Assay Detail
Binding
CHEMBL643473
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Binding affinity against adenosine A1 receptor in rat cortex by the displacement of [3H]cyclohexyladenosine (CHA).
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 8.18 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.64 |
| CHEMBL160369 | — | — | 1 | 9.52 |
| CHEMBL27155 | — | — | 1 | 9.20 |
| CHEMBL34004 | — | — | 1 | 9.07 |
| CHEMBL284578 | — | — | 1 | 8.97 |
| CHEMBL32253 | — | — | 1 | 8.89 |
| CHEMBL416585 | — | — | 1 | 8.74 |
| CHEMBL34504 | — | — | 1 | 8.69 |
| CHEMBL34789 | — | — | 1 | 8.60 |
| CHEMBL158507 | — | — | 1 | 8.56 |
| CHEMBL33816 | — | — | 1 | 8.49 |
| CHEMBL33673 | — | — | 1 | 8.35 |
| CHEMBL285074 | — | — | 1 | 8.30 |
| CHEMBL34784 | — | — | 1 | 8.22 |
| CHEMBL18887 | — | — | 1 | 8.20 |
| CHEMBL428341 | — | — | 1 | 8.16 |
| CHEMBL285865 | — | — | 1 | 8.05 |
| CHEMBL33611 | — | — | 1 | 7.86 |
| CHEMBL33762 | — | — | 1 | 7.66 |
| CHEMBL283908 | — | — | 1 | 7.65 |
| CHEMBL284825 | — | — | 1 | 7.56 |
| CHEMBL33795 | — | — | 1 | 7.51 |
| CHEMBL34120 | — | — | 1 | 7.30 |
| CHEMBL33115 | — | — | 1 | 7.24 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | — | 1 | 7.22 |
| CHEMBL287011 | — | — | 1 | 6.59 |
| CHEMBL32963 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL160369 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL27155 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL34004 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL284578 | — | Ki | = | 1.06 | nM | 8.97 |
| CHEMBL32253 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL416585 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL34504 | — | Ki | = | 2.04 | nM | 8.69 |
| CHEMBL34789 | — | Ki | = | 2.54 | nM | 8.60 |
| CHEMBL158507 | — | Ki | = | 2.75 | nM | 8.56 |
| CHEMBL33816 | — | Ki | = | 3.23 | nM | 8.49 |
| CHEMBL33673 | — | Ki | = | 4.48 | nM | 8.35 |
| CHEMBL285074 | — | Ki | = | 5.02 | nM | 8.30 |
| CHEMBL34784 | — | Ki | = | 5.95 | nM | 8.22 |
| CHEMBL18887 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL428341 | — | Ki | = | 6.96 | nM | 8.16 |
| CHEMBL285865 | — | Ki | = | 8.93 | nM | 8.05 |
| CHEMBL33611 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL33762 | — | Ki | = | 21.8 | nM | 7.66 |
| CHEMBL283908 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL284825 | — | Ki | = | 27.6 | nM | 7.56 |
| CHEMBL33795 | — | Ki | = | 31.1 | nM | 7.51 |
| CHEMBL34120 | — | Ki | = | 49.6 | nM | 7.30 |
| CHEMBL33115 | — | Ki | = | 57.8 | nM | 7.24 |
| CHEMBL62350 | 8-PHENYL THEOPHYLLINE | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL287011 | — | Ki | = | 259.0 | nM | 6.59 |
| CHEMBL32963 | — | Ki | = | 275.0 | nM | 6.56 |