Assay Detail
Binding
CHEMBL4380478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His-tagged MLL1 complex (MLL1/Ash2L/RbBP5/WDR5/DPY-30)-mediated HMT activity using oligonucleosome as substrate preincubated for 15 mins followed by [3H]-SAM addition after 1 hr
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.08 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588661 | — | — | 1 | 8.66 |
| CHEMBL4534270 | — | — | 1 | 8.64 |
| CHEMBL4453355 | — | — | 1 | 8.60 |
| CHEMBL4557848 | — | — | 1 | 8.47 |
| CHEMBL4593719 | — | — | 1 | 8.47 |
| CHEMBL4435250 | — | — | 1 | 8.47 |
| CHEMBL4462065 | — | — | 1 | 8.40 |
| CHEMBL4476662 | — | — | 1 | 8.33 |
| CHEMBL4439051 | — | — | 1 | 8.07 |
| CHEMBL4436638 | — | — | 1 | 8.00 |
| CHEMBL4585441 | — | — | 1 | 7.94 |
| CHEMBL4578661 | — | — | 1 | 7.85 |
| CHEMBL4556167 | — | — | 1 | 7.85 |
| CHEMBL4530969 | — | — | 1 | 7.82 |
| CHEMBL4555492 | — | — | 1 | 7.62 |
| CHEMBL4474045 | — | — | 1 | 7.55 |
| CHEMBL4567878 | — | — | 1 | 7.36 |
| CHEMBL4570860 | — | — | 1 | 7.26 |
| CHEMBL4463776 | — | — | 1 | - |
| CHEMBL4528067 | — | — | 1 | - |
| CHEMBL4463486 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588661 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4534270 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4453355 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4557848 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4593719 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4435250 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4462065 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4476662 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4439051 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4436638 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4585441 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL4578661 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4556167 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4530969 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4555492 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL4474045 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL4567878 | — | IC50 | = | 43.3 | nM | 7.36 |
| CHEMBL4570860 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4463776 | — | IC50 | < | 2.0 | nM | - |
| CHEMBL4528067 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4463486 | — | IC50 | < | 2.0 | nM | - |