Assay Detail
Binding
CHEMBL949479
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.23 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 9.48 |
| CHEMBL46882 | — | — | 1 | 9.29 |
| CHEMBL107400 | SOBETIROME | 2.0 | 1 | 8.96 |
| CHEMBL512383 | — | — | 1 | 8.73 |
| CHEMBL457528 | — | — | 1 | 8.43 |
| CHEMBL41036 | — | — | 1 | 8.11 |
| CHEMBL511862 | — | — | 1 | 7.99 |
| CHEMBL459148 | — | — | 1 | 7.80 |
| CHEMBL457527 | — | — | 1 | 7.73 |
| CHEMBL485758 | — | — | 1 | 7.55 |
| CHEMBL448595 | — | — | 1 | 7.52 |
| CHEMBL471488 | MB07344 | -1.0 | 1 | 7.45 |
| CHEMBL486359 | — | — | 1 | 7.38 |
| CHEMBL485928 | — | — | 1 | 7.21 |
| CHEMBL458784 | — | — | 1 | 6.84 |
| CHEMBL457529 | — | — | 1 | 6.74 |
| CHEMBL516330 | — | — | 1 | 6.73 |
| CHEMBL519721 | — | — | 1 | 6.63 |
| CHEMBL505084 | — | — | 1 | 6.54 |
| CHEMBL486358 | — | — | 1 | 6.52 |
| CHEMBL519215 | — | — | 1 | 6.42 |
| CHEMBL447378 | — | — | 1 | 6.23 |
| CHEMBL485927 | — | — | 1 | 6.05 |
| CHEMBL485939 | — | — | 1 | 5.93 |
| CHEMBL500875 | — | — | 1 | 5.85 |
| CHEMBL486158 | — | — | 1 | 5.75 |
| CHEMBL520857 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1544 | LIOTHYRONINE | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL46882 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL107400 | SOBETIROME | Ki | = | 1.09 | nM | 8.96 |
| CHEMBL512383 | — | Ki | = | 1.84 | nM | 8.73 |
| CHEMBL457528 | — | Ki | = | 3.74 | nM | 8.43 |
| CHEMBL41036 | — | Ki | = | 7.79 | nM | 8.11 |
| CHEMBL511862 | — | Ki | = | 10.3 | nM | 7.99 |
| CHEMBL459148 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL457527 | — | Ki | = | 18.6 | nM | 7.73 |
| CHEMBL485758 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL448595 | — | Ki | = | 30.5 | nM | 7.52 |
| CHEMBL471488 | MB07344 | Ki | = | 35.2 | nM | 7.45 |
| CHEMBL486359 | — | Ki | = | 42.1 | nM | 7.38 |
| CHEMBL485928 | — | Ki | = | 61.6 | nM | 7.21 |
| CHEMBL458784 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL457529 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL516330 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL519721 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL505084 | — | Ki | = | 285.0 | nM | 6.54 |
| CHEMBL486358 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL519215 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL447378 | — | Ki | = | 594.0 | nM | 6.23 |
| CHEMBL485927 | — | Ki | = | 897.0 | nM | 6.05 |
| CHEMBL485939 | — | Ki | = | 1165.0 | nM | 5.93 |
| CHEMBL500875 | — | Ki | = | 1416.0 | nM | 5.85 |
| CHEMBL486158 | — | Ki | = | 1760.0 | nM | 5.75 |
| CHEMBL520857 | — | Ki | = | 3296.0 | nM | 5.48 |