Assay Detail
Binding
CHEMBL4392561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infected Sf9 insect cells assessed as reduction of S-adenosyl-L-homocysteine formation using human recombinant histone H2A (1 to 130 residues) as substrate after 1 hr in the presence of S-adenosyl-L-methionine by high throughput mass spectrometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Nucleoside protein arginine methyltransferase 5 (PRMT5) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.72 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4249337 | ONAMETOSTAT | 1.0 | 1 | 9.89 |
| CHEMBL4564327 | — | — | 1 | 9.80 |
| CHEMBL4541714 | — | — | 1 | 9.60 |
| CHEMBL4577464 | — | — | 1 | 9.49 |
| CHEMBL4454890 | — | — | 1 | 9.40 |
| CHEMBL4543007 | — | — | 1 | 9.10 |
| CHEMBL4579773 | — | — | 1 | 9.10 |
| CHEMBL4541070 | — | — | 1 | 8.30 |
| CHEMBL4439077 | — | — | 1 | 8.20 |
| CHEMBL4540972 | — | — | 1 | 8.10 |
| CHEMBL4556400 | — | — | 1 | 7.80 |
| CHEMBL4576734 | — | — | 1 | 7.70 |
| CHEMBL4589179 | — | — | 1 | 6.90 |
| CHEMBL4539612 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4249337 | ONAMETOSTAT | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4564327 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4541714 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4577464 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4454890 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4543007 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4579773 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4541070 | — | IC50 | = | 5.01 | nM | 8.30 |
| CHEMBL4439077 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4540972 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4556400 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4576734 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4589179 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4539612 | — | IC50 | < | 0.2 | nM | - |