Assay Detail
Binding
CHEMBL3294386
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Inhibition of EZH2 histone methyltransferase activity in EZH2/SUZ12/EED protein complex (unknown origin) using histone H3 peptide/S-adenosylmethionine as substrate after 2 hrs by TR-FRET assay
13
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.75 | 7.80 |
| Inhibition | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3287735 | GSK2816126 | 1.0 | 1 | 7.80 |
| CHEMBL3287733 | — | — | 2 | 6.28 |
| CHEMBL3287734 | — | — | 2 | 6.26 |
| CHEMBL215254 | TANSHINONE IIB | — | 2 | 5.32 |
| CHEMBL363535 | TANSHINONE I | — | 2 | 5.05 |
| CHEMBL2146517 | METHYL TANSHINONATE | — | 2 | 5.02 |
| CHEMBL187266 | TANSHINONE IIA | — | 2 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3287735 | GSK2816126 | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3287733 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3287734 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL215254 | TANSHINONE IIB | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL363535 | TANSHINONE I | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL2146517 | METHYL TANSHINONATE | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL187266 | TANSHINONE IIA | IC50 | = | 28100.0 | nM | 4.55 |
| CHEMBL363535 | TANSHINONE I | Inhibition | - | % | - | |
| CHEMBL187266 | TANSHINONE IIA | Inhibition | - | % | - | |
| CHEMBL215254 | TANSHINONE IIB | Inhibition | - | % | - | |
| CHEMBL3287733 | — | Inhibition | - | % | - | |
| CHEMBL3287734 | — | Inhibition | - | % | - | |
| CHEMBL2146517 | METHYL TANSHINONATE | Inhibition | - | % | - |