Assay Detail
Binding
CHEMBL3862045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 17AAG-induced HSF1-mediated HSP72 expression in human U2OS cells preincubated for 1 hr followed by 17AAG addition measured after overnight incubation by ArrayScan analysis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.47 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3975567 | — | — | 1 | 7.85 |
| CHEMBL3937369 | — | — | 1 | 7.82 |
| CHEMBL3911352 | — | — | 1 | 7.55 |
| CHEMBL3964729 | — | — | 1 | 7.41 |
| CHEMBL3972065 | — | — | 1 | 7.35 |
| CHEMBL3953713 | — | — | 1 | 7.26 |
| CHEMBL3928361 | — | — | 1 | 7.24 |
| CHEMBL3919811 | — | — | 1 | 7.10 |
| CHEMBL3983798 | — | — | 1 | 6.78 |
| CHEMBL3901185 | — | — | 1 | 6.70 |
| CHEMBL3900925 | — | — | 1 | 6.53 |
| CHEMBL3919459 | — | — | 1 | 6.35 |
| CHEMBL3946252 | — | — | 1 | 6.21 |
| CHEMBL3936187 | — | — | 1 | 6.12 |
| CHEMBL3944589 | — | — | 1 | 6.08 |
| CHEMBL3955977 | — | — | 1 | 6.05 |
| CHEMBL3923966 | — | — | 1 | 5.87 |
| CHEMBL3947240 | — | — | 1 | 5.86 |
| CHEMBL3905315 | — | — | 1 | 5.70 |
| CHEMBL3891011 | — | — | 1 | 5.63 |
| CHEMBL3916672 | — | — | 1 | 5.37 |
| CHEMBL3922414 | — | — | 1 | 5.21 |
| CHEMBL3957716 | — | — | 1 | 4.75 |
| CHEMBL3973213 | — | — | 1 | - |
| CHEMBL3969412 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3975567 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3937369 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3911352 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3964729 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3972065 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3953713 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3928361 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3919811 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3983798 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3901185 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL3900925 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL3919459 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3946252 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3936187 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3944589 | — | IC50 | = | 842.0 | nM | 6.08 |
| CHEMBL3955977 | — | IC50 | = | 884.0 | nM | 6.05 |
| CHEMBL3923966 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL3947240 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL3905315 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3891011 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL3916672 | — | IC50 | = | 4280.0 | nM | 5.37 |
| CHEMBL3922414 | — | IC50 | = | 6150.0 | nM | 5.21 |
| CHEMBL3957716 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL3973213 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL3969412 | — | IC50 | > | 30000.0 | nM | - |