Assay Detail
Binding
CHEMBL3829689
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to CDK8 (unknown origin) expressed in human 7dF3 cells preincubated for 2 hrs followed by beta-oestradiol addition measured after 24 hrs by luciferase reporter gene assay
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 7dF3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.69 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3827983 | — | — | 1 | 9.70 |
| CHEMBL3828116 | — | — | 1 | 9.30 |
| CHEMBL3828003 | — | — | 1 | 9.22 |
| CHEMBL3827327 | — | — | 1 | 8.96 |
| CHEMBL3828637 | — | — | 1 | 8.77 |
| CHEMBL3827799 | — | — | 1 | 8.70 |
| CHEMBL3827118 | — | — | 1 | 8.60 |
| CHEMBL3827774 | — | — | 1 | 8.47 |
| CHEMBL3828458 | — | — | 1 | 8.38 |
| CHEMBL3828209 | — | — | 1 | 8.34 |
| CHEMBL3828503 | — | — | 1 | 8.33 |
| CHEMBL3828221 | — | — | 1 | 8.33 |
| CHEMBL3828071 | — | — | 1 | 8.24 |
| CHEMBL3828553 | — | — | 1 | 8.14 |
| CHEMBL3827678 | — | — | 1 | 8.14 |
| CHEMBL3827023 | — | — | 1 | 8.09 |
| CHEMBL3827664 | — | — | 1 | 8.05 |
| CHEMBL3828286 | — | — | 1 | 8.01 |
| CHEMBL3828523 | — | — | 1 | 8.00 |
| CHEMBL3828084 | — | — | 1 | 7.97 |
| CHEMBL3828575 | — | — | 1 | 7.95 |
| CHEMBL3827053 | — | — | 1 | 7.90 |
| CHEMBL3828572 | — | — | 1 | 7.80 |
| CHEMBL3828370 | — | — | 1 | 7.80 |
| CHEMBL3827944 | — | — | 1 | 7.76 |
| CHEMBL3827904 | — | — | 1 | 7.75 |
| CHEMBL3828689 | — | — | 1 | 7.71 |
| CHEMBL3827874 | — | — | 1 | 7.70 |
| CHEMBL3827758 | — | — | 1 | 7.68 |
| CHEMBL3827586 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3827983 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3828116 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3828003 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3827327 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3828637 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3827799 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3827118 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3827774 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3828458 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3828209 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3828503 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3828221 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3828071 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3827678 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3828553 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3827023 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3827664 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3828286 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL3828523 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL3828084 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL3828575 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL3827053 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL3828572 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3828370 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3827944 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL3827904 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL3828689 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL3827874 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL3827758 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3827586 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL3827605 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3828120 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL3827470 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3827699 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3828266 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL3827333 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3827150 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3827673 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3828470 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3827675 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3828310 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3828129 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3827790 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3828169 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL3828472 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL3827482 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3827749 | — | IC50 | = | 1232.0 | nM | 5.91 |
| CHEMBL3827666 | — | IC50 | = | 1418.0 | nM | 5.85 |
| CHEMBL3828430 | — | IC50 | = | 1946.0 | nM | 5.71 |
| CHEMBL3827683 | — | IC50 | = | 2554.0 | nM | 5.59 |