Assay Detail
Binding
CHEMBL4669456
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Agonist activity at recombinant hexa-His-tagged THRalpha LBD (202 to 461 residues) (unknown origin)/recombinant human EE-tagged RXRalpha LBD (225 to 462 residues) assessed as increase in biotinylated GRIP1 peptide recruitment preincubated for 30 mins followed by peptide addition and measured after 30 mins by HTRF assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 18 | 5.76 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL471488 | MB07344 | -1.0 | 1 | 7.89 |
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 7.52 |
| CHEMBL4792904 | — | — | 1 | 6.89 |
| CHEMBL4750520 | — | — | 1 | 6.77 |
| CHEMBL4758498 | — | — | 1 | 6.47 |
| CHEMBL4789231 | — | — | 1 | 6.30 |
| CHEMBL4782668 | — | — | 1 | 5.85 |
| CHEMBL4743629 | — | — | 1 | 5.75 |
| CHEMBL3261331 | RESMETIROM | 4.0 | 1 | 5.52 |
| CHEMBL4787796 | — | — | 1 | 5.39 |
| CHEMBL4792525 | — | — | 1 | 5.19 |
| CHEMBL4776645 | — | — | 1 | 5.09 |
| CHEMBL4745568 | — | — | 1 | 5.03 |
| CHEMBL4755097 | — | — | 1 | 4.95 |
| CHEMBL4759495 | — | — | 1 | 4.90 |
| CHEMBL4741763 | — | — | 1 | 4.88 |
| CHEMBL4790442 | — | — | 1 | 4.79 |
| CHEMBL4753226 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL471488 | MB07344 | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1544 | LIOTHYRONINE | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4792904 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4750520 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4758498 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4789231 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4782668 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4743629 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3261331 | RESMETIROM | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4787796 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4792525 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4776645 | — | EC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL4745568 | — | EC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4755097 | — | EC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL4759495 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL4741763 | — | EC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4790442 | — | EC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL4753226 | — | EC50 | = | 31300.0 | nM | 4.50 |