Assay Detail
Binding
CHEMBL5380643
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of WDR5 (unknown origin) assessed as inhibition constant in presence of 5-{[(5S)-5-(6-{6-[(2S)-2-[(2S)-6-amino-2-[(2S)-5-carbamimidamido-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S,3R)-2-[(2S)-5-carbamimidamido-2-[(2S)-2-acetamidopropanamido]pentanamido]-3-hydroxybutanamido]-4-carboxybutanamido]-3-methylbutanamido]-3-(1H-imidazol-5-yl)propanamido]-4-methylpentanamido]pentanamido]hexanamido]-3-hydroxypropanamido]hexanamido}hexanamido)-5-carbamoylpentyl]carbamoyl}-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid by fluorescence polarization 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 |
Publication
Small molecule WDR5 inhibitors down-regulate lncRNA expression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 9.24 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5434345 | — | — | 1 | 9.57 |
| CHEMBL3798846 | — | — | 1 | 8.91 |
| CHEMBL4472649 | — | — | 1 | - |
| CHEMBL5435898 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5434345 | — | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL3798846 | — | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL4472649 | — | Ki | > | 40000.0 | nM | - |
| CHEMBL5435898 | — | Ki | > | 40000.0 | nM | - |