Assay Detail
Functional
CHEMBL5037229
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Antagonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 min followed by forskolin stimulation and further incubated for 30 mins in presence of NECA by alphascreen LANCE assay
30
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Flp-In-CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Covalent, Clickable Probes for Adenosine A<sub>1</sub> and A<sub>3</sub> Receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.18 | 9.30 |
| pKb | 15 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204703 | — | — | 2 | 9.30 |
| CHEMBL5073669 | — | — | 2 | 9.30 |
| CHEMBL5080823 | — | — | 2 | 9.22 |
| CHEMBL5092788 | — | — | 2 | 9.22 |
| CHEMBL5074992 | — | — | 2 | 8.85 |
| CHEMBL5088372 | — | — | 2 | 8.66 |
| CHEMBL5076192 | — | — | 2 | 8.62 |
| CHEMBL5087305 | — | — | 2 | 8.47 |
| CHEMBL5089483 | — | — | 2 | 8.28 |
| CHEMBL5088628 | — | — | 2 | 7.77 |
| CHEMBL5082113 | — | — | 2 | 7.58 |
| CHEMBL5085088 | — | — | 2 | 7.06 |
| CHEMBL5074615 | — | — | 2 | 7.04 |
| CHEMBL5076572 | — | — | 2 | 7.04 |
| CHEMBL5089727 | — | — | 2 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5073669 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL4204703 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL5080823 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5092788 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5074992 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL5088372 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL5076192 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL5087305 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL5089483 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL5088628 | — | Ki | = | 17.1 | nM | 7.77 |
| CHEMBL5082113 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5085088 | — | Ki | = | 87.5 | nM | 7.06 |
| CHEMBL5074615 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL5076572 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL5089727 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL4204703 | — | pKb | = | 9.27 | — | - |
| CHEMBL5082113 | — | pKb | = | 7.59 | — | - |
| CHEMBL5088628 | — | pKb | = | 7.77 | — | - |
| CHEMBL5074615 | — | pKb | = | 7.04 | — | - |
| CHEMBL5087305 | — | pKb | = | 8.47 | — | - |
| CHEMBL5073669 | — | pKb | = | 9.31 | — | - |
| CHEMBL5085088 | — | pKb | = | 7.06 | — | - |
| CHEMBL5080823 | — | pKb | = | 9.19 | — | - |
| CHEMBL5089483 | — | pKb | = | 8.28 | — | - |
| CHEMBL5076192 | — | pKb | = | 8.62 | — | - |
| CHEMBL5074992 | — | pKb | = | 8.86 | — | - |
| CHEMBL5092788 | — | pKb | = | 9.2 | — | - |
| CHEMBL5089727 | — | pKb | = | 6.23 | — | - |
| CHEMBL5076572 | — | pKb | = | 7.04 | — | - |
| CHEMBL5088372 | — | pKb | = | 8.65 | — | - |