Assay Detail
Binding
CHEMBL3266219
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Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay
22
Total Activities
22
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
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 6.08 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL107400 | SOBETIROME | 2.0 | 1 | 8.52 |
| CHEMBL41036 | — | — | 1 | 8.30 |
| CHEMBL1544 | LIOTHYRONINE | 4.0 | 1 | 8.00 |
| CHEMBL3261325 | — | — | 1 | 6.68 |
| CHEMBL3261333 | — | — | 1 | 6.48 |
| CHEMBL3261322 | — | — | 1 | 6.41 |
| CHEMBL3261335 | — | — | 1 | 6.39 |
| CHEMBL3261324 | — | — | 1 | 6.16 |
| CHEMBL3261327 | — | — | 1 | 6.12 |
| CHEMBL3261323 | — | — | 1 | 6.11 |
| CHEMBL3261336 | — | — | 1 | 6.09 |
| CHEMBL3261334 | — | — | 1 | 5.90 |
| CHEMBL3261332 | — | — | 1 | 5.56 |
| CHEMBL3261321 | — | — | 1 | 5.48 |
| CHEMBL3261331 | RESMETIROM | 4.0 | 1 | 5.43 |
| CHEMBL3261326 | — | — | 1 | 5.37 |
| CHEMBL3261320 | — | — | 1 | 5.15 |
| CHEMBL3261328 | — | — | 1 | 5.05 |
| CHEMBL3261319 | — | — | 1 | 4.92 |
| CHEMBL3261330 | — | — | 1 | 4.84 |
| CHEMBL3261318 | — | — | 1 | 4.81 |
| CHEMBL3261329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL107400 | SOBETIROME | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL41036 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1544 | LIOTHYRONINE | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3261325 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3261333 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3261322 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3261335 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3261324 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3261327 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3261323 | — | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3261336 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3261334 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL3261332 | — | EC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL3261321 | — | EC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL3261331 | RESMETIROM | EC50 | = | 3740.0 | nM | 5.43 |
| CHEMBL3261326 | — | EC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL3261320 | — | EC50 | = | 7010.0 | nM | 5.15 |
| CHEMBL3261328 | — | EC50 | = | 8880.0 | nM | 5.05 |
| CHEMBL3261319 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3261330 | — | EC50 | = | 14390.0 | nM | 4.84 |
| CHEMBL3261318 | — | EC50 | = | 15640.0 | nM | 4.81 |
| CHEMBL3261329 | — | EC50 | - | — | - |