Assay Detail
Binding
CHEMBL5119797
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Binding affinity to recombinant HDAC6 (unknown origin) assessed as inhibition constant using Boc-Lys(acetyl)-AMC as substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs by fluorescence based microplate reader analysis
3
Total Activities
3
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
First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.64 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2364628 | RICOLINOSTAT | 2.0 | 1 | 9.00 |
| CHEMBL5173493 | — | — | 1 | 8.52 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 8.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2364628 | RICOLINOSTAT | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5173493 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2018302 | TUBASTATIN A | Ki | = | 4.0 | nM | 8.40 |