Assay Detail
Binding
CHEMBL1273384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human GST-tagged PRMT1-mediated arginine methylation expressed in Escherichia coli BL21 (DE3) using H4(1-20) and [14C]-AdoMet by scintillation counting
10
Total Activities
10
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
Discovery and mechanistic study of a class of protein arginine methylation inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 4.33 | 4.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092740 | — | — | 1 | 4.89 |
| CHEMBL1271164 | — | — | 1 | 4.30 |
| CHEMBL142304 | STILBAMIDINE | 2.0 | 1 | 4.25 |
| CHEMBL409290 | — | — | 1 | 4.17 |
| CHEMBL221047 | — | — | 1 | 4.04 |
| CHEMBL1271266 | — | — | 1 | - |
| CHEMBL1270653 | — | — | 1 | - |
| CHEMBL1270654 | — | — | 1 | - |
| CHEMBL3351047 | — | — | 1 | - |
| CHEMBL227725 | ALLANTODAPSONE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092740 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL1271164 | — | IC50 | = | 50500.0 | nM | 4.30 |
| CHEMBL142304 | STILBAMIDINE | IC50 | = | 56600.0 | nM | 4.25 |
| CHEMBL409290 | — | IC50 | = | 68200.0 | nM | 4.17 |
| CHEMBL221047 | — | IC50 | = | 91200.0 | nM | 4.04 |
| CHEMBL1271266 | — | IC50 | = | 121700.0 | nM | - |
| CHEMBL1270653 | — | IC50 | = | 1029000.0 | nM | - |
| CHEMBL1270654 | — | IC50 | = | 1063000.0 | nM | - |
| CHEMBL3351047 | — | IC50 | = | 1458000.0 | nM | - |
| CHEMBL227725 | ALLANTODAPSONE | IC50 | = | 1825000.0 | nM | - |