Assay Detail
Binding
CHEMBL4843955
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Inhibition of human recombinant HDAC8 using H2N-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substrate after 90 mins by fluorescence based micro plate assay
25
Total Activities
25
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
Synthesis, structure-activity relationships, cocrystallization and cellular characterization of novel smHDAC8 inhibitors for the treatment of schistosomiasis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.72 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170177 | — | — | 1 | 8.00 |
| CHEMBL4095643 | — | — | 1 | 7.40 |
| CHEMBL4868510 | — | — | 1 | 7.16 |
| CHEMBL4846424 | — | — | 1 | 7.05 |
| CHEMBL4866890 | — | — | 1 | 7.05 |
| CHEMBL4865911 | — | — | 1 | 7.00 |
| CHEMBL4065863 | — | — | 1 | 6.96 |
| CHEMBL3800394 | — | — | 1 | 6.89 |
| CHEMBL4852163 | — | — | 1 | 6.85 |
| CHEMBL4877604 | — | — | 1 | 6.82 |
| CHEMBL4867661 | — | — | 1 | 6.75 |
| CHEMBL4093480 | — | — | 1 | 6.75 |
| CHEMBL4870162 | — | — | 1 | 6.66 |
| CHEMBL4853162 | — | — | 1 | 6.66 |
| CHEMBL4867041 | — | — | 1 | 6.64 |
| CHEMBL4847732 | — | — | 1 | 6.57 |
| CHEMBL4850958 | — | — | 1 | 6.55 |
| CHEMBL4853828 | — | — | 1 | 6.54 |
| CHEMBL4847326 | — | — | 1 | 6.50 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.40 |
| CHEMBL4857763 | — | — | 1 | 6.35 |
| CHEMBL4870946 | — | — | 1 | 6.23 |
| CHEMBL4849600 | — | — | 1 | 6.11 |
| CHEMBL4869895 | — | — | 1 | 6.07 |
| CHEMBL4855490 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170177 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4095643 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4868510 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4846424 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4866890 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4865911 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4065863 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3800394 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4852163 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4877604 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4867661 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4093480 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4870162 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4853162 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4867041 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4847732 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4850958 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4853828 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4847326 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4857763 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4870946 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4849600 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4869895 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4855490 | — | IC50 | = | 1100.0 | nM | 5.96 |