Assay Detail
Binding
CHEMBL5578005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PRMT5 in human HCT-116 cells with MTAP KO assessed as decrease in SMDA level incubated for 48 hrs by immunofluorescence analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein arginine N-methyltransferase 5 (CHEMBL1795116) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and <i>In Vivo</i> Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.65 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5589904 | — | — | 1 | 8.40 |
| CHEMBL5593070 | — | — | 1 | 8.40 |
| CHEMBL5594655 | — | — | 1 | 8.30 |
| CHEMBL5594567 | — | — | 1 | 8.22 |
| CHEMBL5583712 | — | — | 1 | 7.22 |
| CHEMBL5592096 | — | — | 1 | 7.18 |
| CHEMBL5591445 | — | — | 1 | 7.12 |
| CHEMBL5590720 | — | — | 1 | 6.85 |
| CHEMBL5593804 | — | — | 1 | 6.82 |
| CHEMBL5594801 | — | — | 1 | 6.62 |
| CHEMBL5590589 | — | — | 1 | 6.52 |
| CHEMBL5583660 | — | — | 1 | 6.42 |
| CHEMBL5584160 | — | — | 1 | 6.42 |
| CHEMBL5590816 | — | — | 1 | 6.24 |
| CHEMBL5594198 | — | — | 1 | 6.18 |
| CHEMBL5593457 | — | — | 1 | 6.17 |
| CHEMBL5591144 | — | — | 1 | 5.89 |
| CHEMBL5593058 | — | — | 1 | 5.32 |
| CHEMBL5591780 | — | — | 1 | 5.19 |
| CHEMBL5593194 | — | — | 1 | 5.11 |
| CHEMBL5593534 | — | — | 1 | 5.10 |
| CHEMBL5589874 | — | — | 1 | - |
| CHEMBL5594285 | — | — | 1 | - |
| CHEMBL5590674 | — | — | 1 | - |
| CHEMBL5590521 | — | — | 1 | - |
| CHEMBL5592639 | — | — | 1 | - |
| CHEMBL5584072 | — | — | 1 | - |
| CHEMBL5593993 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5589904 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5593070 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5594655 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5594567 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5583712 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5592096 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5591445 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5590720 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5593804 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5594801 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5590589 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5583660 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5584160 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5590816 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5594198 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL5593457 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL5591144 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5593058 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5591780 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5593194 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL5593534 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL5589874 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5594285 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5590674 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5590521 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5592639 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5584072 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5593993 | — | IC50 | > | 30000.0 | nM | - |