Assay Detail
Binding
CHEMBL4026494
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat His-tagged PRMT1 (11 to 353 residues) expressed in Escherichia coli BL21(DE3) using biotinylated H4 peptide (1 to 21 residues) as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of [3H]SAM by microbeta counting method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein arginine N-methyltransferase 1 (CHEMBL1275220) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 5.48 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4094513 | — | — | 1 | 8.28 |
| CHEMBL4084293 | — | — | 1 | 8.22 |
| CHEMBL4073964 | — | — | 1 | 6.41 |
| CHEMBL4097780 | — | — | 1 | 6.15 |
| CHEMBL1617447 | — | — | 1 | 5.52 |
| CHEMBL4087631 | — | — | 1 | 5.44 |
| CHEMBL4078812 | — | — | 1 | 4.47 |
| CHEMBL4079756 | — | — | 1 | 4.35 |
| CHEMBL4077690 | — | — | 1 | 4.31 |
| CHEMBL4101956 | — | — | 1 | 4.28 |
| CHEMBL4075875 | — | — | 1 | 4.27 |
| CHEMBL1625601 | — | — | 1 | 4.07 |
| CHEMBL4060160 | — | — | 1 | - |
| CHEMBL4103085 | — | — | 1 | - |
| CHEMBL4095331 | — | — | 1 | - |
| CHEMBL4067925 | — | — | 1 | - |
| CHEMBL4105514 | — | — | 1 | - |
| CHEMBL4091931 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4094513 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4084293 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4073964 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4097780 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL1617447 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4087631 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4078812 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL4079756 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL4077690 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4101956 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL4075875 | — | IC50 | = | 54000.0 | nM | 4.27 |
| CHEMBL1625601 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL4060160 | — | IC50 | = | 147000.0 | nM | - |
| CHEMBL4103085 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4095331 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4067925 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4105514 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4091931 | — | IC50 | > | 50000.0 | nM | - |