challenge measured after 15 mins by radioimmunoassay relative to NECA | CHEMBL1154768 | |
| NAs.002907 | 8 | ribose-match | Adenosine A2a receptor | |
Other | = | 8.0 | % | Inhibition of [3H]CGS21680 binding to human adenosine A2A receptor expressed in HEK293 cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.002907 | 8 | ribose-match | Adenosine A3 receptor | |
Other | = | 30.0 | % | Inhibition of [125I]AB-MECA binding to human recombinant adenosine A3 receptor expressed in CHO cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL1154768 | |
| NAs.002907 | 8 | ribose-match | Adenosine A1 receptor | |
Other | = | 33.0 | % | Inhibition of [3H]CCPA binding to human recombinant adenosine A1 receptor expressed in CHO cells at 10 uM after 60 mins by liquid scintillation counting | CHEMBL1154768 | |