Assay Detail
Binding
CHEMBL4739211
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Inhibition of PRC2 in human G-401 cells assessed as reduction in methylation of H3K27 trimethylation by HTRF assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | G-401 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.28 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4755618 | — | — | 1 | 8.30 |
| CHEMBL4754048 | — | — | 1 | 7.96 |
| CHEMBL4785927 | — | — | 1 | 7.82 |
| CHEMBL4762963 | — | — | 1 | 7.80 |
| CHEMBL4759335 | — | — | 1 | 7.30 |
| CHEMBL4748924 | — | — | 1 | 6.99 |
| CHEMBL4752420 | — | — | 1 | 4.81 |
| CHEMBL4792277 | — | — | 1 | - |
| CHEMBL4751508 | — | — | 1 | - |
| CHEMBL4763811 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4755618 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4754048 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4785927 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4762963 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4759335 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4748924 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4752420 | — | IC50 | = | 15515.0 | nM | 4.81 |
| CHEMBL4792277 | — | IC50 | - | — | - | |
| CHEMBL4751508 | — | IC50 | - | — | - | |
| CHEMBL4763811 | — | IC50 | - | — | - |