Assay Detail
Binding
CHEMBL5737112
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Comparison of the Effect of Corticosteroids, a ROCK Kinase and Compounds of the Invention on the Inhibition of ROCK-1 Kinase, ROCK-2 Kinase, and TNF-alpha: The TNFα assay quantifies secreted TNFα from RAW264.7 immortalized murine macrophages as an indicator of inflammation. The cells were concurrently treated with LPS (as an inducer of inflammation) and a titration of test molecules or control compounds for 4 hrs. After the incubation period, the media was harvested and assayed via an ELISA assay. ODs of experimental samples are fit to those of a standard curve to extrapolate the TNFα concentration. IC50 values were calculated by fitting a curve to experimental values with the controls as the top and bottom limits of the curve.
21
Total Activities
7
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isoquinoline-steroid conjugates and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.85 | 5.59 |
| kon | 7 | - | - |
| k_off | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5992697 | — | — | 3 | 5.59 |
| CHEMBL5842146 | — | — | 3 | 5.11 |
| CHEMBL5867395 | — | — | 3 | 4.93 |
| CHEMBL5814965 | — | — | 3 | 4.75 |
| CHEMBL5854473 | — | — | 3 | 4.67 |
| CHEMBL5922741 | — | — | 3 | 4.52 |
| CHEMBL5916377 | — | — | 3 | 4.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5992697 | — | IC50 | = | 2573.0 | nM | 5.59 |
| CHEMBL5842146 | — | IC50 | = | 7729.0 | nM | 5.11 |
| CHEMBL5867395 | — | IC50 | = | 11632.0 | nM | 4.93 |
| CHEMBL5814965 | — | IC50 | = | 17730.0 | nM | 4.75 |
| CHEMBL5854473 | — | IC50 | = | 21390.0 | nM | 4.67 |
| CHEMBL5922741 | — | IC50 | = | 30082.0 | nM | 4.52 |
| CHEMBL5916377 | — | IC50 | = | 43246.0 | nM | 4.36 |
| CHEMBL5814965 | — | kon | = | - | — | - |
| CHEMBL5814965 | — | k_off | = | - | s-1 | - |
| CHEMBL5854473 | — | kon | = | - | — | - |
| CHEMBL5854473 | — | k_off | = | - | s-1 | - |
| CHEMBL5842146 | — | kon | = | - | — | - |
| CHEMBL5842146 | — | k_off | = | - | s-1 | - |
| CHEMBL5916377 | — | k_off | = | - | s-1 | - |
| CHEMBL5922741 | — | kon | = | - | — | - |
| CHEMBL5922741 | — | k_off | = | - | s-1 | - |
| CHEMBL5867395 | — | kon | = | - | — | - |
| CHEMBL5867395 | — | k_off | = | - | s-1 | - |
| CHEMBL5992697 | — | kon | = | - | — | - |
| CHEMBL5992697 | — | k_off | = | - | s-1 | - |
| CHEMBL5916377 | — | kon | = | - | — | - |