Assay Detail
Binding
CHEMBL4808435
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PRMT5 (unknown origin) assessed as inhibition of symmetric dimethylation of arginine incubated for 3 days by fluorescence based cellular target engagement assay
33
Total Activities
33
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 5 (CHEMBL1795116) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 33 | 8.51 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4854745 | — | — | 1 | 9.13 |
| CHEMBL4861625 | — | — | 1 | 9.08 |
| CHEMBL4867460 | — | — | 1 | 9.06 |
| CHEMBL4860414 | — | — | 1 | 9.05 |
| CHEMBL4852843 | — | — | 1 | 9.05 |
| CHEMBL4873949 | — | — | 1 | 9.01 |
| CHEMBL4868904 | — | — | 1 | 8.96 |
| CHEMBL4853705 | — | — | 1 | 8.92 |
| CHEMBL4867267 | — | — | 1 | 8.92 |
| CHEMBL4846860 | — | — | 1 | 8.92 |
| CHEMBL4851358 | — | — | 1 | 8.89 |
| CHEMBL4847518 | — | — | 1 | 8.82 |
| CHEMBL4878171 | — | — | 1 | 8.77 |
| CHEMBL4860893 | — | — | 1 | 8.64 |
| CHEMBL4874354 | — | — | 1 | 8.60 |
| CHEMBL4850190 | — | — | 1 | 8.55 |
| CHEMBL4846178 | — | — | 1 | 8.54 |
| CHEMBL4853843 | — | — | 1 | 8.49 |
| CHEMBL4849342 | — | — | 1 | 8.49 |
| CHEMBL4869259 | — | — | 1 | 8.40 |
| CHEMBL4873952 | — | — | 1 | 8.34 |
| CHEMBL4868831 | — | — | 1 | 8.33 |
| CHEMBL4849067 | — | — | 1 | 8.28 |
| CHEMBL4854567 | — | — | 1 | 8.28 |
| CHEMBL4862596 | — | — | 1 | 8.00 |
| CHEMBL4853251 | — | — | 1 | 8.00 |
| CHEMBL4862485 | — | — | 1 | 7.96 |
| CHEMBL4848739 | — | — | 1 | 7.85 |
| CHEMBL4872775 | — | — | 1 | 7.68 |
| CHEMBL4864483 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4854745 | — | EC50 | = | 0.74 | nM | 9.13 |
| CHEMBL4861625 | — | EC50 | = | 0.84 | nM | 9.08 |
| CHEMBL4867460 | — | EC50 | = | 0.87 | nM | 9.06 |
| CHEMBL4860414 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4852843 | — | EC50 | = | 0.89 | nM | 9.05 |
| CHEMBL4873949 | — | EC50 | = | 0.97 | nM | 9.01 |
| CHEMBL4868904 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4853705 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4867267 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4846860 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4851358 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4847518 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4878171 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4860893 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4874354 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4850190 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4846178 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4853843 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4849342 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4869259 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4873952 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4868831 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4849067 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4854567 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4862596 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4853251 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4862485 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4848739 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4872775 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4864483 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4868773 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4862310 | — | EC50 | > | 10.0 | nM | - |
| CHEMBL4874774 | — | EC50 | < | 0.5 | nM | - |