Assay Detail
Binding
CHEMBL5325968
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal 6xHis-tagged human DNA polymerase eta (1 to 511 residues) expressed in Escherichia coli BL21 DE3 using 5'-IRD700-GCAGGTCGACTCCAAAG-3' primer/ 5'-TCGGTACCGGGTTAGCCTTTGGAGTCGACCTGC-3' template as DNA substrate incubated for 60 mins in presence of Mg2+ by bromophenol blue staining based assay
35
Total Activities
35
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
Computer-aided identification, synthesis, and biological evaluation of DNA polymerase η inhibitors for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 4.65 | 5.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL457821 | — | — | 1 | 5.30 |
| CHEMBL5398631 | — | — | 1 | 5.11 |
| CHEMBL243677 | — | — | 1 | 5.06 |
| CHEMBL1277701 | — | — | 1 | 4.99 |
| CHEMBL163316 | 3-O-METHYLQUERCETIN | — | 1 | 4.97 |
| CHEMBL8260 | BAICALEIN | 2.0 | 1 | 4.93 |
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 4.90 |
| CHEMBL150 | KAEMPFEROL | 1.0 | 1 | 4.90 |
| CHEMBL5418159 | — | — | 1 | 4.86 |
| CHEMBL117 | CHRYSIN | — | 1 | 4.83 |
| CHEMBL5272459 | — | — | 1 | 4.83 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 4.80 |
| CHEMBL165064 | ISOKAEMPFERIDE | — | 1 | 4.79 |
| CHEMBL28 | APIGENIN | — | 1 | 4.65 |
| CHEMBL5279962 | — | — | 1 | 4.58 |
| CHEMBL301624 | — | — | 1 | 4.57 |
| CHEMBL222556 | — | — | 1 | 4.52 |
| CHEMBL3326852 | — | — | 1 | 4.47 |
| CHEMBL3326854 | — | — | 1 | 4.21 |
| CHEMBL5280903 | — | — | 1 | 4.07 |
| CHEMBL5284680 | — | — | 1 | 4.06 |
| CHEMBL5271510 | — | — | 1 | 4.06 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 4.03 |
| CHEMBL5440374 | — | — | 1 | 4.01 |
| CHEMBL594248 | — | — | 1 | - |
| CHEMBL5403947 | — | — | 1 | - |
| CHEMBL5411625 | — | — | 1 | - |
| CHEMBL5419567 | — | — | 1 | - |
| CHEMBL5435484 | — | — | 1 | - |
| CHEMBL5409887 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL457821 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5398631 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL243677 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL1277701 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL163316 | 3-O-METHYLQUERCETIN | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL8260 | BAICALEIN | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL150 | KAEMPFEROL | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL5418159 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL117 | CHRYSIN | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL5272459 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL50 | QUERCETIN | IC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL165064 | ISOKAEMPFERIDE | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL28 | APIGENIN | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL5279962 | — | IC50 | = | 26500.0 | nM | 4.58 |
| CHEMBL301624 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL222556 | — | IC50 | = | 30500.0 | nM | 4.52 |
| CHEMBL3326852 | — | IC50 | = | 33500.0 | nM | 4.47 |
| CHEMBL3326854 | — | IC50 | = | 62400.0 | nM | 4.21 |
| CHEMBL5280903 | — | IC50 | = | 84600.0 | nM | 4.07 |
| CHEMBL5284680 | — | IC50 | = | 87500.0 | nM | 4.06 |
| CHEMBL5271510 | — | IC50 | = | 87100.0 | nM | 4.06 |
| CHEMBL44 | GENISTEIN | IC50 | = | 92400.0 | nM | 4.03 |
| CHEMBL5440374 | — | IC50 | = | 98300.0 | nM | 4.01 |
| CHEMBL228623 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5284676 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5281399 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL226507 | SINENSETIN | IC50 | > | 100000.0 | nM | - |
| CHEMBL5418637 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5409887 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5435484 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5419567 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5411625 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5403947 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL594248 | — | IC50 | > | 100000.0 | nM | - |