Assay Detail
Binding
CHEMBL4029489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK8 in human SW620 cells assessed as decrease in STAT1 phosphorylation at Ser727 after 2 hrs by Western blot method
36
Total Activities
36
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
Design and synthesis of selective CDK8/19 dual inhibitors: Discovery of 4,5-dihydrothieno[3',4':3,4]benzo[1,2-d]isothiazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 7.64 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071040 | — | — | 1 | 9.46 |
| CHEMBL4086487 | — | — | 1 | 9.40 |
| CHEMBL4061525 | — | — | 1 | 9.24 |
| CHEMBL4083552 | — | — | 1 | 9.11 |
| CHEMBL4066819 | — | — | 1 | 8.89 |
| CHEMBL4060856 | — | — | 1 | 8.85 |
| CHEMBL4077627 | — | — | 1 | 8.82 |
| CHEMBL4070408 | — | — | 1 | 8.70 |
| CHEMBL4074204 | — | — | 1 | 8.64 |
| CHEMBL4076395 | — | — | 1 | 8.59 |
| CHEMBL4062244 | — | — | 1 | 8.52 |
| CHEMBL4091345 | — | — | 1 | 8.52 |
| CHEMBL4090775 | — | — | 1 | 8.13 |
| CHEMBL4088931 | — | — | 1 | 8.08 |
| CHEMBL4082469 | — | — | 1 | 8.05 |
| CHEMBL4069854 | — | — | 1 | 8.04 |
| CHEMBL4060714 | — | — | 1 | 7.80 |
| CHEMBL4063680 | — | — | 1 | 7.68 |
| CHEMBL4063358 | — | — | 1 | 7.60 |
| CHEMBL4072372 | — | — | 1 | 7.55 |
| CHEMBL4061783 | — | — | 1 | 7.18 |
| CHEMBL4102907 | — | — | 1 | 7.16 |
| CHEMBL4062262 | — | — | 1 | 6.85 |
| CHEMBL4069269 | — | — | 1 | 6.70 |
| CHEMBL4097047 | — | — | 1 | 6.66 |
| CHEMBL4082699 | — | — | 1 | 6.31 |
| CHEMBL4060582 | — | — | 1 | 6.26 |
| CHEMBL4084957 | — | — | 1 | 6.21 |
| CHEMBL4065027 | — | — | 1 | 6.05 |
| CHEMBL4090315 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071040 | — | EC50 | = | 0.35 | nM | 9.46 |
| CHEMBL4086487 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4061525 | — | EC50 | = | 0.58 | nM | 9.24 |
| CHEMBL4083552 | — | EC50 | = | 0.77 | nM | 9.11 |
| CHEMBL4066819 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4060856 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4077627 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4070408 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4074204 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4076395 | — | EC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4062244 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4091345 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4090775 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4088931 | — | EC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4082469 | — | EC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4069854 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4060714 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4063680 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4063358 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4072372 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4061783 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4102907 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4062262 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4069269 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4097047 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4082699 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4060582 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4084957 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4065027 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4090315 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4092709 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4083979 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4073611 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4100438 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4059564 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4091219 | — | EC50 | > | 10000.0 | nM | - |