Assay Detail
Binding
CHEMBL4327367
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Inhibition of PRMT5 (unknown origin)
9
Total Activities
9
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 |
Target
Protein arginine N-methyltransferase 5 (CHEMBL1795116) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of new potent protein arginine methyltransferase 5 (PRMT5) inhibitors by assembly of key pharmacophores from known inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.59 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441584 | — | — | 1 | 9.00 |
| CHEMBL4466233 | PEMRAMETOSTAT | 2.0 | 1 | 8.21 |
| CHEMBL1544509 | — | — | 1 | 7.00 |
| CHEMBL4092336 | — | — | 1 | 6.48 |
| CHEMBL313316 | — | — | 1 | 6.24 |
| CHEMBL4458385 | — | — | 1 | 6.16 |
| CHEMBL4475595 | — | — | 1 | 5.82 |
| CHEMBL4128989 | — | — | 1 | 5.55 |
| CHEMBL4128513 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441584 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4466233 | PEMRAMETOSTAT | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1544509 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4092336 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL313316 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4458385 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4475595 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4128989 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4128513 | — | IC50 | = | 14000.0 | nM | 4.85 |