Assay Detail
Binding
CHEMBL3626889
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human KAT2B catalytic domain 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
22
Total Activities
22
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 | 22 | 5.02 | 5.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL318367 | — | — | 1 | 5.45 |
| CHEMBL1732009 | — | — | 1 | 5.34 |
| CHEMBL1795608 | — | — | 1 | 5.28 |
| CHEMBL3621679 | — | — | 1 | 5.24 |
| CHEMBL1391552 | — | — | 1 | 5.24 |
| CHEMBL1733695 | — | — | 1 | 5.22 |
| CHEMBL1392315 | — | — | 1 | 5.21 |
| CHEMBL1795613 | — | — | 1 | 5.18 |
| CHEMBL1795619 | — | — | 1 | 5.16 |
| CHEMBL1720939 | — | — | 1 | 5.16 |
| CHEMBL1830867 | — | — | 1 | 5.03 |
| CHEMBL2087789 | — | — | 1 | 5.03 |
| CHEMBL106011 | — | — | 1 | 5.01 |
| CHEMBL3621676 | — | — | 1 | 4.97 |
| CHEMBL3621677 | — | — | 1 | 4.93 |
| CHEMBL608699 | — | — | 1 | 4.87 |
| CHEMBL3621672 | — | — | 1 | 4.87 |
| CHEMBL3621678 | — | — | 1 | 4.82 |
| CHEMBL1795618 | — | — | 1 | 4.76 |
| CHEMBL3621675 | — | — | 1 | 4.38 |
| CHEMBL3621673 | — | — | 1 | 4.17 |
| CHEMBL1795624 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL318367 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL1732009 | — | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL1795608 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3621679 | — | IC50 | = | 5820.0 | nM | 5.24 |
| CHEMBL1391552 | — | IC50 | = | 5770.0 | nM | 5.24 |
| CHEMBL1733695 | — | IC50 | = | 6010.0 | nM | 5.22 |
| CHEMBL1392315 | — | IC50 | = | 6190.0 | nM | 5.21 |
| CHEMBL1795613 | — | IC50 | = | 6640.0 | nM | 5.18 |
| CHEMBL1795619 | — | IC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL1720939 | — | IC50 | = | 6950.0 | nM | 5.16 |
| CHEMBL1830867 | — | IC50 | = | 9410.0 | nM | 5.03 |
| CHEMBL2087789 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL106011 | — | IC50 | = | 9740.0 | nM | 5.01 |
| CHEMBL3621676 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL3621677 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL608699 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL3621672 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL3621678 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL1795618 | — | IC50 | = | 17450.0 | nM | 4.76 |
| CHEMBL3621675 | — | IC50 | = | 41800.0 | nM | 4.38 |
| CHEMBL3621673 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL1795624 | — | IC50 | = | 130000.0 | nM | - |