Assay Detail
Binding
CHEMBL4680700
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Inhibition of human full length FLAG-tagged PRMT5/human His6-tagged MEP50 expressed in baculovirus-infected Sf9 cells assessed as reduction in tritium incorporation into peptide substrate using human Histone H4 (1 to 15 residues) and [3H]SAM as substrate preincubated with enzyme and H4 for 30 mins followed by [3H]SAM addition and measured after 120 mins by radioactive flashplate assay
16
Total Activities
16
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
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.13 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4542380 | — | — | 1 | 8.40 |
| CHEMBL3958947 | — | — | 1 | 7.96 |
| CHEMBL3963350 | — | — | 1 | 7.89 |
| CHEMBL3927051 | — | — | 1 | 7.89 |
| CHEMBL3938760 | — | — | 1 | 7.75 |
| CHEMBL4060831 | — | — | 1 | 7.66 |
| CHEMBL3919677 | — | — | 1 | 7.64 |
| CHEMBL3913586 | — | — | 1 | 7.48 |
| CHEMBL3977219 | — | — | 1 | 7.14 |
| CHEMBL3914119 | — | — | 1 | 7.02 |
| CHEMBL3962874 | — | — | 1 | 6.84 |
| CHEMBL3890510 | — | — | 1 | 6.49 |
| CHEMBL3906136 | — | — | 1 | 5.13 |
| CHEMBL4754920 | — | — | 1 | 4.57 |
| CHEMBL3982868 | — | — | 1 | - |
| CHEMBL4764863 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4542380 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3958947 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3963350 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3927051 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3938760 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4060831 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3919677 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3913586 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3977219 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3914119 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3962874 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3890510 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL3906136 | — | IC50 | = | 7450.0 | nM | 5.13 |
| CHEMBL4754920 | — | IC50 | = | 26800.0 | nM | 4.57 |
| CHEMBL3982868 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4764863 | — | IC50 | > | 50000.0 | nM | - |