Assay Detail
Binding
CHEMBL3761793
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant HDAC3 using acetyllysine tripeptide coupled with 7-amino-4-methylcoumarin as substrate 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
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.41 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3759794 | — | — | 1 | 9.10 |
| CHEMBL3759059 | — | — | 1 | 8.92 |
| CHEMBL3758870 | — | — | 1 | 8.85 |
| CHEMBL3758735 | — | — | 1 | 8.80 |
| CHEMBL3758281 | — | — | 1 | 8.74 |
| CHEMBL3759921 | — | — | 1 | 8.70 |
| CHEMBL3758492 | — | — | 1 | 8.62 |
| CHEMBL3759982 | — | — | 1 | 8.47 |
| CHEMBL3758191 | — | — | 1 | 8.27 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.68 |
| CHEMBL3758246 | — | — | 1 | 7.59 |
| CHEMBL3758251 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3759794 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3759059 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3758870 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3758735 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3758281 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3759921 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3758492 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3759982 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3758191 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3758246 | — | IC50 | = | 25.6 | nM | 7.59 |
| CHEMBL3758251 | — | IC50 | = | 61.0 | nM | 7.21 |