Assay Detail
Binding
CHEMBL3829237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant SET7/9 (unknown origin) using biotinylated histone H3-derived peptide/SAM as substrate after 60 mins by AlphaLISA assay
12
Total Activities
12
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
Histone-lysine N-methyltransferase SETD7 (CHEMBL5523) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Steric structure-activity relationship of cyproheptadine derivatives as inhibitors of histone methyltransferase Set7/9.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.71 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL516 | CYPROHEPTADINE | 4.0 | 1 | 5.47 |
| CHEMBL152408 | PIMETHIXENE | 2.0 | 1 | 5.37 |
| CHEMBL152407 | — | — | 1 | 4.79 |
| CHEMBL348199 | — | — | 1 | 4.38 |
| CHEMBL152622 | — | — | 1 | 4.23 |
| CHEMBL347536 | — | — | 1 | 4.02 |
| CHEMBL3827431 | — | — | 1 | - |
| CHEMBL3827386 | — | — | 1 | - |
| CHEMBL3828123 | — | — | 1 | - |
| CHEMBL3827652 | — | — | 1 | - |
| CHEMBL20468 | — | — | 1 | - |
| CHEMBL3828393 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL516 | CYPROHEPTADINE | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL152408 | PIMETHIXENE | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL152407 | — | IC50 | = | 16300.0 | nM | 4.79 |
| CHEMBL348199 | — | IC50 | = | 41500.0 | nM | 4.38 |
| CHEMBL152622 | — | IC50 | = | 59100.0 | nM | 4.23 |
| CHEMBL347536 | — | IC50 | = | 94600.0 | nM | 4.02 |
| CHEMBL3827431 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3827386 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3828123 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3827652 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL20468 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3828393 | — | IC50 | > | 100000.0 | nM | - |