Assay Detail
Binding
CHEMBL4031182
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cGAS in human THP1 cells assessed as reduction in salmon sperm dsDNA-induced IFN-beta expression preincubated for 1 hr followed by dsDNA stimulation for 12 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 4 | - | - |
| IC50 | 1 | 7.22 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL577784 | BX-795 | — | 1 | 7.22 |
| CHEMBL4096573 | — | — | 1 | - |
| CHEMBL4084664 | — | — | 1 | - |
| CHEMBL4062994 | — | — | 1 | - |
| CHEMBL4103560 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL577784 | BX-795 | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4096573 | — | Inhibition | - | % | - | |
| CHEMBL4084664 | — | Inhibition | - | % | - | |
| CHEMBL4062994 | — | Inhibition | - | % | - | |
| CHEMBL4103560 | — | Inhibition | - | % | - |