Assay Detail
Binding
CHEMBL5136399
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of CA200645 from NLuc human A3 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 |
|---|---|---|---|
| Ki | 8 | 7.25 | 9.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL88147 | — | — | 1 | 9.94 |
| CHEMBL5195631 | — | — | 1 | 7.89 |
| CHEMBL464859 | NECA | — | 1 | 7.05 |
| CHEMBL5183118 | — | — | 1 | 6.44 |
| CHEMBL5185411 | — | — | 1 | 6.42 |
| CHEMBL5203865 | — | — | 1 | 5.77 |
| CHEMBL5175347 | — | — | 1 | - |
| CHEMBL5197567 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL88147 | — | Ki | = | 0.1148 | nM | 9.94 |
| CHEMBL5195631 | — | Ki | = | 12.88 | nM | 7.89 |
| CHEMBL464859 | NECA | Ki | = | 89.13 | nM | 7.05 |
| CHEMBL5183118 | — | Ki | = | 363.08 | nM | 6.44 |
| CHEMBL5185411 | — | Ki | = | 380.19 | nM | 6.42 |
| CHEMBL5203865 | — | Ki | = | 1698.24 | nM | 5.77 |
| CHEMBL5175347 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5197567 | — | Ki | > | 10000.0 | nM | - |