Assay Detail
Binding
CHEMBL3779310
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged TRIM24-PHD/bromodomain expressed in Escherichia coli strains BL21 (DE3) cells using biotinylated H3K23ac (1 to 33 residues) peptide after 1 hr by AlphaScreen assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BL21-DE3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transcription intermediary factor 1-alpha (CHEMBL3108638) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.38 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774575 | — | — | 1 | 8.12 |
| CHEMBL3775251 | — | — | 1 | 8.10 |
| CHEMBL3774933 | — | — | 1 | 8.08 |
| CHEMBL3775901 | — | — | 1 | 8.00 |
| CHEMBL3775348 | — | — | 1 | 7.96 |
| CHEMBL3774542 | — | — | 1 | 7.89 |
| CHEMBL3774766 | — | — | 1 | 7.89 |
| CHEMBL3775853 | — | — | 1 | 7.37 |
| CHEMBL3775073 | — | — | 1 | 7.28 |
| CHEMBL3774507 | — | — | 1 | 7.24 |
| CHEMBL3774770 | — | — | 1 | 7.22 |
| CHEMBL3775689 | — | — | 1 | 7.00 |
| CHEMBL3775132 | — | — | 1 | 6.96 |
| CHEMBL3774529 | — | — | 1 | 6.89 |
| CHEMBL3775263 | — | — | 1 | 6.85 |
| CHEMBL3774638 | — | — | 1 | 6.80 |
| CHEMBL3774452 | — | — | 1 | 6.80 |
| CHEMBL3774653 | — | — | 1 | 6.75 |
| CHEMBL3775286 | — | — | 1 | 6.66 |
| CHEMBL3775640 | — | — | 1 | 6.57 |
| CHEMBL3774883 | — | — | 1 | 6.57 |
| CHEMBL3770259 | — | — | 1 | 5.82 |
| CHEMBL3775297 | — | — | 1 | 5.77 |
| CHEMBL3774616 | — | — | 1 | 5.70 |
| CHEMBL3775687 | — | — | 1 | 5.62 |
| CHEMBL3775559 | — | — | 1 | 5.60 |
| CHEMBL3774404 | — | — | 1 | 5.55 |
| CHEMBL3774673 | — | — | 1 | 5.43 |
| CHEMBL3774804 | — | — | 1 | 5.40 |
| CHEMBL3775715 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774575 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3775251 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL3774933 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3775901 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3775348 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3774542 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3774766 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3775853 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3775073 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3774507 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3774770 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3775689 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3775132 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3774529 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3775263 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3774638 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3774452 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3774653 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3775286 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3775640 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3774883 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3770259 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3775297 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3774616 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3775687 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3775559 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3774404 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3774673 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3774804 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3775715 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3774650 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3775440 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL1557110 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL1365878 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3775616 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3774967 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1734009 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3775315 | — | IC50 | = | 36000.0 | nM | 4.44 |