Assay Detail
Binding
CHEMBL3388103
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human HDAC4 (627 to 1085 residues) using fluorogenic acetyl-Lys(trifluoroacetyl)-AMC substrate incubated for 2 hrs by fluorescence assay
6
Total Activities
6
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
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.79 | 4.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2431862 | — | — | 1 | 4.82 |
| CHEMBL356769 | TUBACIN | — | 1 | 4.76 |
| CHEMBL3353053 | — | — | 1 | - |
| CHEMBL2431901 | — | — | 1 | - |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | - |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2431862 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL356769 | TUBACIN | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL3353053 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2431901 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL98 | VORINOSTAT | IC50 | - | — | - | |
| CHEMBL2018302 | TUBASTATIN A | IC50 | > | 30000.0 | nM | - |