Assay Detail
Binding
CHEMBL4733333
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Inhibition of N-terminal His/GST-tagged human p300 HAT (965 to 1810 residues) expressed in Sf9 insect cells using H3 peptide as substrate in presence of Ac-CoA measured after 60 mins
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Current development of CBP/p300 inhibitors in the last decade.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.01 | 6.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4457203 | — | — | 1 | 6.38 |
| CHEMBL4752387 | — | — | 1 | 6.24 |
| CHEMBL4759868 | — | — | 1 | 6.16 |
| CHEMBL206106 | PALMITINE | — | 1 | 5.98 |
| CHEMBL235195 | TAXODIONE | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4457203 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4752387 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4759868 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL206106 | PALMITINE | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL235195 | TAXODIONE | IC50 | = | 4850.0 | nM | 5.31 |