Assay Detail
Binding
CHEMBL3596003
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length HDAC1 (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 | 7.48 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593407 | — | — | 1 | 8.71 |
| CHEMBL3593411 | — | — | 1 | 8.66 |
| CHEMBL3593247 | — | — | 1 | 8.60 |
| CHEMBL3593409 | — | — | 1 | 8.57 |
| CHEMBL1173445 | LARGAZOLE | — | 1 | 8.00 |
| CHEMBL3593415 | — | — | 1 | 7.88 |
| CHEMBL3593413 | — | — | 1 | 7.38 |
| CHEMBL3593408 | — | — | 1 | 6.69 |
| CHEMBL3593410 | — | — | 1 | 6.47 |
| CHEMBL3593412 | — | — | 1 | 6.47 |
| CHEMBL3593406 | — | — | 1 | 6.26 |
| CHEMBL3593414 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593407 | — | IC50 | = | 1.95 | nM | 8.71 |
| CHEMBL3593411 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3593247 | — | IC50 | = | 2.51 | nM | 8.60 |
| CHEMBL3593409 | — | IC50 | = | 2.68 | nM | 8.57 |
| CHEMBL1173445 | LARGAZOLE | IC50 | = | 10.09 | nM | 8.00 |
| CHEMBL3593415 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL3593413 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3593408 | — | IC50 | = | 203.6 | nM | 6.69 |
| CHEMBL3593410 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3593412 | — | IC50 | = | 340.3 | nM | 6.47 |
| CHEMBL3593406 | — | IC50 | = | 544.1 | nM | 6.26 |
| CHEMBL3593414 | — | IC50 | = | 816.9 | nM | 6.09 |