Assay Detail
Binding
CHEMBL2410098
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Inhibition of recombinant His-tagged HDAC2 (1 to 488) (unknown origin) using MAL as substrate incubated for 3 hrs prior to substrate addition measured after 60 mins by fluorescence plate reader analysis
29
Total Activities
29
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
Discovery of potent, isoform-selective inhibitors of histone deacetylase containing chiral heterocyclic capping groups and a N-(2-aminophenyl)benzamide binding unit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.74 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272980 | MOCETINOSTAT | 2.0 | 1 | 7.66 |
| CHEMBL2407719 | — | — | 1 | 7.36 |
| CHEMBL2407731 | — | — | 1 | 7.32 |
| CHEMBL2407718 | — | — | 1 | 7.25 |
| CHEMBL2407736 | — | — | 1 | 7.25 |
| CHEMBL2407735 | — | — | 1 | 7.18 |
| CHEMBL2407733 | — | — | 1 | 7.11 |
| CHEMBL2407723 | — | — | 1 | 7.09 |
| CHEMBL2407721 | — | — | 1 | 7.09 |
| CHEMBL2407717 | — | — | 1 | 7.07 |
| CHEMBL2407720 | — | — | 1 | 6.98 |
| CHEMBL2407722 | — | — | 1 | 6.96 |
| CHEMBL2407732 | — | — | 1 | 6.94 |
| CHEMBL2407730 | — | — | 1 | 6.66 |
| CHEMBL2407742 | — | — | 1 | 6.61 |
| CHEMBL2407734 | — | — | 1 | 6.58 |
| CHEMBL2407724 | — | — | 1 | 6.37 |
| CHEMBL2407716 | — | — | 1 | 6.36 |
| CHEMBL2407725 | — | — | 1 | 6.27 |
| CHEMBL2407738 | — | — | 1 | 6.24 |
| CHEMBL2407737 | — | — | 1 | 6.04 |
| CHEMBL2407743 | — | — | 1 | 5.84 |
| CHEMBL2407740 | — | — | 1 | 4.78 |
| CHEMBL2407729 | — | — | 1 | - |
| CHEMBL2407728 | — | — | 1 | - |
| CHEMBL2407727 | — | — | 1 | - |
| CHEMBL2407726 | — | — | 1 | - |
| CHEMBL2407741 | — | — | 1 | - |
| CHEMBL2407739 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272980 | MOCETINOSTAT | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2407719 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2407731 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2407718 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2407736 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2407735 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2407733 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2407723 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2407721 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2407717 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL2407720 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL2407722 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL2407732 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL2407730 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL2407742 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL2407734 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2407724 | — | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL2407716 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2407725 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL2407738 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL2407737 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL2407743 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL2407740 | — | IC50 | = | 16700.0 | nM | 4.78 |
| CHEMBL2407729 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2407728 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2407727 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2407726 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2407741 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2407739 | — | IC50 | > | 20000.0 | nM | - |