Assay Detail
Binding
CHEMBL5048469
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NF kappa B dependent CDK8/CDK19 in HEK293 cell incubated for 3 hrs in presence of TNF-alpha by Spectra max microtitre plate reader
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.74 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4878072 | — | — | 1 | 7.25 |
| CHEMBL5077066 | — | — | 1 | 7.09 |
| CHEMBL4076837 | SENEXIN B | 1.0 | 1 | 6.96 |
| CHEMBL4856755 | — | — | 1 | 6.95 |
| CHEMBL5087807 | — | — | 1 | 6.93 |
| CHEMBL4868007 | — | — | 1 | 6.91 |
| CHEMBL5094334 | — | — | 1 | 6.86 |
| CHEMBL5083266 | — | — | 1 | 6.86 |
| CHEMBL5087015 | — | — | 1 | 6.80 |
| CHEMBL5086592 | — | — | 1 | 6.74 |
| CHEMBL5091221 | — | — | 1 | 6.68 |
| CHEMBL5080406 | — | — | 1 | 6.61 |
| CHEMBL4855789 | — | — | 1 | 6.60 |
| CHEMBL4851694 | — | — | 1 | 6.50 |
| CHEMBL4226806 | — | — | 1 | 6.46 |
| CHEMBL4863646 | — | — | 1 | 6.38 |
| CHEMBL5094174 | — | — | 1 | 6.06 |
| CHEMBL4875076 | — | — | 1 | - |
| CHEMBL5093671 | — | — | 1 | - |
| CHEMBL4857688 | — | — | 1 | - |
| CHEMBL5088692 | — | — | 1 | - |
| CHEMBL5081291 | — | — | 1 | - |
| CHEMBL5078784 | — | — | 1 | - |
| CHEMBL4857902 | — | — | 1 | - |
| CHEMBL4871564 | — | — | 1 | - |
| CHEMBL5080239 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4878072 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5077066 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4076837 | SENEXIN B | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4856755 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5087807 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4868007 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL5094334 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5083266 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5087015 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5086592 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL5091221 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL5080406 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4855789 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL4851694 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL4226806 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL4863646 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL5094174 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4875076 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5093671 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4857688 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5088692 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5081291 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5078784 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4857902 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4871564 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5080239 | — | IC50 | > | 5000.0 | nM | - |