Assay Detail
Binding
CHEMBL5138944
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length recombinant GST-tagged PRMT1 (2 to 371 residues) using histone H4 as substrate incubated for 20 mins in presence of [3H]-SAM by radioisotope-based filter assay
8
Total Activities
8
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 1 (CHEMBL5524) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.41 | 6.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5173678 | — | — | 1 | 6.08 |
| CHEMBL5180108 | — | — | 1 | 6.07 |
| CHEMBL5191769 | — | — | 1 | 5.75 |
| CHEMBL5186617 | — | — | 1 | 5.58 |
| CHEMBL5202088 | — | — | 1 | 5.31 |
| CHEMBL5206272 | — | — | 1 | 5.07 |
| CHEMBL5170047 | — | — | 1 | 4.93 |
| CHEMBL5199380 | — | — | 1 | 4.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5173678 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL5180108 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5191769 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5186617 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5202088 | — | IC50 | = | 4860.0 | nM | 5.31 |
| CHEMBL5206272 | — | IC50 | = | 8460.0 | nM | 5.07 |
| CHEMBL5170047 | — | IC50 | = | 11670.0 | nM | 4.93 |
| CHEMBL5199380 | — | IC50 | = | 32270.0 | nM | 4.49 |