Assay Detail
Binding
CHEMBL3602659
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Binding affinity to TTR in human plasma assessed as protein stabilization preincubated for 1 hr followed by urea-mediated denaturation by Western blot analysis
9
Total Activities
9
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
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 4.64 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 5.16 |
| CHEMBL28 | APIGENIN | — | 1 | 4.75 |
| CHEMBL898 | DIFLUNISAL | 4.0 | 1 | 4.60 |
| CHEMBL121626 | TOLFENAMIC ACID | 2.0 | 1 | 4.40 |
| CHEMBL509 | MECLOFENAMIC ACID | 4.0 | 1 | 4.30 |
| CHEMBL457 | GEMFIBROZIL | 4.0 | 1 | - |
| CHEMBL93645 | ACECLOFENAC | 2.0 | 1 | - |
| CHEMBL139 | DICLOFENAC | 4.0 | 1 | - |
| CHEMBL63323 | NIFLUMIC ACID | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL151 | LUTEOLIN | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL28 | APIGENIN | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL898 | DIFLUNISAL | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL121626 | TOLFENAMIC ACID | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL509 | MECLOFENAMIC ACID | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL457 | GEMFIBROZIL | IC50 | = | 180000.0 | nM | - |
| CHEMBL93645 | ACECLOFENAC | IC50 | = | 170000.0 | nM | - |
| CHEMBL139 | DICLOFENAC | IC50 | = | 140000.0 | nM | - |
| CHEMBL63323 | NIFLUMIC ACID | IC50 | = | 130000.0 | nM | - |