Assay Detail
Binding
CHEMBL3596005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length HDAC3 (unknown origin) using MAZ1600/MAZ1675 as substrate assessed as release of 7 amino-4-methylcoumarin measured every 5 mins by fluorescence assay
12
Total Activities
12
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
Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.42 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593411 | — | — | 1 | 8.64 |
| CHEMBL3593407 | — | — | 1 | 8.59 |
| CHEMBL3593247 | — | — | 1 | 8.56 |
| CHEMBL3593409 | — | — | 1 | 8.51 |
| CHEMBL1173445 | LARGAZOLE | — | 1 | 8.04 |
| CHEMBL3593415 | — | — | 1 | 7.84 |
| CHEMBL3593413 | — | — | 1 | 7.37 |
| CHEMBL3593410 | — | — | 1 | 6.50 |
| CHEMBL3593408 | — | — | 1 | 6.48 |
| CHEMBL3593412 | — | — | 1 | 6.48 |
| CHEMBL3593414 | — | — | 1 | 6.07 |
| CHEMBL3593406 | — | — | 1 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593411 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL3593407 | — | IC50 | = | 2.59 | nM | 8.59 |
| CHEMBL3593247 | — | IC50 | = | 2.78 | nM | 8.56 |
| CHEMBL3593409 | — | IC50 | = | 3.07 | nM | 8.51 |
| CHEMBL1173445 | LARGAZOLE | IC50 | = | 9.09 | nM | 8.04 |
| CHEMBL3593415 | — | IC50 | = | 14.59 | nM | 7.84 |
| CHEMBL3593413 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL3593410 | — | IC50 | = | 319.5 | nM | 6.50 |
| CHEMBL3593408 | — | IC50 | = | 332.1 | nM | 6.48 |
| CHEMBL3593412 | — | IC50 | = | 332.4 | nM | 6.48 |
| CHEMBL3593414 | — | IC50 | = | 846.5 | nM | 6.07 |
| CHEMBL3593406 | — | IC50 | = | 1151.0 | nM | 5.94 |