Assay Detail
Functional
CHEMBL5136395
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human wild type A1R expressed in CHO-K1 cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a High Affinity Adenosine A<sub>1</sub>/A<sub>3</sub> Receptor Antagonist with a Novel 7-Amino-pyrazolo[3,4-<i>d</i>]pyridazine Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.09 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175347 | — | — | 1 | 9.01 |
| CHEMBL5183118 | — | — | 1 | 8.96 |
| CHEMBL5197567 | — | — | 1 | 8.82 |
| CHEMBL464859 | NECA | — | 1 | 8.74 |
| CHEMBL5203865 | — | — | 1 | 8.62 |
| CHEMBL5185411 | — | — | 1 | 8.15 |
| CHEMBL88147 | — | — | 1 | 7.32 |
| CHEMBL5195631 | — | — | 1 | 7.15 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175347 | — | EC50 | = | 0.9772 | nM | 9.01 |
| CHEMBL5183118 | — | EC50 | = | 1.096 | nM | 8.96 |
| CHEMBL5197567 | — | EC50 | = | 1.514 | nM | 8.82 |
| CHEMBL464859 | NECA | EC50 | = | 1.82 | nM | 8.74 |
| CHEMBL5203865 | — | EC50 | = | 2.399 | nM | 8.62 |
| CHEMBL5185411 | — | EC50 | = | 7.079 | nM | 8.15 |
| CHEMBL88147 | — | EC50 | = | 47.86 | nM | 7.32 |
| CHEMBL5195631 | — | EC50 | = | 70.79 | nM | 7.15 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | EC50 | = | 933.25 | nM | 6.03 |