Assay Detail
Binding
CHEMBL4222305
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-SUMO tagged DOT1L (1 to 416 residues) expressed in Escherichia coli BL21(DE3) using oligonucleosome as substrate measured after 30 mins in presence of SAM by AlphaLISA assay
4
Total Activities
4
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, H3 lysine-79 specific (CHEMBL1795117) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent DOT1L inhibitors by AlphaLISA based High Throughput Screening assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.94 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171169 | — | — | 1 | 7.85 |
| CHEMBL45041 | — | — | 1 | 6.77 |
| CHEMBL4228404 | — | — | 1 | 4.68 |
| CHEMBL1214186 | SINEFUNGIN | 2.0 | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171169 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL45041 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4228404 | — | IC50 | = | 20940.0 | nM | 4.68 |
| CHEMBL1214186 | SINEFUNGIN | IC50 | = | 33710.0 | nM | 4.47 |