Assay Detail
Binding
CHEMBL4392555
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Inhibition of PRMT5 (unknown origin)/MEP50 (unknown origin) using histone H2 as substrate preincubated for 15 to 20 mins followed by S-[methyl-3H]adenosyl-L-methionine addition measured after 60 mins by liquid scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 5 | 8.04 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4536042 | — | — | 1 | 9.22 |
| CHEMBL4457371 | — | — | 1 | 8.70 |
| CHEMBL4465375 | — | — | 1 | 7.77 |
| CHEMBL4554624 | — | — | 1 | 7.58 |
| CHEMBL4459256 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4536042 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4457371 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4465375 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4554624 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4459256 | — | IC50 | = | 116.0 | nM | 6.94 |