Assay Detail
Binding
CHEMBL5111529
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DNA polymerase theta pol domain (1819 to 2590 residues) expressed in Escherichia coli BL21 (DE3) cells preincubated for 15 mins followed by DNA and dNTP addition and measured after 120 mins by Picogreen dye fluorescence intensity analysis
48
Total Activities
48
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
Identification of <b>RP-6685</b>, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 7.59 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5204203 | — | — | 1 | 10.17 |
| CHEMBL5175156 | — | — | 1 | 9.70 |
| CHEMBL5206022 | — | — | 1 | 9.40 |
| CHEMBL5197367 | — | — | 1 | 9.29 |
| CHEMBL5174509 | — | — | 1 | 9.14 |
| CHEMBL5197173 | — | — | 1 | 9.12 |
| CHEMBL5170373 | — | — | 1 | 9.09 |
| CHEMBL5194637 | — | — | 1 | 9.04 |
| CHEMBL5197021 | — | — | 1 | 9.00 |
| CHEMBL5187337 | — | — | 1 | 8.92 |
| CHEMBL5188048 | — | — | 1 | 8.85 |
| CHEMBL5181369 | — | — | 1 | 8.80 |
| CHEMBL5174376 | — | — | 1 | 8.77 |
| CHEMBL5200250 | — | — | 1 | 8.68 |
| CHEMBL5174283 | — | — | 1 | 8.60 |
| CHEMBL5195161 | — | — | 1 | 8.54 |
| CHEMBL5194194 | — | — | 1 | 8.41 |
| CHEMBL5206029 | — | — | 1 | 8.38 |
| CHEMBL5202450 | — | — | 1 | 8.31 |
| CHEMBL5187422 | — | — | 1 | 8.24 |
| CHEMBL5200171 | — | — | 1 | 8.05 |
| CHEMBL5178605 | — | — | 1 | 7.85 |
| CHEMBL5203967 | — | — | 1 | 7.85 |
| CHEMBL5185359 | — | — | 1 | 7.77 |
| CHEMBL5195920 | — | — | 1 | 7.77 |
| CHEMBL5181740 | — | — | 1 | 7.72 |
| CHEMBL5178606 | — | — | 1 | 7.40 |
| CHEMBL5206197 | — | — | 1 | 7.38 |
| CHEMBL5208584 | — | — | 1 | 7.24 |
| CHEMBL5181730 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5204203 | — | IC50 | = | 0.068 | nM | 10.17 |
| CHEMBL5175156 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5206022 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5197367 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL5174509 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5197173 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL5170373 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL5194637 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL5197021 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL5187337 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5188048 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5181369 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5174376 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5200250 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5174283 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5195161 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5194194 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5206029 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5202450 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5187422 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5200171 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5178605 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5203967 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5195920 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5185359 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5181740 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5178606 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5206197 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5208584 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5181730 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5200543 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL5185248 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5175626 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5199017 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5170248 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5190448 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL5188740 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5205344 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5181359 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5190798 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL5202303 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5195660 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5188985 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5179070 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL5173015 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL5181666 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5188372 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5176451 | — | IC50 | > | 100000.0 | nM | - |