Assay Detail
Binding
CHEMBL3626067
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SETD8 catalytic domain expressed in Escherichia coli assessed as reduction in transfer of tritiated methyl group from [3H]SAM to biotinylated H4 (1 to 24) peptide substrate by scintillation proximity assay
43
Total Activities
43
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 |
Publication
Structure-activity relationship studies of SETD8 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 4.63 | 5.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3318284 | — | — | 1 | 5.19 |
| CHEMBL3621706 | — | — | 1 | 5.10 |
| CHEMBL3621701 | — | — | 1 | 5.10 |
| CHEMBL3621704 | — | — | 1 | 5.06 |
| CHEMBL3622290 | — | — | 1 | 5.02 |
| CHEMBL3622293 | — | — | 1 | 4.96 |
| CHEMBL3622271 | — | — | 1 | 4.82 |
| CHEMBL3621703 | — | — | 1 | 4.62 |
| CHEMBL3622261 | — | — | 1 | 4.58 |
| CHEMBL3622262 | — | — | 1 | 4.40 |
| CHEMBL3622263 | — | — | 1 | 4.40 |
| CHEMBL3621702 | — | — | 1 | 4.40 |
| CHEMBL3622264 | — | — | 1 | 4.37 |
| CHEMBL3622292 | — | — | 1 | 4.34 |
| CHEMBL3622294 | — | — | 1 | 4.32 |
| CHEMBL3622289 | — | — | 1 | 4.28 |
| CHEMBL3622291 | — | — | 1 | 4.21 |
| CHEMBL3622267 | — | — | 1 | 4.20 |
| CHEMBL3622274 | — | — | 1 | - |
| CHEMBL3622270 | — | — | 1 | - |
| CHEMBL3622272 | — | — | 1 | - |
| CHEMBL3622273 | — | — | 1 | - |
| CHEMBL3622281 | — | — | 1 | - |
| CHEMBL3622269 | — | — | 1 | - |
| CHEMBL3622268 | — | — | 1 | - |
| CHEMBL3622266 | — | — | 1 | - |
| CHEMBL3622265 | — | — | 1 | - |
| CHEMBL3621705 | — | — | 1 | - |
| CHEMBL3622275 | — | — | 1 | - |
| CHEMBL3622276 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3318284 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3621706 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3621701 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3621704 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL3622290 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL3622293 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3622271 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL3621703 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3622261 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL3622262 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3622263 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3621702 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3622264 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL3622292 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL3622294 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL3622289 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL3622291 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL3622267 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL3622288 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3621699 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL3621700 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622286 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622285 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622284 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622283 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622282 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622287 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622280 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622279 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622278 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622277 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622276 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622275 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3621705 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622265 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622266 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622268 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622269 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622281 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622273 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622272 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3622270 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL3622274 | — | IC50 | > | 250000.0 | nM | - |