Assay Detail
Binding
CHEMBL4380479
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of human N-terminal His6-SUMO tagged WDR5 (22 to 334 residues) expressed in Escherichia coli BL21-Gold(DE3) cells using 10-mer-Thr-FAM peptide as substrate after 1 hr by TR-FRET assay
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| Kd | 21 | 10.04 | 10.64 |
| Ki | 1 | 10.36 | 10.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4463486 | — | — | 1 | 10.64 |
| CHEMBL4476662 | — | — | 1 | 10.57 |
| CHEMBL4534270 | — | — | 1 | 10.52 |
| CHEMBL4557848 | — | — | 1 | 10.52 |
| CHEMBL4585441 | — | — | 1 | 10.49 |
| CHEMBL4530969 | — | — | 1 | 10.48 |
| CHEMBL4439051 | — | — | 1 | 10.46 |
| CHEMBL4453355 | — | — | 1 | 10.37 |
| CHEMBL4441671 | — | — | 1 | 10.36 |
| CHEMBL4435250 | — | — | 1 | 10.31 |
| CHEMBL4555492 | — | — | 1 | 10.26 |
| CHEMBL4593719 | — | — | 1 | 10.21 |
| CHEMBL4556167 | — | — | 1 | 10.20 |
| CHEMBL4474045 | — | — | 1 | 10.05 |
| CHEMBL4578661 | — | — | 1 | 9.85 |
| CHEMBL4436638 | — | — | 1 | 9.80 |
| CHEMBL4570860 | — | — | 1 | 9.30 |
| CHEMBL4567878 | — | — | 1 | 8.82 |
| CHEMBL4528067 | — | — | 1 | 7.80 |
| CHEMBL4463776 | — | — | 1 | - |
| CHEMBL4588661 | — | — | 1 | - |
| CHEMBL4462065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4463486 | — | Kd | = | 0.023 | nM | 10.64 |
| CHEMBL4476662 | — | Kd | = | 0.027 | nM | 10.57 |
| CHEMBL4534270 | — | Kd | = | 0.03 | nM | 10.52 |
| CHEMBL4557848 | — | Kd | = | 0.03 | nM | 10.52 |
| CHEMBL4585441 | — | Kd | = | 0.032 | nM | 10.49 |
| CHEMBL4530969 | — | Kd | = | 0.033 | nM | 10.48 |
| CHEMBL4439051 | — | Kd | = | 0.035 | nM | 10.46 |
| CHEMBL4453355 | — | Kd | = | 0.043 | nM | 10.37 |
| CHEMBL4441671 | — | Ki | = | 0.044 | nM | 10.36 |
| CHEMBL4435250 | — | Kd | = | 0.049 | nM | 10.31 |
| CHEMBL4555492 | — | Kd | = | 0.055 | nM | 10.26 |
| CHEMBL4593719 | — | Kd | = | 0.061 | nM | 10.21 |
| CHEMBL4556167 | — | Kd | = | 0.063 | nM | 10.20 |
| CHEMBL4474045 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL4578661 | — | Kd | = | 0.14 | nM | 9.85 |
| CHEMBL4436638 | — | Kd | = | 0.16 | nM | 9.80 |
| CHEMBL4570860 | — | Kd | = | 0.5 | nM | 9.30 |
| CHEMBL4567878 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL4528067 | — | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL4463776 | — | Kd | < | 0.02 | nM | - |
| CHEMBL4588661 | — | Kd | < | 0.02 | nM | - |
| CHEMBL4462065 | — | Kd | < | 0.02 | nM | - |