Assay Detail
Binding
CHEMBL5329844
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Inhibition of TEAD2 (217 to 447 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells/FAM-labelled YAP1 (60 to 99 residues)(unknown origin) protein-protein interaction preincubated for 24 hrs at 4 degree C with TEAD1 followed by fluorescent labelled YAP1 addition by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.63 | 5.64 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5423389 | — | — | 1 | 5.64 |
| CHEMBL5421684 | — | — | 1 | 5.51 |
| CHEMBL5437226 | — | — | 1 | 4.66 |
| CHEMBL5431273 | — | — | 1 | 4.33 |
| CHEMBL5420439 | — | — | 1 | 4.06 |
| CHEMBL5429883 | — | — | 1 | 3.60 |
| CHEMBL1719036 | — | — | 1 | - |
| CHEMBL5428328 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5423389 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5421684 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL5437226 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL5431273 | — | IC50 | = | 46500.0 | nM | 4.33 |
| CHEMBL5420439 | — | IC50 | = | 86700.0 | nM | 4.06 |
| CHEMBL5429883 | — | IC50 | = | 254000.0 | nM | 3.60 |
| CHEMBL1719036 | — | Inhibition | - | % | - | |
| CHEMBL5428328 | — | Inhibition | - | % | - |