Assay Detail
Binding
CHEMBL4013545
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in HEK293F cells using histone H4 as substrate preincubated for 15 mins followed by substrate/S-adenosyl methionine addition measured after 60 mins by alpha LISA assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 5.30 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4092336 | — | — | 1 | 6.48 |
| CHEMBL4078091 | — | — | 1 | 6.48 |
| CHEMBL4071851 | — | — | 1 | 6.47 |
| CHEMBL4060448 | — | — | 1 | 6.46 |
| CHEMBL4102308 | — | — | 1 | 6.30 |
| CHEMBL4096718 | — | — | 1 | 6.28 |
| CHEMBL4093573 | — | — | 1 | 6.08 |
| CHEMBL4065013 | — | — | 1 | 5.85 |
| CHEMBL4103903 | — | — | 1 | 5.80 |
| CHEMBL4098309 | — | — | 1 | 5.72 |
| CHEMBL4097311 | — | — | 1 | 5.62 |
| CHEMBL4069130 | — | — | 1 | 5.55 |
| CHEMBL4074067 | — | — | 1 | 5.54 |
| CHEMBL4063223 | — | — | 1 | 5.48 |
| CHEMBL4063156 | — | — | 1 | 5.09 |
| CHEMBL4096147 | — | — | 1 | 5.08 |
| CHEMBL4071771 | — | — | 1 | 4.75 |
| CHEMBL1289144 | — | — | 1 | 4.72 |
| CHEMBL1412370 | — | — | 1 | 4.64 |
| CHEMBL4094598 | — | — | 1 | 4.60 |
| CHEMBL4060373 | — | — | 1 | 4.58 |
| CHEMBL4070981 | — | — | 1 | 4.57 |
| CHEMBL4082279 | — | — | 1 | 4.57 |
| CHEMBL1290699 | — | — | 1 | 4.48 |
| CHEMBL4085982 | — | — | 1 | 4.40 |
| CHEMBL3590214 | — | — | 1 | 4.33 |
| CHEMBL4068547 | — | — | 1 | 4.28 |
| CHEMBL4077572 | — | — | 1 | 4.06 |
| CHEMBL4092698 | — | — | 1 | - |
| CHEMBL1349478 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4092336 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4078091 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4071851 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4060448 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4102308 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4096718 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4093573 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4065013 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4103903 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4098309 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4097311 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4069130 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4074067 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4063223 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4063156 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4096147 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4071771 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1289144 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1412370 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4094598 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4060373 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4070981 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4082279 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL1290699 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4085982 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3590214 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL4068547 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL4077572 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL4084944 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1472767 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4081799 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4071261 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4102895 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4086889 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4074678 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1349478 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4092698 | — | IC50 | > | 100000.0 | nM | - |