Assay Detail
Binding
CHEMBL3626893
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Inhibition of recombinant human CBP using biotinylated histone H3 (1 to 21 amino acid residues) as substrate preincubated for 10 mins followed by acetyl-CoA addition measured after 10 mins by time resolved fluorescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs)
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.70 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1370704 | — | — | 1 | 6.36 |
| CHEMBL1795619 | — | — | 1 | 5.90 |
| CHEMBL1795801 | — | — | 1 | 5.84 |
| CHEMBL2419973 | — | — | 1 | 5.78 |
| CHEMBL1795618 | — | — | 1 | 5.71 |
| CHEMBL106011 | — | — | 1 | 5.60 |
| CHEMBL1795624 | — | — | 1 | 5.54 |
| CHEMBL318367 | — | — | 1 | 5.28 |
| CHEMBL3621671 | — | — | 1 | 5.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1370704 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1795619 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL1795801 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL2419973 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL1795618 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL106011 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL1795624 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL318367 | — | IC50 | = | 5280.0 | nM | 5.28 |
| CHEMBL3621671 | — | IC50 | = | 5370.0 | nM | 5.27 |