Assay Detail
Binding
CHEMBL5737862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzymatic Assay: Fluorogenic biochemical assays used recombinant full-length FEN-1 or catalytic domains of Exo1, XPG or GEN1 and 200 nM of a DNA substrate (formed by annealing three oligonucleotidesquencher (5′-CAC GTT GAC TAC CGC TCA ATC CTG ACG AAC ACA TC-BHQ2), flap (5′-TAMRA-GA TGT CAA GCA GTC CTA ACT TTG AGG CAG AGT CCG C) and template (5′-GC GGA CTC TGC CTC AAG ACG GTA GTC AAC GTG-3′) (PMID: 21062821)) in 50 mM Tris pH 8.0, 10 mM MgCl2, 1 mM DTT, and 0.01% Tween-20. Inhibitors arrayed in dose response were added from DMSO stocks (using a V&P 384-pintool head) to the enzyme solution in low volume, black polystyrene 384-well plates (Corning #3677) 15 minutes prior to the addition of the DNA substrate. Reactions were allowed to proceed for 2-4 hours at 25° C. or 37° C. Fluorescence data (Excitation: 530 nm/10 nm bandwidth; Emission: 590 nm/20 nm bandwith) were measured with an Infinite M1000 plate reader (Tecan).
213
Total Activities
71
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
3-hydroxy-quinazoline-2,4-dione derivatives and their use as nuclease modulators
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 71 | 7.49 | 8.25 |
| kon | 71 | - | - |
| k_off | 71 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5968390 | — | — | 3 | 8.25 |
| CHEMBL5774469 | — | — | 3 | 8.18 |
| CHEMBL5823760 | — | — | 3 | 8.17 |
| CHEMBL5771022 | — | — | 3 | 8.12 |
| CHEMBL5866031 | — | — | 3 | 8.07 |
| CHEMBL5845789 | — | — | 3 | 8.07 |
| CHEMBL5769698 | — | — | 3 | 8.03 |
| CHEMBL5760085 | — | — | 3 | 8.03 |
| CHEMBL5971510 | — | — | 3 | 8.03 |
| CHEMBL5886889 | — | — | 3 | 8.03 |
| CHEMBL5769513 | — | — | 3 | 8.01 |
| CHEMBL5800240 | — | — | 3 | 8.00 |
| CHEMBL6022323 | — | — | 3 | 8.00 |
| CHEMBL5868369 | — | — | 3 | 7.96 |
| CHEMBL5822573 | — | — | 3 | 7.96 |
| CHEMBL5879460 | — | — | 3 | 7.94 |
| CHEMBL5751812 | — | — | 3 | 7.94 |
| CHEMBL5813177 | — | — | 3 | 7.89 |
| CHEMBL6059692 | — | — | 3 | 7.89 |
| CHEMBL6056794 | — | — | 3 | 7.89 |
| CHEMBL5758696 | — | — | 3 | 7.88 |
| CHEMBL5862815 | — | — | 3 | 7.86 |
| CHEMBL5972340 | — | — | 3 | 7.85 |
| CHEMBL6042696 | — | — | 3 | 7.85 |
| CHEMBL5780812 | — | — | 3 | 7.84 |
| CHEMBL5998713 | — | — | 3 | 7.83 |
| CHEMBL6011484 | — | — | 3 | 7.83 |
| CHEMBL6010757 | — | — | 3 | 7.81 |
| CHEMBL5855080 | — | — | 3 | 7.80 |
| CHEMBL5952329 | — | — | 3 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5968390 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5774469 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5823760 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5771022 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5866031 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5845789 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5886889 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5769698 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5760085 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5971510 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5769513 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL6022323 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5800240 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5822573 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5868369 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL5879460 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5751812 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5813177 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL6059692 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL6056794 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL5758696 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL5862815 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL6042696 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5972340 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL5780812 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5998713 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL6011484 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL6010757 | — | IC50 | = | 15.6 | nM | 7.81 |
| CHEMBL5952329 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5855080 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL5800924 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL5899616 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL5995448 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL5797788 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL5894124 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL5819838 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL6064176 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL5959749 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL6028630 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL5766160 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL5850135 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL182687 | — | IC50 | = | 20.8 | nM | 7.68 |
| CHEMBL5822823 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL5740169 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL5799671 | — | IC50 | = | 26.1 | nM | 7.58 |
| CHEMBL5837104 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL5851038 | — | IC50 | = | 28.9 | nM | 7.54 |
| CHEMBL5897545 | — | IC50 | = | 35.4 | nM | 7.45 |
| CHEMBL5827550 | — | IC50 | = | 37.3 | nM | 7.43 |
| CHEMBL5937600 | — | IC50 | = | 42.0 | nM | 7.38 |