Assay Detail
Binding
CHEMBL4189067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type recombinant human histone lysine methyltransferase GLP (951 to 1235 residues) expressed in Escherichia coli Rosetta BL21 DE3 PlysS using ARTKQTARKSTGGKA as substrate preincubated for 5 mins followed by substrate/SAM addition measured after 60 mins by MALDI-TOF MS analysis
19
Total Activities
19
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 EHMT1 (CHEMBL6031) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibition of histone lysine methyltransferases G9a and GLP by ejection of structural Zn(II).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.61 | 6.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51085 | EBSELEN | 3.0 | 1 | 6.14 |
| CHEMBL3122204 | — | — | 1 | 6.07 |
| CHEMBL4208308 | — | — | 1 | 6.00 |
| CHEMBL3335712 | — | — | 1 | 5.96 |
| CHEMBL120563 | THIRAM | 2.0 | 1 | 5.96 |
| CHEMBL3335713 | — | — | 1 | 5.82 |
| CHEMBL964 | DISULFIRAM | 4.0 | 1 | 5.80 |
| CHEMBL28517 | E927A | — | 1 | 5.77 |
| CHEMBL118678 | — | — | 1 | 5.57 |
| CHEMBL39469 | BENZENE SELENOIC ACID | — | 1 | 5.31 |
| CHEMBL55934 | NAPHTHOQUINONE | — | 1 | 4.85 |
| CHEMBL107217 | DITIOCARB SODIUM | 2.0 | 1 | 4.09 |
| CHEMBL1543 | GLUTATHIONE | 3.0 | 1 | - |
| CHEMBL1372 | OXIGLUTATIONE | 4.0 | 1 | - |
| CHEMBL602 | CYSTEAMINE | 4.0 | 1 | - |
| CHEMBL1594935 | CYSTAMINE DIHYDROCHLORIDE | — | 1 | - |
| CHEMBL114503 | SODIUM SELENATE | 3.0 | 1 | - |
| CHEMBL1221925 | — | — | 1 | - |
| CHEMBL55659 | ANTHRAQUINONE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51085 | EBSELEN | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3122204 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4208308 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3335712 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL120563 | THIRAM | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3335713 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL964 | DISULFIRAM | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL28517 | E927A | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL118678 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL39469 | BENZENE SELENOIC ACID | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL55934 | NAPHTHOQUINONE | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL107217 | DITIOCARB SODIUM | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL1543 | GLUTATHIONE | IC50 | > | 100000.0 | nM | - |
| CHEMBL1372 | OXIGLUTATIONE | IC50 | > | 100000.0 | nM | - |
| CHEMBL602 | CYSTEAMINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL1594935 | CYSTAMINE DIHYDROCHLORIDE | IC50 | > | 100000.0 | nM | - |
| CHEMBL114503 | SODIUM SELENATE | IC50 | > | 100000.0 | nM | - |
| CHEMBL1221925 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL55659 | ANTHRAQUINONE | IC50 | > | 100000.0 | nM | - |