Assay Detail
Binding
CHEMBL3626895
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Inhibition of recombinant human p300 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
13
Total Activities
13
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 | 13 | 5.14 | 5.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1795608 | — | — | 1 | 5.61 |
| CHEMBL106011 | — | — | 1 | 5.27 |
| CHEMBL1795619 | — | — | 1 | 5.27 |
| CHEMBL318367 | — | — | 1 | 5.24 |
| CHEMBL1795618 | — | — | 1 | 5.24 |
| CHEMBL1795624 | — | — | 1 | 5.23 |
| CHEMBL2087789 | — | — | 1 | 5.17 |
| CHEMBL1733695 | — | — | 1 | 5.09 |
| CHEMBL1392315 | — | — | 1 | 5.09 |
| CHEMBL1795613 | — | — | 1 | 5.08 |
| CHEMBL1391552 | — | — | 1 | 5.03 |
| CHEMBL1720939 | — | — | 1 | 4.89 |
| CHEMBL608699 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1795608 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL106011 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL1795619 | — | IC50 | = | 5320.0 | nM | 5.27 |
| CHEMBL318367 | — | IC50 | = | 5710.0 | nM | 5.24 |
| CHEMBL1795618 | — | IC50 | = | 5740.0 | nM | 5.24 |
| CHEMBL1795624 | — | IC50 | = | 5920.0 | nM | 5.23 |
| CHEMBL2087789 | — | IC50 | = | 6740.0 | nM | 5.17 |
| CHEMBL1733695 | — | IC50 | = | 8140.0 | nM | 5.09 |
| CHEMBL1392315 | — | IC50 | = | 8030.0 | nM | 5.09 |
| CHEMBL1795613 | — | IC50 | = | 8280.0 | nM | 5.08 |
| CHEMBL1391552 | — | IC50 | = | 9350.0 | nM | 5.03 |
| CHEMBL1720939 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL608699 | — | IC50 | = | 24700.0 | nM | 4.61 |