Assay Detail
Binding
CHEMBL3112170
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Inhibition of human recombinant full length HDAC3-NCoR2 using Lys_Ac_AMC as substrate after 60 mins by fluorescence assay
14
Total Activities
14
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
Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.08 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.60 |
| CHEMBL518821 | — | — | 1 | 6.42 |
| CHEMBL3109980 | — | — | 1 | 5.33 |
| CHEMBL3110001 | — | — | 1 | 5.05 |
| CHEMBL3110015 | — | — | 1 | 5.03 |
| CHEMBL3110021 | — | — | 1 | 4.92 |
| CHEMBL3109983 | — | — | 1 | 4.80 |
| CHEMBL3109993 | — | — | 1 | 4.75 |
| CHEMBL3110023 | — | — | 1 | 4.60 |
| CHEMBL3110016 | — | — | 1 | 4.58 |
| CHEMBL3110005 | — | — | 1 | 4.48 |
| CHEMBL3110003 | — | — | 1 | 4.41 |
| CHEMBL3110004 | — | — | 1 | - |
| CHEMBL396097 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL518821 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3109980 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3110001 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL3110015 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3110021 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL3109983 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3109993 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL3110023 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL3110016 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3110005 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3110003 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3110004 | — | IC50 | > | 43000.0 | nM | - |
| CHEMBL396097 | — | IC50 | > | 50000.0 | nM | - |