Assay Detail
Binding
CHEMBL3591483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) 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 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein arginine N-methyltransferase 8 (CHEMBL3108648) ↗| 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 | 7.38 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589029 | — | — | 1 | 8.70 |
| CHEMBL3589030 | — | — | 1 | 8.15 |
| CHEMBL3589026 | — | — | 1 | 8.00 |
| CHEMBL3589028 | — | — | 1 | 8.00 |
| CHEMBL3589031 | — | — | 1 | 8.00 |
| CHEMBL3589027 | — | — | 1 | 7.85 |
| CHEMBL3589037 | — | — | 1 | 7.68 |
| CHEMBL3589033 | — | — | 1 | 7.66 |
| CHEMBL3589032 | — | — | 1 | 7.66 |
| CHEMBL3589036 | — | — | 1 | 7.64 |
| CHEMBL3589913 | — | — | 1 | 7.55 |
| CHEMBL3589038 | — | — | 1 | 7.36 |
| CHEMBL3589034 | — | — | 1 | 7.26 |
| CHEMBL3590417 | — | — | 1 | 7.19 |
| CHEMBL3589912 | — | — | 1 | 7.17 |
| CHEMBL3589035 | — | — | 1 | 7.16 |
| CHEMBL3589042 | — | — | 1 | 6.75 |
| CHEMBL3589039 | — | — | 1 | 6.65 |
| CHEMBL3589043 | — | — | 1 | 6.46 |
| CHEMBL3589040 | — | — | 1 | 6.35 |
| CHEMBL3589041 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589029 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3589030 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3589026 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3589028 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3589031 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3589027 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3589037 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3589033 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3589032 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3589036 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3589913 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3589038 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3589034 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3590417 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3589912 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3589035 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3589042 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL3589039 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL3589043 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL3589040 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3589041 | — | IC50 | = | 1500.0 | nM | 5.82 |