Assay Detail
Binding
CHEMBL3388096
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-GST-tagged HDAC6 (unknown origin) assessed as reduction in deacetylation of Ac-Arg-Gly-Lys(Ac)-AMC substrate by fluorescence assay
21
Total Activities
21
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 | 21 | 7.18 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL356769 | TUBACIN | — | 1 | 8.40 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 7.82 |
| CHEMBL2431862 | — | — | 1 | 7.72 |
| CHEMBL3353062 | — | — | 1 | 7.50 |
| CHEMBL3353053 | — | — | 1 | 7.48 |
| CHEMBL3353054 | — | — | 1 | 7.48 |
| CHEMBL2431901 | — | — | 1 | 7.44 |
| CHEMBL3353056 | — | — | 1 | 7.41 |
| CHEMBL3353057 | — | — | 1 | 7.37 |
| CHEMBL3353067 | — | — | 1 | 7.19 |
| CHEMBL3353065 | — | — | 1 | 7.12 |
| CHEMBL3353061 | — | — | 1 | 7.07 |
| CHEMBL3353068 | — | — | 1 | 7.06 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.05 |
| CHEMBL3353058 | — | — | 1 | 7.00 |
| CHEMBL3353055 | — | — | 1 | 6.96 |
| CHEMBL3353066 | — | — | 1 | 6.89 |
| CHEMBL3353060 | — | — | 1 | 6.72 |
| CHEMBL3353059 | — | — | 1 | 6.55 |
| CHEMBL3353063 | — | — | 1 | 6.46 |
| CHEMBL3353064 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL356769 | TUBACIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2018302 | TUBASTATIN A | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2431862 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3353062 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3353053 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3353054 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2431901 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3353056 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3353057 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3353067 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3353065 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3353061 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3353068 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3353058 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3353055 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3353066 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3353060 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3353059 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3353063 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3353064 | — | IC50 | = | 810.0 | nM | 6.09 |