Assay Detail
Binding
CHEMBL5628402
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 3H-SAM from PRMT1 (unknown origin) using biotinylated-histone H4 peptide as substrate incubated for 45 mins by SPA assay
16
Total Activities
16
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
Development of selective class I protein arginine methyltransferase inhibitors through fragment-based drug design approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.12 | 6.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5633703 | — | — | 1 | 6.34 |
| CHEMBL5633779 | — | — | 1 | 5.96 |
| CHEMBL5633933 | — | — | 1 | 5.70 |
| CHEMBL5633967 | — | — | 1 | 5.61 |
| CHEMBL5631576 | — | — | 1 | 4.89 |
| CHEMBL5632809 | — | — | 1 | 4.89 |
| CHEMBL5631888 | — | — | 1 | 4.84 |
| CHEMBL5633177 | — | — | 1 | 4.82 |
| CHEMBL5633108 | — | — | 1 | 4.77 |
| CHEMBL5633498 | — | — | 1 | 4.64 |
| CHEMBL5631669 | — | — | 1 | 4.55 |
| CHEMBL5632481 | — | — | 1 | 4.48 |
| CHEMBL5633117 | — | — | 1 | - |
| CHEMBL5631984 | — | — | 1 | - |
| CHEMBL5632319 | — | — | 1 | - |
| CHEMBL5631287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5633703 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5633779 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5633933 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5633967 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL5631576 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5632809 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5631888 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL5633177 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5633108 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5633498 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL5631669 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL5632481 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL5633117 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5631984 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5632319 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5631287 | — | IC50 | > | 100000.0 | nM | - |