Assay Detail
Binding
CHEMBL5033188
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human plasma TTR tetramer assessed as displacement of diclofenac-coupled FITC by fluorescence polarization assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and Their Common Age-Related Comorbidities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.26 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3940890 | ACORAMIDIS | 4.0 | 1 | 6.80 |
| CHEMBL5089170 | — | — | 1 | 6.72 |
| CHEMBL5091368 | — | — | 1 | 6.70 |
| CHEMBL5090952 | — | — | 1 | 6.68 |
| CHEMBL5080175 | — | — | 1 | 6.66 |
| CHEMBL5093498 | — | — | 1 | 6.58 |
| CHEMBL5080942 | — | — | 1 | 6.58 |
| CHEMBL5082796 | — | — | 1 | 6.52 |
| CHEMBL2103837 | TAFAMIDIS | 4.0 | 1 | 6.39 |
| CHEMBL5091475 | — | — | 1 | 6.26 |
| CHEMBL5085751 | — | — | 1 | 6.22 |
| CHEMBL5089791 | — | — | 1 | 6.21 |
| CHEMBL5082364 | — | — | 1 | 6.17 |
| CHEMBL5078773 | — | — | 1 | 6.11 |
| CHEMBL5086655 | — | — | 1 | 5.97 |
| CHEMBL5081258 | — | — | 1 | 5.84 |
| CHEMBL5082940 | — | — | 1 | 5.77 |
| CHEMBL5094401 | — | — | 1 | 5.55 |
| CHEMBL5078103 | — | — | 1 | 5.28 |
| CHEMBL5090565 | — | — | 1 | - |
| CHEMBL5076489 | — | — | 1 | - |
| CHEMBL5075496 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3940890 | ACORAMIDIS | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5089170 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5091368 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5090952 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5080175 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5093498 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5080942 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5082796 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2103837 | TAFAMIDIS | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5091475 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5085751 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5089791 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5082364 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL5078773 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5086655 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL5081258 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL5082940 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5094401 | — | IC50 | = | 2820.0 | nM | 5.55 |
| CHEMBL5078103 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5090565 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5076489 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5075496 | — | IC50 | > | 30000.0 | nM | - |