Assay Detail
Binding
CHEMBL3591482
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLAG and hexa-histidine tagged full-length human PRMT6 expressed in HEK293F cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293F |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein arginine N-methyltransferase 6 (CHEMBL1275221) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.68 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589029 | — | — | 1 | 8.70 |
| CHEMBL3589043 | — | — | 1 | 8.70 |
| CHEMBL3589042 | — | — | 1 | 8.52 |
| CHEMBL3590417 | — | — | 1 | 8.30 |
| CHEMBL3589026 | — | — | 1 | 8.15 |
| CHEMBL3589030 | — | — | 1 | 8.10 |
| CHEMBL3589039 | — | — | 1 | 8.00 |
| CHEMBL3589028 | — | — | 1 | 8.00 |
| CHEMBL3589031 | — | — | 1 | 8.00 |
| CHEMBL3589027 | — | — | 1 | 7.96 |
| CHEMBL3589912 | — | — | 1 | 7.96 |
| CHEMBL3589040 | — | — | 1 | 7.89 |
| CHEMBL3589041 | — | — | 1 | 7.70 |
| CHEMBL3589032 | — | — | 1 | 7.64 |
| CHEMBL3589033 | — | — | 1 | 7.60 |
| CHEMBL3589913 | — | — | 1 | 7.60 |
| CHEMBL3589034 | — | — | 1 | 7.50 |
| CHEMBL3589035 | — | — | 1 | 6.50 |
| CHEMBL3589036 | — | — | 1 | 6.49 |
| CHEMBL3589037 | — | — | 1 | 6.34 |
| CHEMBL3589038 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589029 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3589043 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3589042 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3590417 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3589026 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3589030 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3589039 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3589028 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3589031 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3589027 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3589912 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3589040 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3589041 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3589032 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3589033 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3589913 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3589034 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3589035 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL3589036 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL3589037 | — | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL3589038 | — | IC50 | = | 1900.0 | nM | 5.72 |