Assay Detail
Binding
CHEMBL5548207
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cGAS in dsDNA activated mouse RAW-Lucia ISG cells preincubated for 1 hr followed by cGAMP addition and measured after 24 hrs by luminescence based QUANTI-Luc assay
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | RAW-Lucia ISG |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Pharmacological Evaluation of Spiro[carbazole-3,3'-pyrrolidine] Derivatives as cGAS Inhibitors for Treatment of Acute Lung Injury.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.16 | 5.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5573599 | — | — | 1 | 5.99 |
| CHEMBL5575511 | — | — | 1 | 5.50 |
| CHEMBL5571941 | — | — | 1 | 5.33 |
| CHEMBL5583962 | — | — | 1 | 5.06 |
| CHEMBL5570975 | — | — | 1 | 5.05 |
| CHEMBL5574373 | — | — | 2 | 5.05 |
| CHEMBL5569271 | — | — | 1 | 4.94 |
| CHEMBL5082056 | — | — | 2 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5573599 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5575511 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5571941 | — | IC50 | = | 4710.0 | nM | 5.33 |
| CHEMBL5583962 | — | IC50 | = | 8690.0 | nM | 5.06 |
| CHEMBL5570975 | — | IC50 | = | 8910.0 | nM | 5.05 |
| CHEMBL5574373 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5574373 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5569271 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL5082056 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL5082056 | — | IC50 | = | 14640.0 | nM | 4.83 |