Assay Detail
Binding
CHEMBL1261324
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-cyanopindolol from human adrenergic beta3 receptor expressed in CHO cells
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Thienopyrimidines as β3-adrenoceptor agonists: hit-to-lead optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 52 | 6.89 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1257675 | — | — | 1 | 9.00 |
| CHEMBL1257555 | — | — | 1 | 8.14 |
| CHEMBL1257913 | — | — | 1 | 8.07 |
| CHEMBL1257797 | — | — | 1 | 8.05 |
| CHEMBL1258025 | — | — | 1 | 7.96 |
| CHEMBL1258023 | — | — | 1 | 7.96 |
| CHEMBL1258257 | — | — | 1 | 7.85 |
| CHEMBL1255596 | — | — | 1 | 7.77 |
| CHEMBL1258258 | — | — | 1 | 7.77 |
| CHEMBL1257915 | — | — | 1 | 7.64 |
| CHEMBL1257676 | — | — | 1 | 7.52 |
| CHEMBL1258824 | — | — | 1 | 7.43 |
| CHEMBL1258599 | — | — | 1 | 7.39 |
| CHEMBL1258024 | — | — | 1 | 7.38 |
| CHEMBL1258705 | — | — | 1 | 7.33 |
| CHEMBL1258371 | — | — | 1 | 7.31 |
| CHEMBL1258142 | — | — | 1 | 7.23 |
| CHEMBL1258143 | — | — | 1 | 7.21 |
| CHEMBL1258484 | — | — | 1 | 7.20 |
| CHEMBL1258704 | — | — | 1 | 7.19 |
| CHEMBL1257554 | — | — | 1 | 7.14 |
| CHEMBL1257916 | — | — | 1 | 7.12 |
| CHEMBL1258026 | — | — | 1 | 7.12 |
| CHEMBL1258825 | — | — | 1 | 7.07 |
| CHEMBL1258597 | — | — | 1 | 7.07 |
| CHEMBL1258370 | — | — | 1 | 7.06 |
| CHEMBL1258144 | — | — | 1 | 7.05 |
| CHEMBL1258596 | — | — | 1 | 6.97 |
| CHEMBL1258486 | — | — | 1 | 6.95 |
| CHEMBL1257914 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1257675 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1257555 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL1257913 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL1257797 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1258025 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1258023 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1258257 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1255596 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1258258 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1257915 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1257676 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1258824 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1258599 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL1258024 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1258705 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL1258371 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL1258142 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL1258143 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL1258484 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL1258704 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL1257554 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL1257916 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL1258026 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL1258825 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL1258597 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL1258370 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL1258144 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL1258596 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL1258486 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL1257914 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL1257204 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL1258372 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL1258483 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL1258260 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL1258940 | — | Ki | = | 331.0 | nM | 6.48 |
| CHEMBL1257325 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL1083995 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL1258259 | — | Ki | = | 499.0 | nM | 6.30 |
| CHEMBL1258707 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL1257324 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL1258598 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL1257326 | — | Ki | = | 770.0 | nM | 6.11 |
| CHEMBL1257437 | — | Ki | = | 919.0 | nM | 6.04 |
| CHEMBL1257438 | — | Ki | = | 932.0 | nM | 6.03 |
| CHEMBL1258485 | — | Ki | = | 989.0 | nM | 6.00 |
| CHEMBL1257674 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL1258373 | — | Ki | = | 1390.0 | nM | 5.86 |
| CHEMBL1258706 | — | Ki | = | 1385.0 | nM | 5.86 |
| CHEMBL1257323 | — | Ki | = | 2646.0 | nM | 5.58 |
| CHEMBL1257440 | — | Ki | = | 3300.0 | nM | 5.48 |