Assay Detail
Binding
CHEMBL5734269
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro evaluation of inhibitory activity against WT-TTR: In vitro evaluation of inhibitory activity against WT-TTR amyloid fibril formation of AT09 and reference compounds. Reference compounds (thyroxine, tafamidis and 2OHPCB80) are represented by dash bars and AT09 compounds by solid-gray bars. All compounds were analyzed at 2×, 1× and 0.5× the molar concentration of wild-type TTR (3.6 μM). Upon assay completion at 72 hours incubation at 37° C., the percentage of amyloid fibril formation was normalized against the positive control (black bar) corresponding to 100% of amyloid formation in the absence of test compounds.
15
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.65 | 5.80 |
| kon | 5 | - | - |
| k_off | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL83116 | — | — | 3 | 5.80 |
| CHEMBL5807923 | — | — | 3 | 5.70 |
| CHEMBL1624 | LEVOTHYROXINE | 4.0 | 3 | 5.66 |
| CHEMBL5928490 | — | — | 3 | 5.60 |
| CHEMBL2103837 | TAFAMIDIS | 4.0 | 3 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL83116 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL5807923 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL1624 | LEVOTHYROXINE | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5928490 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL2103837 | TAFAMIDIS | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5807923 | — | kon | = | - | — | - |
| CHEMBL5807923 | — | k_off | = | - | s-1 | - |
| CHEMBL5928490 | — | kon | = | - | — | - |
| CHEMBL5928490 | — | k_off | = | - | s-1 | - |
| CHEMBL2103837 | TAFAMIDIS | kon | = | - | — | - |
| CHEMBL2103837 | TAFAMIDIS | k_off | = | - | s-1 | - |
| CHEMBL83116 | — | kon | = | - | — | - |
| CHEMBL83116 | — | k_off | = | - | s-1 | - |
| CHEMBL1624 | LEVOTHYROXINE | kon | = | - | — | - |
| CHEMBL1624 | LEVOTHYROXINE | k_off | = | - | s-1 | - |