Assay Detail
Binding
CHEMBL5038526
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RNA polymerase 1 in human A-375 assessed as RPA194 degradation measured after 4 hrs by Hoechst 33342 staining based assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
DNA-directed RNA polymerase I subunit RPA1 (CHEMBL3286067) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Evaluation of Novel Angular Fused Pyridoquinazolinonecarboxamides as RNA Polymerase I Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 5.92 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5091256 | — | — | 1 | 6.80 |
| CHEMBL3289420 | — | — | 1 | 6.75 |
| CHEMBL5091818 | — | — | 1 | 6.68 |
| CHEMBL3289398 | — | — | 1 | 6.48 |
| CHEMBL3289421 | — | — | 1 | 6.43 |
| CHEMBL5093823 | — | — | 1 | 6.38 |
| CHEMBL5072152 | — | — | 1 | 6.33 |
| CHEMBL5076121 | — | — | 1 | 6.27 |
| CHEMBL5088110 | — | — | 1 | 6.23 |
| CHEMBL5074659 | — | — | 1 | 6.22 |
| CHEMBL5089364 | — | — | 1 | 6.22 |
| CHEMBL5091051 | — | — | 1 | 6.19 |
| CHEMBL5094886 | — | — | 1 | 6.19 |
| CHEMBL5082214 | — | — | 1 | 6.13 |
| CHEMBL5090345 | — | — | 1 | 6.11 |
| CHEMBL5093028 | — | — | 1 | 6.11 |
| CHEMBL5080399 | — | — | 1 | 6.04 |
| CHEMBL5071620 | — | — | 1 | 6.00 |
| CHEMBL5080842 | — | — | 1 | 6.00 |
| CHEMBL5077311 | — | — | 1 | 5.98 |
| CHEMBL5084657 | — | — | 1 | 5.94 |
| CHEMBL5094505 | — | — | 1 | 5.86 |
| CHEMBL5091868 | — | — | 1 | 5.77 |
| CHEMBL5089676 | — | — | 1 | 5.72 |
| CHEMBL5091418 | — | — | 1 | 5.41 |
| CHEMBL5083095 | — | — | 1 | 5.38 |
| CHEMBL5088652 | — | — | 1 | 5.26 |
| CHEMBL5080196 | — | — | 1 | 5.24 |
| CHEMBL5089657 | — | — | 1 | 5.22 |
| CHEMBL5081206 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5091256 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3289420 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5091818 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3289398 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3289421 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5093823 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL5072152 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5076121 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5088110 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5074659 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5089364 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5091051 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5094886 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5082214 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5093028 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5090345 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL5080399 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5071620 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5080842 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL5077311 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL5084657 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL5094505 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL5091868 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5089676 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5091418 | — | IC50 | = | 3940.0 | nM | 5.41 |
| CHEMBL5083095 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5088652 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5080196 | — | IC50 | = | 5750.0 | nM | 5.24 |
| CHEMBL5089657 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5081206 | — | IC50 | = | 6860.0 | nM | 5.16 |
| CHEMBL5072213 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL5085694 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5087954 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5092554 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5081532 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5087053 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5082744 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5089702 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5072616 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5088523 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5075517 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5079682 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5086969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5092630 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5087593 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5078970 | — | IC50 | > | 10000.0 | nM | - |