Assay Detail
Binding
CHEMBL4770962
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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
16
Total Activities
16
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 dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.74 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4534486 | — | — | 1 | 9.10 |
| CHEMBL4078458 | — | — | 1 | 7.57 |
| CHEMBL4206936 | — | — | 1 | 7.30 |
| CHEMBL4789607 | — | — | 1 | 7.19 |
| CHEMBL4105068 | — | — | 1 | 7.16 |
| CHEMBL4790363 | — | — | 1 | 6.95 |
| CHEMBL4781368 | — | — | 1 | 6.80 |
| CHEMBL4784767 | — | — | 1 | 6.64 |
| CHEMBL4788940 | — | — | 1 | 6.44 |
| CHEMBL4786813 | — | — | 1 | 6.35 |
| CHEMBL4786752 | — | — | 1 | 6.33 |
| CHEMBL4780727 | — | — | 1 | 6.26 |
| CHEMBL4782406 | — | — | 1 | 6.25 |
| CHEMBL4789481 | — | — | 1 | 6.04 |
| CHEMBL4792281 | — | — | 1 | 6.02 |
| CHEMBL4797308 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4534486 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4078458 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4206936 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4789607 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4105068 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4790363 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4781368 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4784767 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4788940 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4786813 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL4786752 | — | IC50 | = | 465.0 | nM | 6.33 |
| CHEMBL4780727 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL4782406 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4789481 | — | IC50 | = | 908.0 | nM | 6.04 |
| CHEMBL4792281 | — | IC50 | = | 956.0 | nM | 6.02 |
| CHEMBL4797308 | — | IC50 | = | 3193.0 | nM | 5.50 |