Assay Detail
Functional
CHEMBL5136396
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Antagonist activity at human wild type A3R expressed in Flp-In-CHO 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
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Flp-In-CHO |
| 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 | 7 | 9.12 | 9.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL464859 | NECA | — | 1 | 9.93 |
| CHEMBL5175347 | — | — | 1 | 9.50 |
| CHEMBL5197567 | — | — | 1 | 9.33 |
| CHEMBL5183118 | — | — | 1 | 9.27 |
| CHEMBL5185411 | — | — | 1 | 9.04 |
| CHEMBL5203865 | — | — | 1 | 8.94 |
| CHEMBL5195631 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL464859 | NECA | EC50 | = | 0.1175 | nM | 9.93 |
| CHEMBL5175347 | — | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL5197567 | — | EC50 | = | 0.4677 | nM | 9.33 |
| CHEMBL5183118 | — | EC50 | = | 0.537 | nM | 9.27 |
| CHEMBL5185411 | — | EC50 | = | 0.912 | nM | 9.04 |
| CHEMBL5203865 | — | EC50 | = | 1.148 | nM | 8.94 |
| CHEMBL5195631 | — | EC50 | = | 15.85 | nM | 7.80 |